An agent derived from licorice root. It is used for the treatment of digestive tract ulcers, especially in the stomach. Antidiuretic side effects are frequent, but otherwise the drug is low in toxicity.
A genus of leguminous herbs or shrubs whose roots yield GLYCYRRHETINIC ACID and its derivative, CARBENOXOLONE.
An oleanolic acid from GLYCYRRHIZA that has some antiallergic, antibacterial, and antiviral properties. It is used topically for allergic or infectious skin inflammation and orally for its aldosterone effects in electrolyte regulation.
Connections between cells which allow passage of small molecules and electric current. Gap junctions were first described anatomically as regions of close apposition between cells with a narrow (1-2 nm) gap between cell membranes. The variety in the properties of gap junctions is reflected in the number of CONNEXINS, the family of proteins which form the junctions.
Hydroxysteroid dehydrogenases that catalyzes the reversible conversion of CORTISOL to the inactive metabolite CORTISONE. Enzymes in this class can utilize either NAD or NADP as cofactors.
Triterpenes are a class of naturally occurring compounds consisting of six isoprene units arranged to form a 30-carbon skeleton, often found in plants and some animals, with various bioactivities including anti-inflammatory, antiviral, and cytotoxic properties.
Enzymes of the oxidoreductase class that catalyze the dehydrogenation of hydroxysteroids. (From Enzyme Nomenclature, 1992) EC 1.1.-.
A class of compounds composed of repeating 5-carbon units of HEMITERPENES.
Plants whose roots, leaves, seeds, bark, or other constituent parts possess therapeutic, tonic, purgative, curative or other pharmacologic attributes, when administered to man or animals.
A low-affinity 11 beta-hydroxysteroid dehydrogenase found in a variety of tissues, most notably in LIVER; LUNG; ADIPOSE TISSUE; vascular tissue; OVARY; and the CENTRAL NERVOUS SYSTEM. The enzyme acts reversibly and can use either NAD or NADP as cofactors.
Isomeric forms and derivatives of octanol (C8H17OH).
Ulceration of the GASTRIC MUCOSA due to contact with GASTRIC JUICE. It is often associated with HELICOBACTER PYLORI infection or consumption of nonsteroidal anti-inflammatory drugs (NSAIDS).
A group of homologous proteins which form the intermembrane channels of GAP JUNCTIONS. The connexins are the products of an identified gene family which has both highly conserved and highly divergent regions. The variety contributes to the wide range of functional properties of gap junctions.
A naturally occurring glucocorticoid. It has been used in replacement therapy for adrenal insufficiency and as an anti-inflammatory agent. Cortisone itself is inactive. It is converted in the liver to the active metabolite HYDROCORTISONE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p726)
A 43-kDa peptide which is a member of the connexin family of gap junction proteins. Connexin 43 is a product of a gene in the alpha class of connexin genes (the alpha-1 gene). It was first isolated from mammalian heart, but is widespread in the body including the brain.
A PEPTIC ULCER located in the DUODENUM.
A heterogeneous group of drugs used to produce muscle relaxation, excepting the neuromuscular blocking agents. They have their primary clinical and therapeutic uses in the treatment of muscle spasm and immobility associated with strains, sprains, and injuries of the back and, to a lesser degree, injuries to the neck. They have been used also for the treatment of a variety of clinical conditions that have in common only the presence of skeletal muscle hyperactivity, for example, the muscle spasms that can occur in MULTIPLE SCLEROSIS. (From Smith and Reynard, Textbook of Pharmacology, 1991, p358)
A thiazide diuretic with actions and uses similar to those of HYDROCHLOROTHIAZIDE. It has been used in the treatment of familial hyperkalemia, hypertension, edema, and urinary tract disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p810)
A condition caused by the overproduction of ALDOSTERONE. It is characterized by sodium retention and potassium excretion with resultant HYPERTENSION and HYPOKALEMIA.
The narrow subcapsular outer zone of the adrenal cortex. This zone produces a series of enzymes that convert PREGNENOLONE to ALDOSTERONE. The final steps involve three successive oxidations by CYTOCHROME P-450 CYP11B2.
A hormone secreted by the ADRENAL CORTEX that regulates electrolyte and water balance by increasing the renal retention of sodium and the excretion of potassium.
The outer layer of the adrenal gland. It is derived from MESODERM and comprised of three zones (outer ZONA GLOMERULOSA, middle ZONA FASCICULATA, and inner ZONA RETICULARIS) with each producing various steroids preferentially, such as ALDOSTERONE; HYDROCORTISONE; DEHYDROEPIANDROSTERONE; and ANDROSTENEDIONE. Adrenal cortex function is regulated by pituitary ADRENOCORTICOTROPIN.
A group of CORTICOSTEROIDS primarily associated with water and electrolyte balance. This is accomplished through the effect on ION TRANSPORT in renal tubules, resulting in retention of sodium and loss of potassium. Mineralocorticoid secretion is itself regulated by PLASMA VOLUME, serum potassium, and ANGIOTENSIN II.
A pair of glands located at the cranial pole of each of the two KIDNEYS. Each adrenal gland is composed of two distinct endocrine tissues with separate embryonic origins, the ADRENAL CORTEX producing STEROIDS and the ADRENAL MEDULLA producing NEUROTRANSMITTERS.
Cytoplasmic proteins that specifically bind MINERALOCORTICOIDS and mediate their cellular effects. The receptor with its bound ligand acts in the nucleus to induce transcription of specific segments of DNA.

Corticosteroid-dependent sodium transport in a novel immortalized mouse collecting duct principal cell line. (1/219)

The final control of sodium balance takes place in the cortical collecting duct (CCD) of the nephron, where corticosteroid hormones regulate sodium reabsorption by acting through mineralocorticoid (MR) and/or glucocorticoid (GR) receptors. A clone of principal CCD cells (mpkCCDc14) has been established that is derived from a transgenic mouse (SV40 large T antigen under the control of the SV40 enhancer/L-type pyruvate kinase promoter). Cells grown on filters form polarized monolayers with high electrical transepithelial resistance (R(T) approximately 4700 ohm x cm2) and potential difference (P(D) approximately -50 mV) and have an amiloride-sensitive electrogenic sodium transport, as assessed by the short-circuit current method (Isc approximately 11 microA/cm2). Reverse transcription-PCR experiments using rat MR primers, [3H]aldosterone, and [3H]dexamethasone binding and competition studies indicated that the mpkCCDc14 cells exhibit specific MR and GR. Aldosterone increased Isc in a dose- (10(-10) to 10(-6) M) and time-dependent (2 to 72 h) manner, whereas corticosterone only transiently increased Isc (2 to 6 h). Consistent with the expression of 11beta-hydroxysteroid dehydrogenase type 2, which metabolizes glucocorticoids to inactive 11-dehydroderivates, carbenoxolone potentiated the corticosterone-stimulated Isc. Aldosterone (5x10(-7) M)-induced Isc (fourfold) was associated with a three- to fivefold increase in alpha-ENaC mRNA (but not in those for beta- or gamma-ENaC) and three- to 10-fold increases in alpha-ENaC protein synthesis. In conclusion, this new immortalized mammalian CCD clonal cell line has retained a high level of epithelial differentiation and sodium transport stimulated by aldosterone and therefore represents a useful mammalian cell system for identifying the genes controlled by aldosterone.  (+info)

Regulation of 11beta-hydroxysteroid dehydrogenase type 2 by diuretics and the renin-angiotensin-aldosterone axis. (2/219)

In the kidney and colon 11beta-hydroxysteroid dehydrogenase type 2 (11beta-HSD2) inactivates cortisol to cortisone, thereby protecting the non-selective mineralocorticoid receptor from cortisol. Deficiency of 11beta-HSD2 results in cortisol-mediated sodium retention and hypertension, suggesting that the physiological regulation of 11beta-HSD2 in mineralocorticoid target tissues may be important in modulating sodium homoeostasis and blood pressure control. Using the human epithelial colon cell line SW-620, reverse transcriptase-polymerase chain reaction and enzyme kinetic analysis indicated expression of only 11beta-HSD2 (Km for cortisol 66 nmol/l). Bradykinin (10(-8) to 10(-12) mol/l), frusemide (10(-4) to 10(-9) mol/l), benzamiloride hydrochloride (10(-5) to 10(-10) mol/l) and atrial natriuretic peptide (10(-6) to 10(-10) mol/l) had no effect on 11beta-HSD2 expression. Using a range of concentrations of angiotensin II (2x10(-8) to 2x10(-5) mol/l) a significant reduction in activity was seen but only at supra-physiological concentrations, [e.g. 2x10(-6) mol/l at 4 h pretreatment: 36.7+/-2.0 pmol cortisone. h-1.mg-1 (mean+/-S.E.M.) compared with 45.1+/-1.7 pmol.h-1.mg-1 in control; P<0.05]. The angiotensin-converting enzyme inhibitors captopril, enalapril, lisinopril, perindopril, quinapril and trandolapril at 10(-7) mol/l, but not fosinopril, significantly increased 11beta-HSD2 activity after pretreatment for 16 or 24 h (P<0.05-P<0.01 compared with control). No effects were seen at 4 h pretreatment. Hydrochlorothiazide (10(-7) mol/l) significantly decreased 11beta-HSD2 activity (P<0.05 compared with control) at 4 h pretreatment. Commonly used diuretics, atrial natriuretic peptide and physiological concentrations of angiotensin II and bradykinin do not alter 11beta-HSD2 activity. In contrast, a series of angiotensin-converting enzyme inhibitors significantly increase 11beta-HSD2 activity in vitro. This may explain how intrarenal infusions of angiotensin-converting enzyme inhibitors increase renal sodium excretion independent of circulating concentrations of angiotensin II. The interaction between angiotensin-converting enzyme inhibitors and 11beta-HSD2 may be an additional mechanism by which the former can lower blood pressure.  (+info)

Role of gap junctions in the responses to EDHF in rat and guinea-pig small arteries. (3/219)

1. In guinea-pig internal carotid arteries with an intact endothelium, acetylcholine (10 microM) and levcromakalim (10 microM) each hyperpolarized the smooth muscle whereas a 5 mM elevation of extracellular K(+) was without effect. 2. Incubation of the carotid artery with the gap junction inhibitors carbenoxolone (100 microM) or gap 27 (500 microM) essentially abolished the hyperpolarization to acetylcholine but it was without effect on that to levcromakalim. Carbenoxolone had no effect on the acetylcholine-induced endothelial cell hyperpolarization but inhibited the smooth muscle hyperpolarization induced by the endothelial cell K(+) channel opener, 1-ethyl-2-benzimidazolinone (600 microM). 3. In rat hepatic and mesenteric arteries with endothelium, carbenoxolone (100 or 500 microM) depolarized the smooth muscle but did not modify hyperpolarizations induced by KCl or levcromakalim. In the mesenteric (but not the hepatic) artery, the acetylcholine-induced hyperpolarization was inhibited by carbenoxolone. 4. Phenylephrine (1 microM) depolarized the smooth muscle cells of intact hepatic and mesenteric arteries, an effect enhanced by carbenoxolone. Gap 27 did not have a depolarizing action. In the presence of phenylephrine, acetylcholine-induced hyperpolarization of both hepatic and mesenteric artery myocytes was partially inhibited by each of the gap junction inhibitors. 5. Collectively, the data suggest that gap junctions play some role in the EDHF (endothelium-derived hyperpolarizing factor) response in rat hepatic and mesenteric arteries. However, in the guinea-pig internal carotid artery, electrotonic propagation of endothelial cell hyperpolarizations via gap junctions may be the sole mechanism underlying the response previously attributed to EDHF.  (+info)

Precision of the pacemaker nucleus in a weakly electric fish: network versus cellular influences. (4/219)

We investigated the relative influence of cellular and network properties on the extreme spike timing precision observed in the medullary pacemaker nucleus (Pn) of the weakly electric fish Apteronotus leptorhynchus. Of all known biological rhythms, the electric organ discharge of this and related species is the most temporally precise, with a coefficient of variation (CV = standard deviation/mean period) of 2 x 10(-4) and standard deviation (SD) of 0.12-1.0 micros. The timing of the electric organ discharge is commanded by neurons of the Pn, individual cells of which we show in an in vitro preparation to have only a slightly lesser degree of precision. Among the 100-150 Pn neurons, dye injection into a pacemaker cell resulted in dye coupling in one to five other pacemaker cells and one to three relay cells, consistent with previous results. Relay cell fills, however, showed profuse dendrites and contacts never seen before: relay cell dendrites dye-coupled to one to seven pacemaker and one to seven relay cells. Moderate (0.1-10 nA) intracellular current injection had no effect on a neuron's spiking period, and only slightly modulated its spike amplitude, but could reset the spike phase. In contrast, massive hyperpolarizing current injections (15-25 nA) could force the cell to skip spikes. The relative timing of subthreshold and full spikes suggested that at least some pacemaker cells are likely to be intrinsic oscillators. The relative amplitudes of the subthreshold and full spikes gave a lower bound to the gap junctional coupling coefficient of 0.01-0.08. Three drugs, called gap junction blockers for their mode of action in other preparations, caused immediate and substantial reduction in frequency, altered the phase lag between pairs of neurons, and later caused the spike amplitude to drop, without altering the spike timing precision. Thus we conclude that the high precision of the normal Pn rhythm does not require maximal gap junction conductances between neurons that have ordinary cellular precision. Rather, the spiking precision can be explained as an intrinsic cellular property while the gap junctions act to frequency- and phase-lock the network oscillations.  (+info)

11 beta-hydroxysteroid dehydrogenase type 1 is a predominant 11 beta-reductase in the intact perfused rat liver. (5/219)

11 beta-Hydroxysteroid dehydrogenase type 1 (11 beta-HSD-1), a regulator of intrahepatocellular glucocorticoid activity, is bidirectional in homogenates but catalyses 11 beta-reduction (regenerating glucocorticoid) in intact primary hepatocytes in culture. To examine this discrepancy at the whole-organ level, we examined 11 beta-HSD-1 activity in the intact bivascularly perfused rat liver. On a single pass through male rat liver, 44+/-5% of 11-dehydrocorticosterone (11-DHC) recovered was 11 beta-reduced to corticosterone, whereas 10+/-1% of corticosterone was 11 beta-dehydrogenated to 11-DHC. 11 beta-Reduction was less in female liver (21+/-2%, P<0.01) and was significantly greater with perfusion of all substrate via the portal vein (50+/-3%) than via the hepatic artery (30+/-2%, P<0.05). 11 beta-Reductase activity was not saturated by 11-DHC (10(-)(9)-10(-)(6) M). Perfusion with carbenoxolone (CBX, 10(-)(6)-10(-)(3 )M) did not alter 11 beta-reduction of 11-DHC. In contrast, pretreatment with CBX in vivo (10 mg/day) for 7 days inhibited 11 beta-reductase (19+/-4% conversion, P<0.01). Concentrations of 11-DHC in male rat plasma were 44+/-6 nM. Thus 11 beta-HSD-1 is predominantly an 11 beta-reductase in the intact rat liver and is only inhibited by chronic administration of CBX. The substantial concentrations of plasma 11-DHC as substrate suggest that 11 beta-HSD-1 activity and its potential selective inhibition could modify glucocorticoid action in vivo.  (+info)

Type 1 11beta -hydroxysteroid dehydrogenase mediates glucocorticoid activation and insulin release in pancreatic islets. (6/219)

Metabolic transformation of glucocorticoid hormones constitutes a determinant of their cell-specific effects. The most important reaction for this class of steroids is the reversible C11 keto/beta-hydroxyl conversion between receptor-binding 11beta-OH steroids and the nonbinding 11-oxo compounds, carried out by 11beta-hydroxysteroid dehydrogenases (11beta-HSDs). In this study, we determined the role of glucocorticoid conversion by 11beta-HSD in pancreatic islets and its function in the regulation of insulin release. Pancreatic islets isolated from ob/ob mice display type 1 11beta-hydroxysteroid dehydrogenase activity, i.e. in intact cells the reductive reaction prevails, leading from dehydrocorticosterone to corticosterone. Expression of type 1 11beta-HSD mRNA was detected by reverse transcriptase-polymerase chain reaction in islets isolated from ob/ob mice and also from human tissue. Incubation of beta-cells in the presence of 11-dehydrocorticosterone leads to a dose-dependent inhibition of insulin release, indicating cellular activation of 11-dehydrocorticosterone to the receptor ligand, further confirmed by reporter gene assays. Inhibition of 11beta-HSD activity by carbenoxolone reverses inhibition of insulin release. The presence of 11beta-HSD in islets supports the concept that reactivation of inert circulating hormone precursors in a cell-specific manner plays a major role in glucocorticoid physiology in rodents and man.  (+info)

Apoptosis in rat placenta is zone-dependent and stimulated by glucocorticoids. (7/219)

Apoptosis, or physiological cell death, is elevated in the placenta of human pregnancies complicated by fetal growth retardation, suggesting that placental apoptosis may be a key factor in the overall control of feto-placental growth. The present study used DNA internucleosomal fragmentation analysis to characterize apoptosis in the two morphologically and functionally distinct regions of the rat placenta, the basal and labyrinth zones, during the last week of pregnancy (Days 16, 22, and 23). In addition, because glucocorticoids are potent inhibitors of feto-placental growth and can stimulate apoptosis in other tissues, we examined whether dexamethasone treatment in vivo induces placental apoptosis. DNA fragmentation was clearly evident in both placental zones at each stage of pregnancy, with higher levels evident in the basal zone compared with the labyrinth zone on Days 22 and 23. TUNEL analysis, which identifies dying cells in situ, demonstrated positive staining of cells in the basal zone, particularly giant trophoblast cells. Dexamethasone treatment increased DNA fragmentation in the basal zone but not the labyrinth zone. Similarly, maternal treatment with carbenoxolone, which can enhance local concentrations of endogenous glucocorticoid by inhibition of 11 beta-hydroxysteroid dehydrogenase, also increased DNA fragmentation in the basal zone but not in the labyrinth zone. These effects of dexamethasone and carbenoxolone on placental apoptosis were associated with reduced placental and fetal weights. In conclusion, this study shows that apoptosis occurs in both zones of the rat placenta, particularly in the basal zone near term, and is elevated after increased glucocorticoid exposure in vivo. These data support the hypothesis that placental apoptosis is an important player in the regulation of feto-placental growth, and establish the rat as a useful model to study the endocrine control of placental apoptosis.  (+info)

Electrical coupling and excitatory synaptic transmission between rhythmogenic respiratory neurons in the preBotzinger complex. (8/219)

Breathing pattern is postulated to be generated by brainstem neurons. However, determination of the underlying cellular mechanisms, and in particular the synaptic interactions between respiratory neurons, has been difficult. Here we used dual recordings from two distinct populations of brainstem respiratory neurons, hypoglossal (XII) motoneurons, and rhythmogenic (type-1) neurons in the preBotzinger complex (preBotC), the hypothesized site for respiratory rhythm generation, to determine whether electrical and chemical transmission is present. Using an in vitro brainstem slice preparation from newborn mice, we found that intracellularly recorded pairs of XII motoneurons and pairs of preBotC inspiratory type-1 neurons showed bidirectional electrical coupling. Coupling strength was low (<0.10), and the current that passed between two neurons was heavily filtered (corner frequency, <10 Hz). Dual recordings also demonstrated unidirectional excitatory chemical transmission (EPSPs of approximately 3 mV) between type-1 neurons. These data indicate that respiratory motor output from the brainstem involves gap junction-mediated current transfer between motoneurons. Furthermore, bidirectional electrical coupling and unidirectional excitatory chemical transmission are present between type-1 neurons in the preBotC and may be important for generation or modulation of breathing rhythm.  (+info)

Carbenoxolone is a synthetic derivative of glycyrrhizin, which is found in the root of the licorice plant. It has been used in the treatment of gastric and duodenal ulcers due to its ability to increase the mucosal resistance and promote healing. Carbenoxolone works by inhibiting the enzyme 11-beta-hydroxysteroid dehydrogenase, which leads to an increase in the levels of cortisol and other steroids in the body. This can have various effects on the body, including anti-inflammatory and immunosuppressive actions.

However, long-term use of carbenoxolone has been associated with serious side effects such as hypertension, hypokalemia (low potassium levels), and edema (fluid retention). Therefore, its use is generally limited to short-term treatment of gastric and duodenal ulcers.

Medical Definition: Carbenoxolone

A synthetic derivative of glycyrrhizin, used in the treatment of gastric and duodenal ulcers due to its ability to increase mucosal resistance and promote healing. It is an inhibitor of 11-beta-hydroxysteroid dehydrogenase, leading to increased levels of cortisol and other steroids in the body, with potential anti-inflammatory and immunosuppressive effects. However, long-term use is associated with serious side effects such as hypertension, hypokalemia, and edema.

"Glycyrrhiza" is the medical term for the licorice plant (Glycyrrhiza glabra), which belongs to the legume family. The root of this plant contains glycyrrhizin, a sweet-tasting compound that has been used in traditional medicine for various purposes such as treating coughs, stomach ulcers, and liver disorders. However, excessive consumption of glycyrrhizin can lead to serious side effects like high blood pressure, low potassium levels, and even heart problems. Therefore, it is important to use licorice products under the guidance of a healthcare professional.

Glycyrrhetinic acid is defined medically as a pentacyclic triterpenoid derived from glycyrrhizin, which is found in the root of licorice plants. It has been used in traditional medicine for its anti-inflammatory and expectorant properties.

Glycyrrhetinic acid works by inhibiting the enzyme 11-beta-hydroxysteroid dehydrogenase, which is responsible for converting cortisol to cortisone. This can lead to increased levels of cortisol in the body, which can have various effects, including lowering potassium levels and increasing sodium levels, leading to fluid retention and high blood pressure in some individuals.

In addition to its use in traditional medicine, glycyrrhetinic acid has been studied for its potential benefits in treating a variety of conditions, including cancer, HIV, and hepatitis. However, more research is needed to confirm these potential benefits and to fully understand the risks and side effects associated with its use.

Gap junctions are specialized intercellular connections that allow for the direct exchange of ions, small molecules, and electrical signals between adjacent cells. They are composed of arrays of channels called connexons, which penetrate the cell membranes of two neighboring cells and create a continuous pathway for the passage of materials from one cytoplasm to the other. Each connexon is formed by the assembly of six proteins called connexins, which are encoded by different genes and vary in their biophysical properties. Gap junctions play crucial roles in many physiological processes, including the coordination of electrical activity in excitable tissues, the regulation of cell growth and differentiation, and the maintenance of tissue homeostasis. Mutations or dysfunctions in gap junction channels have been implicated in various human diseases, such as cardiovascular disorders, neurological disorders, skin disorders, and cancer.

11-Beta-Hydroxysteroid dehydrogenases (11-β-HSDs) are a group of enzymes that play a crucial role in the metabolism of steroid hormones, particularly cortisol and cortisone, which belong to the class of glucocorticoids. These enzymes exist in two isoforms: 11-β-HSD1 and 11-β-HSD2.

1. 11-β-HSD1: This isoform is primarily located within the liver, adipose tissue, and various other peripheral tissues. It functions as a NADPH-dependent reductase, converting inactive cortisone to its active form, cortisol. This enzyme helps regulate glucocorticoid action in peripheral tissues, influencing glucose and lipid metabolism, insulin sensitivity, and inflammation.
2. 11-β-HSD2: This isoform is predominantly found in mineralocorticoid target tissues such as the kidneys, colon, and salivary glands. It functions as a NAD+-dependent dehydrogenase, converting active cortisol to its inactive form, cortisone. By doing so, it protects the mineralocorticoid receptor from being overstimulated by cortisol, ensuring aldosterone specifically binds and activates this receptor to maintain proper electrolyte and fluid balance.

Dysregulation of 11-β-HSDs has been implicated in several disease states, including metabolic syndrome, type 2 diabetes, hypertension, and psychiatric disorders. Therefore, understanding the function and regulation of these enzymes is essential for developing novel therapeutic strategies to treat related conditions.

Triterpenes are a type of natural compound that are composed of six isoprene units and have the molecular formula C30H48. They are synthesized through the mevalonate pathway in plants, fungi, and some insects, and can be found in a wide variety of natural sources, including fruits, vegetables, and medicinal plants.

Triterpenes have diverse structures and biological activities, including anti-inflammatory, antiviral, and cytotoxic effects. Some triterpenes are also used in traditional medicine, such as glycyrrhizin from licorice root and betulinic acid from the bark of birch trees.

Triterpenes can be further classified into various subgroups based on their carbon skeletons, including squalene, lanostane, dammarane, and ursane derivatives. Some triterpenes are also modified through various biochemical reactions to form saponins, steroids, and other compounds with important biological activities.

Hydroxysteroid dehydrogenases (HSDs) are a group of enzymes that play a crucial role in steroid hormone metabolism. They catalyze the oxidation and reduction reactions of hydroxyl groups on the steroid molecule, which can lead to the activation or inactivation of steroid hormones. HSDs are involved in the conversion of various steroids, including sex steroids (e.g., androgens, estrogens) and corticosteroids (e.g., cortisol, cortisone). These enzymes can be found in different tissues throughout the body, and their activity is regulated by various factors, such as hormones, growth factors, and cytokines. Dysregulation of HSDs has been implicated in several diseases, including cancer, diabetes, and cardiovascular disease.

Terpenes are a large and diverse class of organic compounds produced by a variety of plants, including cannabis. They are responsible for the distinctive aromas and flavors found in different strains of cannabis. Terpenes have been found to have various therapeutic benefits, such as anti-inflammatory, analgesic, and antimicrobial properties. Some terpenes may also enhance the psychoactive effects of THC, the main psychoactive compound in cannabis. It's important to note that more research is needed to fully understand the potential medical benefits and risks associated with terpenes.

Medicinal plants are defined as those plants that contain naturally occurring chemical compounds which can be used for therapeutic purposes, either directly or indirectly. These plants have been used for centuries in various traditional systems of medicine, such as Ayurveda, Chinese medicine, and Native American medicine, to prevent or treat various health conditions.

Medicinal plants contain a wide variety of bioactive compounds, including alkaloids, flavonoids, tannins, terpenes, and saponins, among others. These compounds have been found to possess various pharmacological properties, such as anti-inflammatory, analgesic, antimicrobial, antioxidant, and anticancer activities.

Medicinal plants can be used in various forms, including whole plant material, extracts, essential oils, and isolated compounds. They can be administered through different routes, such as oral, topical, or respiratory, depending on the desired therapeutic effect.

It is important to note that while medicinal plants have been used safely and effectively for centuries, they should be used with caution and under the guidance of a healthcare professional. Some medicinal plants can interact with prescription medications or have adverse effects if used inappropriately.

11-Beta-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) is an enzyme that plays a crucial role in the metabolism of steroid hormones, particularly cortisol, in the body. Cortisol is a glucocorticoid hormone produced by the adrenal glands that helps regulate various physiological processes such as metabolism, immune response, and stress response.

11β-HSD1 is primarily expressed in liver, fat, and muscle tissues, where it catalyzes the conversion of cortisone to cortisol. Cortisone is a biologically inactive form of cortisol that is produced when cortisol levels are high, and it needs to be converted back to cortisol for the hormone to exert its effects.

By increasing the availability of active cortisol in these tissues, 11β-HSD1 has been implicated in several metabolic disorders, including obesity, insulin resistance, and type 2 diabetes. Inhibitors of 11β-HSD1 are currently being investigated as potential therapeutic agents for the treatment of these conditions.

Octanols are a type of chemical compound known as alcohols, specifically they are fatty alcohols with a chain of 8 carbon atoms. The most common octanol is called 1-octanol, which has the chemical formula CH3(CH2)7OH. It is a colorless oily liquid that is used in the synthesis of other chemicals and as a solvent. Octanols are often used as standards for measuring the partition coefficient between octanol and water, which is a measure of a compound's hydrophobicity or lipophilicity. This property is important in understanding how a compound may be absorbed, distributed, metabolized, and excreted in the body.

A stomach ulcer, also known as a gastric ulcer, is a sore that forms in the lining of the stomach. It's caused by a breakdown in the mucous layer that protects the stomach from digestive juices, allowing acid to come into contact with the stomach lining and cause an ulcer. The most common causes are bacterial infection (usually by Helicobacter pylori) and long-term use of nonsteroidal anti-inflammatory drugs (NSAIDs). Stomach ulcers may cause symptoms such as abdominal pain, bloating, heartburn, and nausea. If left untreated, they can lead to more serious complications like internal bleeding, perforation, or obstruction.

Connexins are a family of proteins that form the structural units of gap junctions, which are specialized channels that allow for the direct exchange of small molecules and ions between adjacent cells. These channels play crucial roles in maintaining tissue homeostasis, coordinating cellular activities, and enabling communication between cells. In humans, there are 21 different connexin genes that encode for these proteins, with each isoform having unique properties and distributions within the body. Mutations in connexin genes have been linked to a variety of human diseases, including hearing loss, skin disorders, and heart conditions.

Cortisone is a type of corticosteroid hormone that is produced naturally in the body by the adrenal gland. It is released in response to stress and helps to regulate metabolism, reduce inflammation, and suppress the immune system. Cortisone can also be synthetically produced and is often used as a medication to treat a variety of conditions such as arthritis, asthma, and skin disorders. It works by mimicking the effects of the natural hormone in the body and reducing inflammation and suppressing the immune system. Cortisone can be administered through various routes, including oral, injectable, topical, and inhalational.

Connexin 43 is a protein that forms gap junctions, which are specialized channels that allow for the direct communication and transport of small molecules between adjacent cells. Connexin 43 is widely expressed in many tissues, including the heart, brain, and various types of epithelial and connective tissues. In the heart, connexin 43 plays a crucial role in electrical conduction and coordination of contraction between cardiac muscle cells. Mutations in the gene that encodes connexin 43 have been associated with several human diseases, including certain types of cardiac arrhythmias and skin disorders.

A duodenal ulcer is a type of peptic ulcer that develops in the lining of the first part of the small intestine, called the duodenum. It is characterized by a break in the mucosal layer of the duodinal wall, leading to tissue damage and inflammation. Duodenal ulcers are often caused by an imbalance between digestive acid and mucus production, which can be exacerbated by factors such as bacterial infection (commonly with Helicobacter pylori), nonsteroidal anti-inflammatory drug use, smoking, and stress. Symptoms may include gnawing or burning abdominal pain, often occurring a few hours after meals or during the night, bloating, nausea, vomiting, loss of appetite, and weight loss. Complications can be severe, including bleeding, perforation, and obstruction of the duodenum. Diagnosis typically involves endoscopy, and treatment may include antibiotics (if H. pylori infection is present), acid-suppressing medications, lifestyle modifications, and potentially surgery in severe cases.

Central muscle relaxants are a class of pharmaceutical agents that act on the central nervous system (CNS) to reduce skeletal muscle tone and spasticity. These medications do not directly act on the muscles themselves but rather work by altering the messages sent between the brain and the muscles, thereby reducing excessive muscle contraction and promoting relaxation.

Central muscle relaxants are often prescribed for the management of various neuromuscular disorders, such as multiple sclerosis, spinal cord injuries, cerebral palsy, and stroke-induced spasticity. They may also be used to treat acute musculoskeletal conditions like strains, sprains, or other muscle injuries.

Examples of central muscle relaxants include baclofen, tizanidine, cyclobenzaprine, methocarbamol, and diazepam. It is important to note that these medications can have side effects such as drowsiness, dizziness, and impaired cognitive function, so they should be used with caution and under the guidance of a healthcare professional.

Bendroflumethiazide is a diuretic medication, which means it helps the body get rid of excess salt and water by increasing urine production. It is primarily used to treat high blood pressure and edema (swelling) caused by various medical conditions.

The drug works by inhibiting the reabsorption of sodium and chloride ions in the distal convoluted tubule of the kidney, which leads to increased water excretion. This results in a decrease in blood volume and, consequently, reduced blood pressure.

Bendroflumethiazide is available under various brand names, such as Aprinox, Corrida, and Natrilix. It's important to note that this medication should only be taken under the supervision of a healthcare professional, as it can have side effects and interact with other medications.

Hyperaldosteronism is a medical condition characterized by the overproduction of aldosterone, a hormone produced by the adrenal glands. Aldosterone helps regulate sodium and potassium balance and blood pressure by promoting sodium retention and potassium excretion in the kidneys.

There are two types of hyperaldosteronism: primary and secondary. Primary hyperaldosteronism is caused by an overproduction of aldosterone from an abnormality within the adrenal gland, such as a tumor (Conn's syndrome) or hyperplasia. Secondary hyperaldosteronism occurs when there is an excess production of renin, a hormone produced by the kidneys, which then stimulates the adrenal glands to produce more aldosterone. This can be caused by various conditions that affect kidney function, such as renal artery stenosis or heart failure.

Symptoms of hyperaldosteronism may include high blood pressure, low potassium levels (hypokalemia), muscle weakness, and frequent urination. Diagnosis typically involves measuring aldosterone and renin levels in the blood, as well as other tests to determine the underlying cause. Treatment depends on the type and cause of hyperaldosteronism but may include medications, surgery, or lifestyle changes.

Zona glomerulosa is a region of the adrenal gland, specifically the outer portion of the adrenal cortex. It is responsible for producing mineralocorticoids, with the principal one being aldosterone. Aldosterone helps regulate electrolyte and fluid balance in the body by increasing the reabsorption of sodium ions and water in the distal nephron of the kidney while promoting the excretion of potassium ions. This process assists in maintaining blood pressure and volume within normal ranges. The zona glomerulosa's function is primarily under the control of the renin-angiotensin-aldosterone system (RAAS).

Aldosterone is a hormone produced by the adrenal gland. It plays a key role in regulating sodium and potassium balance and maintaining blood pressure through its effects on the kidneys. Aldosterone promotes the reabsorption of sodium ions and the excretion of potassium ions in the distal tubules and collecting ducts of the nephrons in the kidneys. This increases the osmotic pressure in the blood, which in turn leads to water retention and an increase in blood volume and blood pressure.

Aldosterone is released from the adrenal gland in response to a variety of stimuli, including angiotensin II (a peptide hormone produced as part of the renin-angiotensin-aldosterone system), potassium ions, and adrenocorticotropic hormone (ACTH) from the pituitary gland. The production of aldosterone is regulated by a negative feedback mechanism involving sodium levels in the blood. High sodium levels inhibit the release of aldosterone, while low sodium levels stimulate its release.

In addition to its role in maintaining fluid and electrolyte balance and blood pressure, aldosterone has been implicated in various pathological conditions, including hypertension, heart failure, and primary hyperaldosteronism (a condition characterized by excessive production of aldosterone).

The adrenal cortex is the outer portion of the adrenal gland, which is located on top of the kidneys. It plays a crucial role in producing hormones that are essential for various bodily functions. The adrenal cortex is divided into three zones:

1. Zona glomerulosa: This outermost zone produces mineralocorticoids, primarily aldosterone. Aldosterone helps regulate sodium and potassium balance and thus influences blood pressure by controlling the amount of fluid in the body.
2. Zona fasciculata: The middle layer is responsible for producing glucocorticoids, with cortisol being the most important one. Cortisol regulates metabolism, helps manage stress responses, and has anti-inflammatory properties. It also plays a role in blood sugar regulation and maintaining the body's response to injury and illness.
3. Zona reticularis: The innermost zone produces androgens, primarily dehydroepiandrosterone (DHEA) and its sulfate form (DHEAS). These androgens are weak compared to those produced by the gonads (ovaries or testes), but they can be converted into more potent androgens or estrogens in peripheral tissues.

Disorders related to the adrenal cortex can lead to hormonal imbalances, affecting various bodily functions. Examples include Addison's disease (insufficient adrenal cortical hormone production) and Cushing's syndrome (excessive glucocorticoid levels).

Mineralocorticoids are a class of steroid hormones that primarily regulate electrolyte and fluid balance in the body. The most important mineralocorticoid is aldosterone, which is produced by the adrenal gland in response to signals from the renin-angiotensin system. Aldosterone acts on the distal tubules and collecting ducts of the nephrons in the kidneys to increase the reabsorption of sodium ions (Na+) and water into the bloodstream, while promoting the excretion of potassium ions (K+) and hydrogen ions (H+) into the urine. This helps maintain blood pressure and volume, as well as ensuring a proper balance of electrolytes in the body. Other mineralocorticoids include cortisol and corticosterone, which have weak mineralocorticoid activity and play a more significant role as glucocorticoids, regulating metabolism and immune response.

The adrenal glands are a pair of endocrine glands that are located on top of the kidneys. Each gland has two parts: the outer cortex and the inner medulla. The adrenal cortex produces hormones such as cortisol, aldosterone, and androgens, which regulate metabolism, blood pressure, and other vital functions. The adrenal medulla produces catecholamines, including epinephrine (adrenaline) and norepinephrine (noradrenaline), which help the body respond to stress by increasing heart rate, blood pressure, and alertness.

Medical Definition:

Mineralocorticoid Receptors (MRs) are a type of nuclear receptor protein that are activated by the binding of mineralocorticoid hormones, such as aldosterone. These receptors are expressed in various tissues and cells, including the kidneys, heart, blood vessels, and brain.

When activated, MRs regulate gene expression related to sodium and potassium homeostasis, water balance, and electrolyte transport. This is primarily achieved through the regulation of ion channels and transporters in the distal nephron of the kidney, leading to increased sodium reabsorption and potassium excretion.

Abnormalities in mineralocorticoid receptor function have been implicated in several diseases, including hypertension, heart failure, and primary aldosteronism.

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Anti-aggregation agents such as apomorphine, or carbenoxolone. The latter has commonly been used as a treatment for peptic ... By binding with high affinity to Aβ42 fragments, primarily via hydrogen bonding, carbenoxolone captures the peptides before ... Sharma S, Nehru B, Saini A (September 2017). "Inhibition of Alzheimer's amyloid-beta aggregation in-vitro by carbenoxolone: ...
A synthetic analog, carbenoxolone, was developed in Britain.[citation needed] Both glycyrrhetinic acid and carbenoxolone have a ...
Steer, H.W.; D.G. Colin-Jones (1975). "Mucosal changes in gastric ulceration and their response to carbenoxolone sodium". Gut. ...
Steer HW, Colin-Jones DG (1975). "Mucosal changes in gastric ulceration and their response to carbenoxolone sodium". Gut. 16 (8 ...
Berg M, Geisel A, Necheles H (1975). "The influence of carbenoxolone on steroid-induced ulcer and mucus secretion in the rat". ...
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11β-HSD1 is inhibited by carbenoxolone, a drug typically used in the treatment of peptic ulcers. Moreover, 18alpha-glycyrrhizic ...
11α-OHP is a more potent inhibitor of 11β-HSD than enoxolone (glycyrrhetinic acid) or carbenoxolone in vitro (IC50 = 0.9 nM; ...
Gastric cytoprotective drugs include carbenoxolone, deglycyrrhizinised liquorice, sucralfate (aluminium hydroxide and sulphated ...
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title = "Encapsulated carbenoxolone reduces lung metastases",. abstract = "Carbenoxolone is an anti-inflammatory compound and a ... Encapsulated carbenoxolone reduces lung metastases. Adi Karsch-Bluman, Shimrit Avraham, Miri Assayag, Ouri Schwob, Ofra Benny* ... Encapsulated carbenoxolone reduces lung metastases. / Karsch-Bluman, Adi; Avraham, Shimrit; Assayag, Miri et al. In: Cancers, ... Carbenoxolone is an anti-inflammatory compound and a derivate of a natural substance from the licorice plant. We previously ...
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  • PANX1 channel inhibition using probenecid (PBN) or carbenoxolone (CBX) reduced the proliferation of our panel of high-risk NB cell lines. (jcancer.org)
  • most ATP-induced ethidium uptake since this was drastically reduced Terlipressin by Panx1 channel blockers (10Panx1, Probenecid and low carbenoxolone concentration) and absent in T cells derived from Panx1? (2011globalhealth.org)
  • Carbenoxolone (CBX) is a glycyrrhetinic acid derivative with a steroid-like structure, similar to substances found in the root of the licorice plant. (wikipedia.org)
  • Carbenoxolone is an anti-inflammatory compound and a derivate of a natural substance from the licorice plant. (huji.ac.il)
  • Carbenoxolone, spironolactone, mefloquine and other old, well-known drugs have been shown to have Panx1 blocking activity as an off-target pharmacological effect and found to be effective in in vivo animal tumor models. (pannextherapeutics.com)
  • To 11β-HSD1, the compounds were anchored similar than unselective compound carbenoxolone, whereas in 11β-HDS2, they adopted a flipped binding mode. (helsinki.fi)
  • Sonamukhi possesses laxative properties to help harden stools and relieve constipation .Mulethi has glycyrrhizin and its compound, carbenoxolone which is effective in treating constipation . (vigyanveda.com)
  • Formulations used clinically typically contain carbenoxolone sodium. (guidetopharmacology.org)
  • It is a palatable tablet containing 20 mg carbenoxolone sodium plus aluminium hydroxide, magnesium trisilicate, sodium bicarbonate and alginic acid. (bmj.com)
  • The daily dose of carbenoxolone is 100 mg (less than in the treatment of gastric ulcer) and the daily sodium 'load' is 13 mmol. (bmj.com)
  • In part, confusion arises from the many different forms of the herb, its constituents, concentrates, and derivatives, such as the antiulcer drug carbenoxolone sodium, deglycyrrhizinated licorice (DGL), or parenteral products such as SNMC (no longer available) from Japan. (interactionsguide.com)
  • Sodium may increase the risk of oedema associated with antihypertensive agents (calcium channel blockers, vasodilators), corticosteroids, non-steroidal anti-inflammatory agents, oestrogens, liquorice and carbenoxolone. (thevitaminsshoppe.com.au)
  • Use Caution Monitor Closely (1)albuterol and carbenoxolone both decrease serum potassium. (tantrakamala.com)
  • The 4 include crude extracts of the whole plant, DGL combined with other agents (ie, Caved-S), DGL alone, and drug analogs of glycyrrhizin derivatives (eg, carbenoxolone, enoxolone). (naturalmedicinejournal.com)
  • The endothelium-derived hyperpolarising factor (EDHF) response in mesenteric arteries was investigated using wire myography, and the involvement of myoendothelial gap junctions (MEGJs) was assessed using the putative gap junction inhibitor carbenoxolone. (gla.ac.uk)
  • Carbenoxolone may decrease the amount of active glucocorticoid in the brain, because the drug inhibits 11β-HSD, an enzyme which regenerates cortisol, an active glucocorticoid, from inactive cortisone. (wikipedia.org)
  • Arguments, as increased efficiency is a requirement of biological with IC50 thiazide diuretics, and carbenoxolone are enhanced by corticosteroids. (worldblindnesssummit.com)
  • Carbenoxolone is a modestly potent, reasonably effective, water-soluble blocker of gap junctions. (wikipedia.org)
  • A response inhibited by the hemi-channel blocker carbenoxolone (200µM, 30mins). (lincoln.ac.uk)
  • Both systemic and intranasal administrations of carbenoxolone effectively minimize metastatic formation in a lung colonization model in mice. (huji.ac.il)
  • Spinal GFAP expression was significantly increased by FeCl 2 and intrathecal injection of carbenoxolone (an astrocyte gap junction decoupler) at day 3 significantly reduced TIIP, suggesting that spinal astrocyte activation plays an important role. (utmb.edu)
  • Notably, the therapeutic effect of a single intranasal administration of 25 mg/kg carbenoxolone, in the form of drug-loaded particles, had a similar effect in reducing metastatic lesions in the lungs to that of a 10-fold dose of the free drug via intraperitoneal injections, three times per week over the course of four weeks. (huji.ac.il)
  • To further enhance carbenoxolone{\textquoteright}s activity and localization in the lungs, thereby reducing the potential adverse side effects resulting from systemic exposure, we developed a poly(lactic-co-glycolic acid) (PLGA) slow-release system for pulmonary delivery which maintains drug activity in-vitro, as demonstrated in the anoikis assay. (huji.ac.il)
  • Carbenoxolone has also been investigated for nootropic effects. (wikipedia.org)
  • Carbenoxolone is derived from licorice root, and has a steroid-like chemical structure. (guidetopharmacology.org)
  • Carbenoxolone prevents chemical eye ischemia-reperfusion-induced cell death via 11beta-hydroxysteroid dehydrogenase type 1 inhibition. (ac.ir)
  • Carbenoxolone attenuated the EDHF response in the WKY, suggestive of the involvement of myoendothelial gap junctions in EDHF. (gla.ac.uk)
  • We previously showed that carbenoxolone reduces the metastatic burden in the lungs of mice through its antagonistic effect on high mobility group box 1 (HMGB1). (huji.ac.il)
  • Carbenoxolone is used for the treatment of peptic, esophageal and oral ulceration and inflammation. (wikipedia.org)
  • Carbenoxolone has also been used in topical creams such as Carbosan gel, marketed for treatment of lip sores and mouth ulcers. (wikipedia.org)
  • Carbenoxolone (CBX) is a glycyrrhetinic acid derivative with a steroid-like structure, similar to substances found in the root of the licorice plant. (wikipedia.org)
  • A genus of leguminous herbs or shrubs whose roots yield GLYCYRRHETINIC ACID and its derivative, CARBENOXOLONE . (online-medical-dictionary.org)
  • Carbenoxolone is a modestly potent, reasonably effective, water-soluble blocker of gap junctions. (wikipedia.org)
  • The gap junction uncoupler carbenoxolone prevented both conducted dilation and intercellular spread of dye through gap junctions. (unideb.hu)
  • Blockade of gap junctions with carbenoxolone or Ca 2+ -activated chloride channels (CaCCs) with 4,4′-diisothiocyanato-2,2′-stilbenedisulphonic acid disodium salt prevented Ca 2+ transients in PCA and venular pericytes and disrupted the synchrony of Ca 2+ transients in capillary and PCV pericytes. (edu.au)
  • Importantly, the responses to the uncaging stimuli shown in Figure 3B were not significantly attenuated by the gap junction inhibitor carbenoxolone (Figure S4), suggesting that gap junctions do not contribute to the LE-mediated currents evoked by uncaging CYLE around the soma. (camkkinases.com)
  • The gap-junction inhibitor carbenoxolone suppresses the differentiation of Th17 cells through inhibition of IL-23 expression in antigen presenting cells. (uchicago.edu)
  • Cx43-induced Pb uptake was attenuated after blockage of Cx43 hemichannels with its inhibitor, carbenoxolone. (nih.gov)
  • Serum carbenoxolone in patients with gastric and duodenal ulcer: Absorption, efficacy and side-effects. (bmj.com)
  • 12. Carbenoxolone treatment ameliorated metabolic syndrome in WNIN/Ob obese rats, but induced severe fat loss and glucose intolerance in lean rats. (nih.gov)
  • Effects of carbenoxolone in lean and obese Zucker rats. (nih.gov)
  • Mouth administration from the 11HSD inhibitor MK-2894 manufacture carbenoxolone to uremic rats for 2 wk improved blood sugar tolerance and insulin awareness, improved insulin signaling, and decreased hepatic appearance of gluconeogenic and lipogenic genes. (acancerjourney.info)
  • Carbenoxolone has also been used in topical creams such as Carbosan gel, marketed for treatment of lip sores and mouth ulcers. (wikipedia.org)
  • Treatment of herpes genitalis with carbenoxolone and cicloxolone creams: a double blind placebo controlled clinical trial. (bmj.com)
  • Carbenoxolone is used for the treatment of peptic, esophageal and oral ulceration and inflammation. (wikipedia.org)
  • The administration of octanol and carbenoxolone both failed to attenuate the neurological deficits induced by SAH, and they did not reduce neuronal apoptosis. (e-core.org)
  • Experimental Groups and Quantification of SAH Prior to surgery animals were randomly assigned to one of five groups: (1) SHAM surgery plus the R428 administration of vehicle solution (triglyceride oil), (2) SAH surgery + vehicle solution (triglyceride oil), (3) SAH + 260.46 mg/kg of octanol, (4) SAH +781.38 mg/kg of octanol, or (5) SAH + 100 mg/kg of Rabbit polyclonal to KLHL1 carbenoxolone. (e-core.org)
  • Cabbage contains gefarnate -compound similar to carbenoxolone, a remedy used in ulcers treatments. (healthyfoodhouse.com)