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ABSTRACT: Phytochemical investigation of the aerial parts of Callistemon lanceolatus DC (Myrtaceae) led to the isolation of two new flavones characterized as 5,7-dihydroxy-6,8-dimethyl- 4′ -methoxy flavone (1) and 8-(2-hydroxypropan-2-yl)-5-hydroxy-7-methoxy-6-methyl-4′-methoxy flavone (2) along with the seven known phytoconstituents. The structures of new compounds have been established on the basis of chemical and spectral studies and known compounds were compared with the published literature data. The isolated flavones exhibited blood glucose lowering effect in streptozotocin induced diabetic rats.
Fitoterapia 12/2012; · 1.85 Impact Factor
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ABSTRACT: Leaves of Platanus orientalis Linn. are used in folk medicine as a wound-healer and ophthalmologic agent. Phytol derivatives from the leaves of plane-tree show anti-ulcer activity. Its analgesic and anti-inflammatory effects for knee pain were known to Persian scientists and hakims.
The ethanolic extract of Platanus orientalis Linn. and its various fractions were given at a dose of 100mg/kg po and 200mg/kg po for testing their anti-inflammatory activity by carrageenan induced hind paw edema. The analgesic activity of the ethanolic extract and its fractions has been carried out by tail-flick method and writhing test at a dosage of 200mg/kg po. Gastric ulceration studies have been further carried out to study the ulcerogenic risk evaluation of the ethanolic extract and its various fractions at a dose of 600mg/kg body weight.
Among the tested fractions, chloroform fraction exhibited better inhibition (68.33%) at 200mg/kg po dosage when compared to the standard drug Ibuprofen (66.66%) after 3h in the carrageenan induced hind paw edema. The ethanolic extract and all its fractions especially the chloroform (p<0.01) showed significant analgesic activity with insignificant ulceration as compared to the standard drug i.e. Ibuprofen. The histopathological study of ethanolic extract and its fractions revealed that none of them cause ulcer.
The present study indicates that Platanus orientalis Linn. has significant anti-inflammatory and analgesic effect.
Journal of ethnopharmacology 07/2012; 143(1):236-40. · 2.32 Impact Factor
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ABSTRACT: Geraniol (GOH), a naturally occurring monoterpene, has been shown to have antiproliferative, cell cycle arrest and apoptosis-inducing effects, and represents a promising cancer chemopreventive agent. In the present study, we investigated the chemopreventive potential of GOH (50 and 100 mg kg(-1) body weight) against 7,12-dimethylbenz[a]anthracene (DMBA)/12-O-tetradecanoylphorbol 13-acetate (TPA)-mediated skin tumorigenesis in Swiss albino mice. The topical treatment of GOH, 30 min prior to TPA (2 µg per 200 µl of acetone) treatment significantly inhibited TPA-induced skin edema, hyperplasia, COX-2 induction and oxidative stress response. The GOH treatment also resulted in reduction of TPA-induced ornithine decarboxylase activity and [(3) H] thymidine incorporation by 53% (P < 0.001) and 41% (P < 0.001), respectively. We found that GOH treatment significantly inhibited the tumor incidence and number of tumors (P < 0.001) and extended the latency period from 4 weeks in DMBA/TPA treatment group to 10 weeks in GOH-pretreated mice. Furthermore, we observed that GOH treatment significantly suppressed the Ras/Raf/ERK1/2 signaling pathway in skin tumor. Consistently, GOH-treated skin tumors showed reduced expression of Bcl-2 and increased expression of Bax in these lesions. Thus, it was concluded that GOH inhibits DMBA/TPA-mediated skin tumorigenesis by attenuating the Ras proliferation pathway and inducing pro-apoptotic state via inhibition of oxidative stress response and inflammation. Copyright © 2012 John Wiley & Sons, Ltd.
Journal of Applied Toxicology 07/2012; · 2.48 Impact Factor
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ABSTRACT: To investigate the anti-inflammatory and anti-nociceptive activities of the crude ethanolic extract of Adiantum capillus veneris Linn. (Adiantaceae) and its various fractions.
The ethanolic extract and its fractions were given at a dose of 200 mg/kg po and 300 mg/kg po for testing their anti-inflammatory activity by carrageenan induced hind paw edema. The analgesic activity of the ethanolic extract and its fractions has been carried out by tail-flick method and writhing test at a dosage of 300 mg/kg po. Gastric ulceration studies have been further carried out to study the antiulcer effect of the ethanolic extract and its various fractions at dose of 900 mg/kg body weight.
Amongst the tested fractions, the ethyl acetate fraction exhibited better inhibition (67.27%) at 300 mg/kg po dosage when compared to the standard drug Indomethacin (63.63%) after 3h in the carrageenan induced hind paw edema. The anti-inflammatory activity of the ethanolic extract and its various fractions appear to be related to the inhibition of NO release, and the decreasing TNF-α level. The ethanolic extract and all its fractions especially the ethyl acetate (p<0.01) showed significant analgesic activity with insignificant ulceration as compared to the standard drug, i.e. ibuprofen. The histopathological study of ethanolic extract and its fractions reveals that none of them cause ulcer.
The present study indicates that Adiantum capillus veneris Linn. has significant anti-inflammatory and analgesic effect.
Journal of ethnopharmacology 12/2011; 138(3):741-7. · 2.32 Impact Factor
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ABSTRACT: A series of 1-(4-methoxyphenyl)-2-[5-{(biphenyl-4-yloxy)methyl}4-(substituted phenyl)-3-mercapto-(4H)-1,2,4-triazol-3-ylthio)] ethanones (6a-6s) and 4-(substituted phenyl)-3-(morpholin/pyrrolidin-4-ylmethylthio)-5-(4-phenylphenoxymethyl)-4H-1,2,4-triazoles (7a-7e) were synthesized in order to obtain new compounds with potent anti-inflammatory and analgesic activity with insignificant ulceration. Among the synthesized compounds, (6c), (6e), (6g) and (6l) from triazole series and (7b) and (7e) from Mannich base series were found to exhibit significant anti-inflammatory activity with 59.69, 59.69, 64.69, 79.84, 54.54, 79.69% and 52.55, 57.50, 72.52, 83.03, 60.06, 84.08% inhibition of paw edema at 3 h and 5 h respectively, in comparison to the standard drug ibuprofen (78.93 and 82.58% at 3 h and 5 h). The active compounds were further tested for their analgesic activity and gastric ulceration study. Compounds 6g, 7b and 7e exhibited significant analgesic activity with reaction time (3.60, 3.22, 3.88 s) respectively at 60 min. without causing any gastric irritation. These compounds were also screened for their in vitro antimicrobial activity, Compounds 6f, 6g, 6h, 6l, 6o, 6p, 7a, 7b and 7c showed significant zone of inhibition against various antimicrobial stains. It is concluded that the compounds 6g, 7b and 7e possess a good spectrum of activities. Compound 7e may be considered potent for development of better anti-inflammatory agent. The antimicrobial activity revealed that most of the compounds showed moderate to significant activity. Compounds containing nitro, chloro, bromo and fluoro group showing better activity. All the compounds from 7a, 7b and 7e were active against gram positive bacteria (S. aureus).
Archiv der Pharmazie 11/2011; 345(3):203-14. · 1.71 Impact Factor
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Archiv der Pharmazie 11/2011; 345(3):203 - 214. · 1.71 Impact Factor
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ABSTRACT: A series of novel 2-[4-aryl-5-{(quinolin-8-yloxy)methyl}-4H-1,2,4-triazol-3-ylthio]-1-arylethanones (6a-6j) and 8-{(5-aryl-1,3,4-oxadiazol-2-yl)methoxy}quinolines (7a-7d) were synthesized from the corresponding 4-arnyl-1-(2- quinolin-8-yloxy)acetyl) thiosemicarbazides (4a-4d) and hydrazides (3) respectively. The prepared compounds were screened for their anti-inflammatory, analgesic, ulcerogenic and antimicrobial activities. The anti-inflammatory activities were determined by carrageenan induced rat paw edema method. Compounds 6c, 6d, 6f 6j, 7b and 7e significantly inhibited the rat paw edema depending upon the dose employed. These compounds exhibited insignificant ulceration compared to the standard drug Indomethacin. The compounds were also evaluated for their in vitro antimicrobial activity. Some compounds have shown moderate to good activity whereas compound 7b has shown significant zone of inhibition compared to the standard drug Ampicillin against gram negative microorganisms.
Medicinal chemistry (Shāriqah (United Arab Emirates)) 11/2011; 7(6):663-73. · 1.64 Impact Factor
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ABSTRACT: The hypoglycaemic activity of the ethanolic extract and different fractions of leaves of Bambusa arundinacea were carried out in streptozotocin induced diabetic rats. The effect of the extract and different fractions on biochemical parameters were also assessed to evaluate their activity in controlling diabetes related metabolic conditions. The biochemical parameters include lipid peroxidation, reduced glutathione levels and activity of antioxidant enzymes. The results indicate that the ethyl acetate fraction at 150 mg/kg b.w. significantly lowers blood glucose level (105±15.58 mg/dL) comparable to standard drug glibenclamide (95 ± 10.64 mg/dL) (3 mg/kg b.w.) with insignificant ulceration compared to the standard. Also, there was reduction in lipid peroxidation level and glutathione levels and elevation in the activity of antioxidant enzymes. From the phytochemical investigation, β-sitosterol glucoside and stigmasterol have been isolated in pure form from the ethyl acetate and chloroform fractions. This study suggests that leaf extract of Bambusa arundinacea could be potentially useful for treatment of hyperglycaemia.
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ABSTRACT: The hypoglycaemic activity of the ethanolic extract, petroleum ether and chloroform fractions of leaves of Callistemon lanceolatus were carried out in streptozotocin induced diabetic rats for 30 days. The effect on biochemical parameters (lipid peroxidation, reduced glutathione levels, activity of antioxidant enzymes) were also assessed to evaluate their activity in controlling diabetes related metabolic conditions. The results indicate that the chloroform fraction at 150 mg/kg b.w. significantly lowers blood glucose level with insignificant ulceration compared to the standard drug glibenclamide (3 mg/kg b.w.). Also, there was reduction in lipid peroxidation level and reduced glutathione levels and elevation in the activity of antioxidant enzymes.
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ABSTRACT: Naturally-derived farnesol has been reported for its chemopreventive and chemotherapeutic efficacy in various cancers. However, the mechanism of action of farnesol is still to be elucidated. The present study demonstrates the chemopreventive potential of farnesol on 9,10-dimethylbenz(a)anthracene (DMBA)-initiated and 12-O-tetradecanoylphorbol-13-acetate (TPA)-promoted skin tumorigenesis in Swiss albino mice.
Farnesol at three different doses 25, 50 and 100 mg/kg body weight was topically applied to the mouse skin, 30 min prior to TPA (2 microg/200 microl acetone) to evaluate edema, hyperplasia, expression of cyclooxygenase-2 (COX-2), oxidative stress response and hyperproliferation, and expression of Ras, Raf, p-ERK1/2, Bax and Bcl-2 in DMBA/TPA-induced tumors.
Farnesol at both the low doses significantly reduced the TPA-induced skin edema, hyperplasia, expression of COX-2 and oxidative stress response. Interestingly, higher dose of farnesol did not show any significant response. Pretreatment of farnesol significantly decreased TPA-induced ornithine decarboxylase (ODC) activity and [(3)H]thymidine incorporation in dose-dependent manner. During promotion phase, farnesol with higher dose significantly regressed tumor incidence and tumor burden with an extension of latency period of 4-8 weeks. More importantly, low doses of farnesol significantly inhibited Ras/Raf/ERK1/2 signaling pathway in mouse skin tumors whereas higher dose of farnesol induced the pathway. Moreover, farnesol at all doses altered Bax/Bcl-2 ratio which leads to induction of apoptosis as confirmed by DNA fragmentation.
These findings revealed that oxidative stress, inflammation, Ras/Raf/ERK1/2 pathway and apoptosis collectively played a crucial role in the chemopreventive activity of farnesol to inhibit the murine skin tumorigenesis.
Life sciences 06/2009; 85(5-6):196-205. · 2.56 Impact Factor
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ABSTRACT: Chemical studies on the seeds of Zanthoxylum alatum Roxb. (Rutaceae) led to the isolation of two new phenolic constituents characterized as 3-methoxy-11-hydroxy-6,8-dimethylcarboxylate biphenyl (3) and 3,5,6,7-tetrahydroxy-3',4'-dimethoxyflavone-5-beta-D-xylopyranoside (6), along with the five known compounds, 1-methoxy-1,6,3-anthraquinone, 1-hydroxy-6,13-anthraquinone, 2-hydroxybenzoic acid, 2-hydroxy-4-methoxy benzoic acid, and stigmasta-5-en-3beta-D-glucopyranoside, on the basis of spectral data and chemical analyses.
Journal of Asian natural products research 02/2009; 11(1):91-5. · 0.61 Impact Factor
