Pingyangmycin is an anticancer drug known as bleomycin A5 (A5), discovered in the Pingyang County of Zhejiang Province of China. Bleomycin (BLM) is a mixture of mainly two compounds (A2 and B2), which is on the World Health Organizations list of essential medicines. Both BLM and A5 are hydrophilic molecules that depend on transporters or endocytosis receptors to get inside of cells. Once inside, the anticancer activities rely on their abilities to produce DNA breaks, thus leading to cell death. Interestingly, the half maximal inhibitory concentration (IC50) of BLMs in different cancer cell lines varies from nM to μM ranges. Different cellular uptake, DNA repair rate, and/or increased drug detoxification might be some of the reasons; however, the molecules and signaling pathways responsible for these processes are largely unknown. In the current study, we purified the A2 and B2 from the BLM and tested the cytotoxicities and the molecular mechanisms of each individual compound or in combination with six
In last decades, biologically active natural compound (R)-goniothalamin and its derivatives received great attention from researchers. The reason for this interest is the wide range of biological properties of goniothalamin; including anti-microbial, antiprotozoan, anti-inflammatory, cytotoxic and anti-proliferative activities. The present study sets out the asymmetric large scale synthesis of α,β- unsaturated lactone derivative (R)-(+)-6-(2-Methylnaphthalen-1-yl)-5,6-dihydro-2Hpyran- 2-one. In recent studies, this linker modified analog of goniothalamin was shown to be cytotoxic against PC-3 (prostate cancer) and MCF-7 (human breast cancer) cell lines with half maximal inhibitory concentration values of 0.13 μM and 2.6 μM, respectively. The preparation of the target compound consists of three steps. First, asymmetric synthesis of homoallylic alcohol using (R)-Tol-BINAP AgF catalyst complex was performed with allyltrimethoysilane. After that, treating the chiral homoallylic alcohol ...
ABSTRACT The present study aims to investigate the cytotoxic effect of the major aflatoxins (B1, B2, G2 and G2) and also aflatoxin combination, using a simple, rapid and cheap cytotoxicity test like MTT (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide) assay in three in vitro models (human umbilical vein endothelial cells [HUVEC], human lung fibroblasts [HFL] and A2780 cell line) and to extrapolate the data to in vivo situation using a prediction model. A difference in cell sensitivity has been observed for B1 and B1 + B2, in the following order A2789 > HFL > HUVEC, while for B2, G1, G2, Mix (B1 + B2 + G1 + G2) the order was HFL > A2789 > HUVEC when comparing the IC50 (half maximal inhibitory concentration) values. We confirm that in vitro cytotoxicity test MTT assay is able to predict in vivo toxicity, at least for aflatoxins using the prediction model. The values of LD50 (lethal dose 50%) calculated from experiments are different for each cell line. This fact may indicate that ...
BioAssay record AID 64221 submitted by ChEMBL: In vitro minimum inhibition concentration against Escherichia coli D21f2, LPS mutant; Range is from 25-50.
Cadmium (Cd) is harmful for humans and animals, especially for the reproductive system. However, the mechanism of its toxicity has not been elucidated, and how to alleviate its toxicity is very important. This study aimed to explore the role and mechanism of action of sulforaphane (SFN) in protecting mouse Leydigs (TM3) cells from cadmium (Cd)-induced damage. The half-maximal inhibitory concentration (IC50) of Cd and the safe doses of SFN were determined using a methyl thiazolyl tetrazolium (MTT) assay. The testosterone secretion from TM3 cells was measured using the enzyme-linked immunosorbent assay. The intracellular oxidative stress was evaluated using corresponding kits. The cell apoptosis was detected using flow cytometry. The mRNA expression of genes associated with NF-E2-related factor 2 (Nrf2)/antioxidant response element (ARE) signaling was detected using reverse transcriptionâ »polymerase chain reaction, including Nrf2, heme oxygenase I (HO-1), glutathione peroxidase (GSH-Px), ...
In this study we (i) calculated half-maximal inhibitory concentrations (IC.sub.50) by motility tests against O. felineus adults and newly excysted metacercarie ...
WK23 is an inhibitor based on four aromatic groups and able to efficiently fill the binding pockets of MDM2/MDMX, its median inhibitory concentration (IC50) values to MDM2/MDMX are 1.17 and 36 uM, respectively
1 FPL 63547, in its active diacid form, was a potent inhibitor of rabbit lung angiotensin converting enzyme (ACE) in vitro (IC50… Expand ...
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A8326 AZD-5438 AZD5438 is a potent small molecule inhibitor of cyclin-dependent kinase (CDK) 1, 2 and 9 with half maximal inhibitory concentration IC50 of 16 nmol/L, 6 nmol/L and 20 nmol/L respectively. AZD5438 has also been found to potently inhibit the human cyclin E/CDK2 complex, the cyclin B1/CDK1 complex and the cyclin A/CDK2 complex with IC50 of 0.006 μM, 0.016 μM and 0.045 μM respectively. In previous studies, AZD5438 has exhibited significant anti-proliferative activity in a few human tumor cell lines with IC50 ranging from 0.2 μmol/L to 1.7 μmol/L, in which the phosphorylation of a few proteins, including CDK substrates pRb, nucleolin, protein phosphatase 1a and RNA polymerase II COOH-terminal domain, and cell cycling at G2-M, S and G1 phases were inhibited. ...
Curcumin (1) and ten derivatives (2-11) were synthesized and evaluated as cytotoxic and antioxidant agents. The results of primary screening by Sulforhodamine B assay against five human cancer cell lines (U-251 MG, glioblastoma; PC-3, human prostatic; HCT-15, human colorectal; K562, human chronic myelogenous leukemia; and SKLU-1, non-small cell lung cancer) allowed us to calculate the half maximal inhibitory concentration (IC50) values for the more active compounds against HCT-15 and K562 cell lines. Compounds 2 and 10 were the most active against both cell lines and were more active than curcumin itself. Thiobarbituric acid reactive substances (TBARS) assay showed that 7 has potent activity; even stronger than curcumin, α-tocopherol, and quercetin.
IL-12, a heterodimeric cytokine, consists of two disulfide-linked subunits, p40 and p35. We investigated the role of p40 in ligand binding and signal transduction by expressing this subunit alone in COS cells. Culture media of the transfected COS cells exhibited specific dose-dependent binding to KIT225/K6 cells, a human T cell line that expresses IL-12R. Analysis of the culture media by SDS-PAGE and Western blotting demonstrated the presence of 40-kDa monomers and 80-kDa disulfide-linked homodimers. The two p40 species were purified and identified by N-terminal sequencing and proteolytic peptide mapping. Characterization of the p40 proteins for binding and bioactivity showed that both the p40 monomer and dimer inhibited 125I-labeled IL-12 binding to IL-12R, but the 80-kDa species, having a 50% inhibitory concentration (IC50) of 20 to 70 ng/ml, was at least 20-fold more effective than the monomer. Although neither the monomer nor the dimer stimulated human PHA-blast proliferation, the 80-kDa ...
BioAssay record AID 594378 submitted by ChEMBL: Cell cycle arrest in human K562 cells assessed as accumulation at G0-G1 phase at IC100 after 24 hrs using propidium iodide staining by flow cytometry (Rvb = 43.40%).
Dengue is a major mosquito-borne disease currently with no effective antiviral or vaccine available. Effort to find antivirals for it has focused on bioflavonoids, a plant-derived polyphenolic compounds with many potential health benefits. In the present study, antiviral activity of four types of bioflavonoid against dengue virus type -2 (DENV-2) in Vero cell was evaluated. Anti-dengue activity of these compounds was determined at different stages of DENV-2 infection and replication cycle. DENV replication was measured by Foci Forming Unit Reduction Assay (FFURA) and quantitative RT-PCR. Selectivity Index value (SI) was determined as the ratio of cytotoxic concentration 50 (CC50) to inhibitory concentration 50 (IC50) for each compound. The half maximal inhibitory concentration (IC50) of quercetin against dengue virus was 35.7 μg mL-1 when it was used after virus adsorption to the cells. The IC50 decreased to 28.9 μg mL-1 when the cells were treated continuously for 5 h before virus infection and up to
Betulinic acid (BA) is a novel antineoplastic agent under evaluation for tumor therapy. Because of the selective cytotoxic effects of BA in tumor cells (including gliomas), the combination of this agent with conservative therapies (such as radiotherapy and chemotherapy) may be useful. Previously, the combination of BA with irradiation under hypoxic conditions had never been studied. In this study, the effects of 3 to 30 μM BA on cytotoxicity, migration, the protein expression of PARP, survivin and HIF-1α, as well as radiosensitivity under normoxic and hypoxic conditions were analyzed in the human malignant glioma cell lines U251MG and U343MG. Cytotoxicity and radiosensitivity were analyzed with clonogenic survival assays, migration was analyzed with Boyden chamber assays (or scratch assays) and protein expression was examined with Western blot analyses. Under normoxic conditions, a half maximal inhibitory concentration (IC50) of 23 μM was observed in U251MG cells and 24 μM was observed in U343MG
The study was carried out to evaluate the antioxidant activity and α-amylase activity inhibitory potential of Sarotherodon galillaeus muscle protein hydrolysates. Sarotherodon galillaeus muscle protein isolate was hydrolysed with three digestive proteases namely trypsin, chymotrypsin and pepsin. Degree of hydrolysis was determined. The antioxidative potential of the hydrolysates was investigated using DPPH radical scavenging, ferric reducing power, hydrogen peroxide scavenging and metal chelating activity. The ability of the hydrolysates to inhibit the activity of sugar-hydrolysing enzyme was also evaluated. Highest degree of hydrolysis was obtained with pepsin (55.86%) followed by trypsin (47.11%) and chymotrypsin (42.36%) after 6 hrs of hydrolysis. The half maximal inhibitory concentration (IC50) of hydrolysates produced by trypsin, chymotrypsin and pepsin for DPPH radical scavenging activity were 1.26 ± 0.95, 0.98 ± 0.07 and 1.18 ± 0.34 mg/ml respectively. Trypsin-produced hydrolysates ...
Microalgae are at the start of the food chain, and many are known producers of a significant amount of lipids with essential fatty acids. However, the bioactivity of microalgal lipids for anti-inflammatory and antithrombotic activities have rarely been investigated. Therefore, for a sustainable source of the above bioactive lipids, the present study was undertaken. The total lipids of microalga Chlorococcum sp., isolated from the Irish coast, were fractionated into neutral-, glyco-, and phospho-lipids, and were tested in vitro for their anti-inflammatory and antithrombotic activities. All tested lipid fractions showed strong anti-platelet-activating factor (PAF) and antithrombin activities in human platelets (half maximal inhibitory concentration (IC50) values ranging ~25-200 µg of lipid) with the highest activities in glyco- and phospho-lipid fractions. The structural analysis of the bioactive lipid fraction-2 revealed the presence of specific sulfoquinovosyl diacylglycerols (SQDG) bioactive ...
Background and purpose: Artemisia is one of the well-known herbal medicinal plants for antimicrobial, insecticidal, antioxidant, and antimalarial activities. The antiproliferative effects of dichloromethane extracts of Artemisia biennis (A. biennis) and A. ciniformis and the petroleum ether extract of A. ciniformis have been demonstrated previously on human cancerous cell lines. In the current study, further fractionation was carried out on the aforementioned extracts and their cytotoxic effects were evaluated on three human cancer cell lines; B16/F10, PC3, and MCF7. F1 to F16, F1 to F11, and F1 to F10 were resulted from the fractionation of dichloromethane extracts of A. biennis, A. ciniformis, and petroleum ether extract of A. ciniformis, respectively. Experimental approach: The cytotoxic effects of 16 (F1-F16), 11 (F1-F11) and 10 (F1-F10) fractions, on B16/F10, PC3, and MCF7 cell lines were assessed using resazurin to measure viability and propidium iodide staining (sub G1) and flow ...
Artemisinin is the frontline fast-acting anti-malarial against P. falciparum. Emergence and spread of resistant parasite in eastern-India poses a threat to national malaria control programs. Therefore, the objective of our study is to evaluate the artesunate-sulfadoxine-pyrimethamine efficacy in Central India. 180 monoclonal P. falciparum-infected patients received standard ASSP therapy during August 2015-January 2017, soon after diagnosis and monitored over next 42-days. Artemisinin-resistance was assessed through in-vivo parasite clearance half-life (PC1/2), ex-vivo ring-stage survivability (RSA), and genome analysis of kelch13 and other candidate gene (pfcrt, pfmdr1, pfatpase 6, pfdhfr and pfdhps). ...
Masitinib (AB1010) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC50=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC50s=540/800 nM), Lyn (IC50= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib (AB1010) has anti-proliferative, pro-apoptotic activity and low toxicity. - Mechanism of Action & Protocol.
InChI=1S/C28H30N6OS/c1-20-5-10-24(16-25(20)31-28-32-26(19-36-28)23-4-3-11-29-17-23)30-27(35)22-8-6-21(7-9-22)18-34-14-12-33(2)13-15-34/h3-11,16-17,19H,12-15,18H2,1-2H3,(H,30,35)(H,31,32) ...
The Quantitative Structure-Activity Relationship of a series of novel Thiazoline derivatives with anticancer activity has been studied by using the density functional theory by B3LYP/ 6-31G. Descriptors of quantum mechanics of 21 thiazoline derivatives with known activity were obtained. Multiple linear regressions were employed to model the relationships between molecular descriptors and biological activity of molecules using stepwise method. The most model shows not only significant statistical quality, but also predictive ability, with the square of adjusted correlation coefficient (R2=0.945) and standard error (SE=0.586). We find that the anticancer activity expressed that as half maximal inhibitory concentration (IC50), closely relates to the highest occupied molecular orbital, dipole moment, softness, hardness, ionization energy, electron affinity. Accordingly can be offered a quantitative model, and interpret the activity of the compounds relying on the multivariate statistical analysis. This
Masitinib is a selective tyrosine kinase inhibitor with potent activity against the juxta membrane domain of c-Kit. Masitinib is also thought to promote survival via modulation of immunostimulation-mediated anticancer effects and modulation of the tumor microenvironment. The objective of this study was to evaluate the efficacy and safety of masitinib with respect to dacarbazine in the treatment of non-resectable or metastatic stage 3 or stage 4 melanoma carrying a mutation in the juxta membrane domain of c-Kit. Following a protocol amendment, the dacarbarzine treatment group was closed and recruitment restricted to masitinib treatment of chemo-naïve (first-line) patients ...
Sapacitabine cancer drug molecule (nucleoside analogue). Stylized skeletal formula (chemical structure): Atoms are shown as color-coded circles: hydrogen (hidden), carbon (grey), nitrogen (blue), oxygen (red). - Stock Image F018/3177
AC220 (Quizartinib) is a uniquely potent and selective FLT3 inhibitor with IC50 of 0.56 ± 0.3 nM and >10 mM for MC4-11 and A375, respectively.
Sigma-Aldrich offers abstracts and full-text articles by [Marta Leirós, Eva Alonso, Mostafa E Rateb, Wael E Houssen, Rainer Ebel, Marcel Jaspars, Amparo Alfonso, Luis M Botana].
【市場調査レポート】タッチパネル用コントローラーICの世界市場2017-2021 | 発行日:2017年4月12日 | 商品コード:IRTNTR12538 | 発行/調査会社:Technavio | Global Touch Controller IC Market 2017-2021 | キーワード:グローバル、電子、タッチパネルコントローラーIC、タッチスクリーン [市場規模/動向/予測など世界の産業分析レポート販売のマーケットレポート.jp]
Masitinib is a selective, oral tyrosine kinase inhibitor with neuroprotective capability demonstrated via numerous preclinical studies. Two of masitinibs main cellular targets are the mast cell and microglia cell. It is well-established that mast cells play a prominent role in neuroinflammatory processes. Microglia, resident immune cells of the central nervous system (CNS), also constitute an important source of neuroinflammatory mediators and may have fundamental roles in numerous neurodegenerative disorders. The development of masitinib in ALS is therefore based on the pharmacological action of masitinib in microglia cells and mast cells, thereby slowing microglial-related disease progression, reducing neuro-inflammation, and modulating the neuronal microenvironment in both central and peripheral nervous systems. This is a multicenter, double-blind, randomized, placebo-controlled, parallel-group (two ascending dose titrations of masitinib and matching placebo), comparative study of oral ...
Anticancer bisdioxopiperazines, including ICRF-154, razoxane (Raz, ICRF-159) and ICRF-193, are a family of anticancer agents developed in the UK, especially targeting metastases of neoplasms. Two other bisdioxopiperazine derivatives, probimane (Pro) and MST-16, were synthesized at the Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China. Cytotoxic activities and mechanisms of Raz (+)-steroisomer (ICRF-187, dexrazoxane), Pro and MST-16 against tumor cells were evaluated by MTT colorimetry, flow cytometry and karyotyping. Pro was cytotoxic to human tumor cell lines in vitro (IC50|50 μM for 48 h). Four human tumor cell lines (SCG-7901, K562, A549 and HL60) were susceptible to Pro at low inhibitory concentrations (IC50 values | 10 μM for 48 h). Although the IC50 against HeLa cell line of vincristine (VCR, 4.56 μM), doxorubicin (Dox, 1.12 μM) and 5-fluoruouracil (5-Fu, 0.232 μM) are lower than Pro (5.12 μM), ICRF-187 (129 μM) and MST-16 (26.4 μM), VCR, Dox and 5-Fu shows
Anticancer bisdioxopiperazines, including ICRF-154, razoxane (Raz, ICRF-159) and ICRF-193, are a family of anticancer agents developed in the UK, especially targeting metastases of neoplasms. Two other bisdioxopiperazine derivatives, probimane (Pro) and MST-16, were synthesized at the Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China. Cytotoxic activities and mechanisms of Raz (+)-steroisomer (ICRF-187, dexrazoxane), Pro and MST-16 against tumor cells were evaluated by MTT colorimetry, flow cytometry and karyotyping. Pro was cytotoxic to human tumor cell lines in vitro (IC50|50 μM for 48 h). Four human tumor cell lines (SCG-7901, K562, A549 and HL60) were susceptible to Pro at low inhibitory concentrations (IC50 values | 10 μM for 48 h). Although the IC50 against HeLa cell line of vincristine (VCR, 4.56 μM), doxorubicin (Dox, 1.12 μM) and 5-fluoruouracil (5-Fu, 0.232 μM) are lower than Pro (5.12 μM), ICRF-187 (129 μM) and MST-16 (26.4 μM), VCR, Dox and 5-Fu shows
Class I PI3Ks can form an allosteric or specificity pocket (adjacent to the adenine pocket) only in the presence of propeller-like inhibitors (29). The half-maximal inhibitory concentrations (IC50s) for the propeller-like PI3K inhibitors (e.g., PIK-39) (fig. S9) are generally much worse for Vps34 than other PI3Ks. This is probably due to increased rigidity of the Vps34 pocket arising from a bulky residue substituted in the P loop (Phe612-Hs, Phe673-Dm) that packs against the aromatic hinge residue unique to Vps34 (Phe684-Hs, Tyr746-Dm). These differences effectively close off a corner of the adenine-binding pocket, giving it a more constrained appearance.. Currently there is no high-affinity, specific inhibitor of Vps34. We determined the structure of a complex of Vps34 with 3-methyladenine (3-MA) (Fig. 4, B and C), which is often used as a specific inhibitor of autophagy. We also determined the structures of Vps34 in complexes with three multi-targeted inhibitors: (i) PIK-90, (ii) PIK-93, ...
Scorpion venom-derived peptidyl toxins are valuable pharmacological tools for investigating the structure-function relationship of ion channels. Here, we report the purification, sequencing and functional characterization of a new K(+) channel blocker (MeuKTX) from the venom of the scorpion Mesobuthus eupeus. Effects of MeuKTX on ten cloned potassium channels in Xenopus oocytes were evaluated using two-electrode voltage-clamp recordings. MeuKTX is the orthologue of BmKTX (α-KTx3.6), a known Kv1.3 blocker from the scorpion Mesobuthus martensii, and classified as α-KTx3.13. MeuKTX potently blocks rKv1.1, rKv1.2 and hKv1.3 channels with 50% inhibitory concentration (IC(50)) of 203.15 ± 4.06 pM, 8.92 ± 2.3 nM and 171 ± 8.56 pM, respectively, but does not affect rKv1.4, rKv1.5, hKv3.1, rKv4.3, and hERG channels even at 2 μM concentration. At this high concentration, MeuKTX is also active on rKv1.6 and Shaker IR. Our results also demonstrate that MeuKTX and BmKTX have the same channel spectrum ...
Oxidative damage to the vascular endothelium may play an important role in the pathogenesis of atherosclerosis and aging, and may account in part for reduced vascular prostacyclin (PGI2) synthesis associated with both conditions. Using H2O2 to induce injury, we investigated the effects of oxidative damage on PGI2 synthesis in cultured endothelial cells (EC). Preincubation of EC with H2O2 produced a dose-dependent inhibition (inhibitory concentration [IC50] = 35 microM) of PGI2 formation from arachidonate. The maximum dose-related effect occurred within 1 min after exposure although appreciable H2O2 remained after 30 min (30% of original). In addition, H2O2 produced both a time- and dose-dependent injury leading to cell disruption, lactate dehydrogenase release, and 51Cr release from prelabeled cells. However, in dramatic contrast to H2O2 effects on PGI2 synthesis, loss of cellular integrity required doses in excess of 0.5 mM and incubation times in excess of 1 h. The superoxide-generating ...
immune Uncategorized Col4a2, Masitinib ( AB1010) interactions where the biological aftereffect of an publicity depends upon an individuals genotype are widely held to become ubiquitous-and rightly thus considering epidemiologists have got long abandoned the paradigm of ascribing disease to either character or nurture (if indeed they ever considered etiology in unifactoral conditions) and today seek to comprehend the joint actions of both character and nurture. gene-environment connections in individual observational research stands in sharpened contrast towards the wide-spread proof for gene-environment relationship from experimental research in model microorganisms (2). This discrepancy is certainly a puzzle. Masitinib ( AB1010) Will there be something fundamentally different about the biology of individual complicated attributes? Are there limitations to how gene-environment interactions have been analyzed in humans? Or both? Stenzel et al. (3) discuss two important methodological ...
Silibinin has limited in vitro antiproliferative activity in 4T1 cells 4T1-luc tumor cells were seeded in triplicates in 96-well plates at a concentration of 10
To discover leads for next-generation chemoprotective antimalarial drugs, we tested more than 500,000 compounds for their ability to inhibit liver-stage development of luciferase-expressing Plasmodium spp. parasites (681 compounds showed a half-maximal inhibitory concentration of less than 1 micromolar). Cluster analysis identified potent and previously unreported scaffold families as well as other series previously associated with chemoprophylaxis. Further testing through multiple phenotypic assays that predict stage-specific and multispecies antimalarial activity distinguished compound classes that are likely to provide symptomatic relief by reducing asexual blood-stage parasitemia from those which are likely to only prevent malaria. Target identification by using functional assays, in vitro evolution, or metabolic profiling revealed 58 mitochondrial inhibitors but also many chemotypes possibly with previously unidentified mechanisms of action.
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It was initially hard for me to know how to get started and contribute in this project and I think there are others how feel the same way, so Im describing here how I approached it. Its not the only way or even the correct way but just an experience Ive had so far.. ...
Each year the government adds an addional amount of money to our school budget for children who are eligible for free school meals, for Children in Care and for those who are members of service families. This is know as the Pupil Premium.. With the introduction of Universal Infant Free School Meals, parents who are on certain benefits, such as Income Support, are still encouraged to apply for Free School Meals, to enable their children to qualify for the Pupil Premium.. At Millbrook School, this money is particularly used to in the staffing line of the budget to enable more support to be given to the qualifying children, whether this be in general or specific programmes of study. A more detailed report on the expenditure can be found below along with our policy. ...
Results: All the evaluations were performed in triplicates and results were noted down. It was observed that aqueous extract of C. sativus fruits showed a maximum DPPH radical scavenging activity (p,0.0001), half-maximal inhibitory concentration (IC50) at a concentration of 122.67 μg/ml. The ethyl acetate fraction of C. sativus fruits exhibited maximum hyaluronidase (p,0.0001), MMP-1/collagenase (p,0.04), and tyrosinase (p,0.04) inhibitory activity, IC50 at a concentration of 59.54, 45.79, and 24.46 μg/ml, respectively. The elastase (p,0.0001) inhibitory activity by n-butanol fraction of C. sativus fruits extract was maximum, IC50 at a concentration of 52.76 μg/ml. ...
TY - JOUR. T1 - A conformational and structure-activity relationship study of cytotoxic 3,5-bis(arylidene)-4-piperidones and related N-acryloyl analogues. AU - Dimmock, J. R.. AU - Padmanilayam, M. P.. AU - Puthucode, R. N.. AU - Nazarali, A. J.. AU - Motaganahalli, N. L.. AU - Zello, G. A.. AU - Quail, J. W.. AU - Oloo, E. O.. AU - Kraatz, H. B.. AU - Prisciak, J. S.. AU - Allen, T. M.. AU - Santos, C. L.. AU - Balzarini, J.. AU - De Clercq, E.. AU - Manavathu, E. K.. PY - 2001/2/15. Y1 - 2001/2/15. N2 - A series of 3,5-bis(arylidene)-4-piperidones 1 and related N-acryloyl analogues 2 were prepared as candidate cytotoxic agents with a view to discerning those structural features which contributed to bioactivity. A number of the compounds were markedly cytotoxic toward murine P388 and L1210 leukemic cells and also to human Molt 4/C8 and CEM neoplasms. Approximately 40% of the IC50 values generated were lower than the figures obtained for melphalan. In virtually all cases, the N-acyl compounds ...
A new study reviews the potential for curcumin and nanosystems to treat COVID-19. Curcumin has been characterized and studied thoroughly, as a natural molecule with medicinal properties. Its tolerability and safety have been well documented, with a maximum dose of 12 g/day. Curcumin inhibits viral enzymes due to its ability to inhibit the virus itself, as well as to modulate inflammatory pathways. It regulates viral transcription and regulation, binds with high potency to the viral main protease (Mpro) enzyme that is key to replication, and inhibits viral attachment and entry into the host cell. It may also disrupt viral structures. It has been reported to inhibit the 3C-like protease (3CLpro) more effectively than other natural products, including quercetin, or drugs like chloroquine and hydroxychloroquine. It also inhibits papain-like protease (PLpro) with a 50% inhibitory concentration (IC50) of 5.7 µM that surpasses quercetin and other natural products. Modeling studies have shown that ...
As expected, the soluble CD4 positive control inhibited CXCR4 (50% inhibitory concentration [IC(50)] 3.7 μg/ml) and CCR5 (IC(50) 0.03 μg/ml) tropic HIV-1 infectivity. Free melittin doses ,2 μM were not cytotoxic and were highly effective in reducing HIV-1 infectivity for both CXCR4 and CCR5 strains in TZM-bl reporter cells, while VK2 vaginal cell viability was adversely affected at all free melittin doses tested. However, VK2 cell viability was not affected at any dose of melittin-loaded nanoparticles. Melittin nanoparticles safely and significantly decreased CXCR4 (IC(50) 2.4 μM and IC(90) 6.9 μM) and CCR5 (IC(50) 3.6 μM and IC(90) 11.4 μM) strain infectivity of TZM-bl reporter cells. Furthermore, melittin nanoparticles captured more HIV-1 than blank nanoparticles.. ...
Pharmaceuticals 2016, 9, 78 19 of 33 aptamers, exhibited cross-protection against infections of H1N1, H5N1, H7N7, and H7N9 influenza viruses, with a 50% inhibitory concentration (IC50) around 10 nM. The association of the viral polymerase, bound to the cap, and eIF4GI may be involved in the preferential translation of viral mRNAs during influenza infection. In addition, the interaction of NS1, bound to a conserved 5untranslated region (UTR) element of the viral mRNA, with eIF4GI and PABP1 could promote the formation of a closed loop between the 5′ and 3′ ends of the viral mRNA; (4) RIG-I is a cytosolic receptor for non-self RNA that mediates immune responses against viral infections through IFNα/β production. Mitochondrial antiviral-signaling (MAVS) protein. Table 6 shows information on the aptamers described against influenza virus. Vaccination is a powerful approach to diminish the effects of influenza epidemics, but the use of antiviral drugs can also be very useful, particularly in ...
Exploration of Scaffolds from Natural Products with Antiplasmodial Activities, Currently Registered Antimalarial Drugs and Public Malarial Screen Data. . Biblioteca virtual para leer y descargar libros, documentos, trabajos y tesis universitarias en PDF. Material universiario, documentación y tareas realizadas por universitarios en nuestra biblioteca. Para descargar gratis y para leer online.
The present invention relates to a mast cell inhibitor, a pharmaceutical composition and a method for the treatment of patients afflicted with Parkinsons disease, wherein said patients are treated with a tyrosine kinase inhibitor or mast cell inhibitor, in particular masitinib, or a compound selected from imatinib, cromolyn sodium, midostaurin, BLU-285, bosutinib, ibrutinib, LAS189386, DP-2618, fostamatinib, dasatinib, sunitinib, axitinib, pazopanib, and toceranib or a pharmaceutically acceptable salt or solvate thereof, optionally in combination with at least one pharmaceutically active ingredient.
Novel anti-HIV-1 agents derived from betulinic acid have been greatly concerned. 3D-QSAR and molecular docking studies were applied to rationalize the structural requirements responsible for the anti-HIV activity of these compounds. The CoMFA and CoMSIA models resulted from 28 molecules gave rcv² values of 0.599 and 0
In an interview with |em|Targeted Oncology|/em|, Jorge E. Cortes, MD, discussed the results from the QuANTUM-R trial, as well as some other studies investigating the use of quizartinib in different patient populations in AML.
The selective activity of genes is affected by displacements (morpho-genetic movements) of cells, their spatial location. They are provided by the ability of cells to actively move and adhere (selective formation of contacts with each other, in which glycocalyx plays an important role). Neighboring cells exert physical, chemical, and other influences on the cells that migrated and came into contact with them, selectively activating and inactivating the genes of their nuclei. Morphogenetic movement of cells is one of the mechanisms of selective activation of genes ...
Laurie Arliss, professor of speech communication, has worked with the Exploratory Program for more than a dozen years and has taught at IC since 1984. Her...
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e-Dentico - dwumiesięcznik stomatologa praktyka, polsko-angielski poradnik stomatologiczny. MNiSW: 5 pkt, IC: 5,5 pkt., punkty edukacyjne: 30 pkt.