Antiproliferative constituents in plants 10. Flavones from the leaves of Lantana montevidensis Briq. and consideration of structure-activity relationship.
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The flavonoid fraction from the leaves of Lantana montevidensis Briq. (Verbenaceae) showed antiproliferative activity against human gastric adenocarcinoma (MK-1, GI50: 12 microg/ml), human uterus carcinoma (HeLa, 5 microg/ml), and murine melanoma (B16F10, 5 microg/ml) cells in vitro. Bioactivity-guided chemical investigation of the fraction has resulted in the isolation of apigenin (10) and ten 5,6,7-oxygenated flavones: cirsilineol (1), eupatorin (2), 5,4'-dihydroxy-6,7,3',5'-tetramethoxyflavone (3), 5,6-dihydroxy-7,3',4'-trimethoxyflavone (4), 5,6,4'-trihydroxy-7,3',5'-trimethoxyflavone (5), 5,6,3'-trihydroxy-7,4'-dimethoxyflavone (6), 5,3',4'-trihydroxy-6,7,5'-trimethoxyflavone (7), cirsiliol (8), hispidulin (9), and eupafolin (11). Antiproliferative activity of the isolated flavones, some other related flavones (luteolin, baicalein, 6-hydroxyluteolin, pectolinarigenin, jaceosidin, desmethoxycentaureidin, eupatilin, and chrysin) from other plant materials, and synthetic 6- and 7-methoxyflavones was evaluated, and the structure-activity relationships were examined. (+info)
Pentacyclic triterpenoids from the aerial parts of Lantana camara.
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Three new pentacyclic triterpenoids, camaryolic acid (1), methylcamaralate (2) and camangeloyl acid (3) and six known compounds beta-sitosterol 3-O-beta-D-glucopyranoside (4), octadecanoic acid (5), docosanoic acid (6), palmitic acid (7), camaric acid (8) and lantanolic acid (9) were isolated from the aerial parts of Lantana camara. Structures of the new compounds were elucidated by spectroscopic and chemical methods. (+info)
Evaluation of antimotility effect of Lantana camara L. var. acuelata constituents on neostigmine induced gastrointestinal transit in mice.
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BACKGROUND: Lantana camara L. (Verbenaceae), a widely growing shrub which is toxic to some animal species, has been used in the traditional medicine for treating many ailments. The purpose of the present study was to evaluate the antimotility effects of Lantana camara leaf constituents in mice intestine. METHODS: Evaluation of antimotility activity was done in intestine of mice treated with Lantana camara leaf powder, Lantana camara methanolic extract (LCME), lantadene A, neostigmine and neostigmine + LCME. Neostigmine was used as a promotility agent. Intestinal motility was assessed by charcoal meal test and gastrointestinal transit rate was expressed as the percentage of the distance traversed by the charcoal divided by the total length of the small intestine. The antidiarrheal effect of LCME was studied against castor oil induced diarrhea model in mice. RESULTS: The intestinal transit with LCME at a dose of 500 mg/kg was 26.46% whereas the higher dose (1 g/kg) completely inhibited the transit of charcoal in normal mice. The % intestinal transit in the neostigmine pretreated groups was 24 and 11 at the same doses respectively. When the plant extracts at 125 and 250 mg/kg doses were administered intraperitonealy, there was significant reduction in fecal output compared with castor oil treated mice. At higher doses (500 and 1000 mg/kg), the fecal output was almost completely stopped. CONCLUSION: The remarkable antimotility effect of Lantana camara methanolic extract against neostigmine as promotility agent points towards an anticholinergic effect due to Lantana camara constituents and attests to its possible utility in secretory and functional diarrheas and other gastrointestinal disorders. This effect was further confirmed by significant inhibition of castor oil induced diarrhea in mice by various doses of LCME. (+info)
Two new pentacyclic triterpenoids from Lantana camara LINN.
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Two new pentacyclic triterpenoids, namely lantanoic acid (1) and camaranoic acid (2), and six known compounds such as lantic acid, camarinic acid, camangeloyl acid, camarinin, oleanonic acid, and ursonic acid were isolated from the aerial parts of Lantana camara LINN. Structures of the new constituents were elucidated by chemical transformation and spectral studies including 1D ((1)H- and (13)C-NMR) and 2D ((1)H-(1)H correlation spectroscopy (COSY), nuclear Overhauser effect spectroscopy (NOESY), (1)H-(1)H total correlation spectroscopy (TOCSY), J-resolved, (1)H-detected heteronuclear multiple quantum coherence (HMQC), and heteronuclear multiple bond connectivity (HMBC)) NMR spectroscopy. (+info)
Mosquito larvicidal constituents from Lantana viburnoides sp viburnoides var kisi (A. rich) Verdc (Verbenaceae).
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BACKGROUND & OBJECTIVES: Lantana viburnoides sp viburnoides var kisi is used in Tanzania ethnobotanically to repel mosquitoes as well as in traditional medicine for stomach ache relief. Bioassay-guided fractionation and subtraction bioassays of the dichloromethane extract of the root barks were carried out in order to identify the bioactive components for controlling Anopheles gambiae s.s. mosquito larvae. METHODS: Twenty late III or early IV instar larvae of An. gambiae s.s. were exposed to various concentrations of the plant extracts, fractions, blends and pure compounds, and were assayed in the laboratory by using the protocol of WHO 1996. Mean mortalities were compared using Dunnett's test (p < 0.05) and lethal concentration calculated by Lackfit Inversel of the SAS programme. RESULTS: The crude extract (LC50 = 7.70 ppm in 72 h) and fractions exhibited different level of mosquito larvicidal activity with subtraction of some fractions resulting in activity enhancement. The active fractions contained furanonaphthaquinones regio-isomers (LC50 = 5.48-5.70 ppm in 72 h) and the lantadene triterpenoid camaric acid (LC50 = 6.19 ppm in 72 h) as active principles while the lupane triterpenoid betulinic acid (LC50 < 10 ppm in 72 h) was obtained from the least active fraction. INTERPRETATION & CONCLUSION: Crude extracts and some fractions had higher or comparable larvicidal activity to the pure compounds. These results demonstrate that L. viburnoides sp viburnoides var kisi extracts may serve as larvicides for managing various mosquito habitats even in their semi-purified form. The isolated compounds can be used as distinct markers in the active extracts or plant materials belonging to the genus Lantana. (+info)
Adulticidal activity of essential oil of Lantana camara leaves against mosquitoes.
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BACKGROUND & OBJECTIVES: Development of insect resistance to synthetic pesticides, high operational cost and environmental pollution have created the need for developing alternative approaches to control vector-borne diseases. In the present study we have investigated the insecticidal activity of essential oil isolated from the leaves of Lantana camara against mosquito vectors. METHODS: Essential oil was isolated from the leaves of L. camara using hydro-distillation method. Bioassay test was carried out by WHO method for determination of adulticidal activity against mosquitoes. Different compounds were identified by gas chromatography-mass spectrometry analysis. RESULTS: LD(50) values of the oil were 0.06, 0.05, 0.05, 0.05 and 0.06 mg/cm(2) while LD(90) values were 0.10, 0.10, 0.09, 0.09 and 0.10 mg/cm(2) against Ae. aegypti, Cx. quinquefasciatus, An. culicifacies, An. fluvialitis and An. stephensi respectively. KDT(50) of the oil were 20, 18, 15, 12, and 14 min and KDT(90) values were 35, 28 25, 18, 23 min against Ae. aegypti, Cx. quinquefasciatus, An. culicifacies, An. fluviatilis and An. stephensi, respectively on 0.208 mg/cm(2) impregnated paper. Studies on persistence of essential oil of L. camara on impregnated paper revealed that it has more adulticidal activity for longer period at low storage temperature. Gas chromatographic-mass spectrometric analysis of essential oil showed 45 peaks. Caryophyllene (16.37%), eucalyptol (10.75%), alpha-humelene (8.22%) and germacrene (7.41%) were present in major amounts and contributed 42.75 per cent of the total constituents. INTERPRETATION & CONCLUSIONS: Essential oil from the leaves of L. camara possesses adulticidal activity against different mosquito species that could be utilized for development of oil-based insecticide as supplementary to synthetic insecticides. (+info)
The anti-mycobacterial activity of Lantana camara a plant traditionally used to treat symptoms of tuberculosis in South-western Uganda.
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INTRODUCTION: Tuberculosis continues to be a devastating public health problem. Many communities in Uganda use medicinal plants to treat various infections, including respiratory tract infections. There are claims that some can treat tuberculosis. Verifying some of these claims could lead to discovery of lead compounds for development of a TB drug. METHODS: Chloroform and methanol extracts of L. camara collected from South-western Uganda were screened against three strains of Mycobacterium tuberculosis using the agar-well diffusion method. H37Rv, the rifampicin-resistant TMC-331 and a non-resistant wild strain (28-25271). The MIC and MBC were determined using the Agar dilution method on Middle brook 7H11. RESULTS: The methanol extract showed the highest activity against all the three strains used, with zones of inhibition of 18.0-22.5 mm and MIC values of 20 microg/ml for H37Rv and 15 microg/ml for both TMC-331 and wild stain. The values for rifampicin were 1.0 microg/ml for both H37Rv and wild strain but rifampicin hardly showed any activity on TMC-331. The MBC value for the methanol extract of L. camara was 30microg/ml for the H37Rv, and 20microg/ml for both the TMC-331 and wild strains of M. tuberculosis. The MBC for rifampicin was 2.0microg/ml for both H37Rv and the wild strain. CONCLUSION: We conclude that L. camara contains principles active against M. tuberculosis, which merit further research. (+info)
Ingestion of Lantana camara is not associated with significant effects in children.
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