Gastroprotective effect of b-LupeoL: roLe of prostaGLandins, suLfhydryLs and nitric oxide (original) (raw)
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Gastroprotective Effect of β-LupeoL: RoLe of ProstaGLandins, SuLfhydryLs and Nitric Oxide
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This investigation evaluated the gastroprotective effect of β-lupeol, isolated from Pseudobombax ellipticum. Gastric mucosal damage was induced in rats by intragastric ethanol (1mL/rat). Rats treated orally with β-lupeol suspended in Tween 80 at 3, 10, 30 and 100 mg/kg, showed 21, 60, 79 and 77 % gastroprotection respectively. The gastroprotection observed at 30 mg/kg for this compound was reverted in rats pretreated with indomethacin (10 mg/kg. s.c.) or N-ethylmaleimide (NEM 10 mg/kg, s.c.), suggesting that the gastroprotective mechanism of this triterpene involves, at least in part, the participation of prostaglandins and endogenous sulfhydryls. The gastroprotective effect of β-lupeol was not affected by the pretreatment with L-NAME (70 mg/kg, i.p.), a nitric oxide (NO)-synthase inhibitor. Carbenoxolone was used as gastroprotective model drug and showed dose dependent gastroprotective effect (26, 44 and 88% of gastroprotection, at 1, 10 and 30 mg/kg, respectively). The participation of prostaglandins, sulfhydryls and nitric oxide was observed in the gastroprotective mechanism of carbenoxolone.
Gastroprotective effect of Astragaloside IV: role of prostaglandins, sulfhydryls and nitric oxide
Journal of Pharmacy and Pharmacology, 2005
This investigation evaluated the gastroprotective effect of β-lupeol, isolated from Pseudobombax ellipticum. Gastric mucosal damage was induced in rats by intragastric ethanol (1mL/rat). Rats treated orally with β-lupeol suspended in Tween 80 at 3, 10, 30 and 100 mg/kg, showed 21, 60, 79 and 77 % gastroprotection respectively. The gastroprotection observed at 30 mg/kg for this compound was reverted in rats pretreated with indomethacin (10 mg/kg. s.c.) or N-ethylmaleimide (NEM 10 mg/kg, s.c.), suggesting that the gastroprotective mechanism of this triterpene involves, at least in part, the participation of prostaglandins and endogenous sulfhydryls. The gastroprotective effect of β-lupeol was not affected by the pretreatment with L-NAME (70 mg/kg, i.p.), a nitric oxide (NO)-synthase inhibitor. Carbenoxolone was used as gastroprotective model drug and showed dose dependent gastroprotective effect (26, 44 and 88% of gastroprotection, at 1, 10 and 30 mg/kg, respectively). The participation of prostaglandins, sulfhydryls and nitric oxide was observed in the gastroprotective mechanism of carbenoxolone.
Lupeol and lupeol esters protect the gastric ulcer in rats
Natural Products: An Indian Journal, 2014
Objective: The lupeol isolated from the bioassay guided fractionation of the ethanol extract from the stem bark of the Crataeva nurvala, showed promising antiulcer effect in our random screening programme of natural products. Therefore we planned to make some derivatives of the lupeol, whichmay further enhance the antiulcer activity.Materials andmethods:A one-step synthesis of long chain fatty acid and aromatic esters derivative of the lupeol with different acid halides and acids were done. A series of esters derivatives of lupeol were prepared and bio assayed for the antiulcer activity in Cold restraint induced gastric ulcer(CRU). Results: Few derivatives of lupeol (Lupeol acetate, Lupeol toluate, Lupeol palmitate, Lupeol stearate,) showed more potent percentages of antiulcer activity in Cold restraint induced gastric ulcer model in rats (table-1) as compared to the basic molecule lupeol. Conclusion: In our studies it was found that the esters derivatives of lupeol posses better an...
Gastroprotective effect of lupeol on ethanol-induced gastric damage and the underlying mechanism
Inflammopharmacology, 2009
The effect of lupeol, a natural pentacyclic triterpene on ethanol-induced gastric damage in mice was evaluated. The gastroprotection was assessed by determination of changes in mean gastric lesion area, quantification of mucosal non-protein sulfhydryls (NP-SH), and characterized using drugs that influence the endogenous prostaglandins, a 2 -adrenoceptors, nitric oxide, K ATP -channels, and intracellular calcium. Orally administered lupeol (3, 10, and 30 mg/kg) significantly and dose-dependently attenuated the ethanol-induced gastric damage by 39-69%, whereas the positive control N-acetylcysteine (NAC, 300 mg/kg, i.p.) afforded 32% protection. Both lupeol and NAC restored the NP-SH depleted by ethanol but the lupeol effect was only marginal. Lupeol gastroprotection was attenuated by indomethacin and L-NAME, the respective COX and NO-synthase inhibitors and was weakly sensitive to a 2 -adrenergic antagonist yohimbine and K ATP -channel blocker glibenclamide, but more profoundly to calcium blocker verapamil. These pharmacological effects of lupeol may synergistically contribute to alleviating the ethanolassociated gastric damage, which is multifactorial.
A Review on Pharmacological Activities of Lupeol and its Triterpene Derivatives
Journal of Drug Delivery and Therapeutics
Lupeol is a pentacyclic triterpenoid commonly distributed in the plant kingdom and is found in edible fruits and vegetables. It is a naturally occurring triterpene that is used to reduce the inflammatory responses and also have immunomodulating properties. Lupeol and its derivatives have a great potential to act as an anti- inflammatory, anti-microbial, anti-proliferative, anti-invasive, anti-angiogenic, anti-protozoal, and cholesterol-lowering agent. Various studies have shown that anti-inflammatory activity of lupeol through the modulation of p-38 pathways inhibits neuroinflammation in the cerebellum and induces neuroprotection. It has been also found effective on lung cancer (i.e A427 cancer cells and normal MRC-5 cells). Observation of inhibiting the growth of lung cancer cells is checked by MTT assay. Lupeol and its ester lupeol linoleate have been used to reduce the levels of hypercholesterolemia in the rats and decrease the activities of such enzymes namely Na+, K+-ATPase, Ca2...
Journal of Pharmacy and Pharmacology, 2008
The gastroprotective effect of DDF (3,6-dimethoxy-6 6 -dimethyl-2 3 7 8 -chromeneflavone) from Lonchocarpus araripensis Benth. (Leguminosae) on gastric damage induced by absolute ethanol (96%, 0.2 mL/mouse) and indometacin kg −1 , p.o.) in mice was investigated. Intraperitoneally administered DDF at dose levels of 50, 100 and 200 mg kg −1 markedly reduced the gastric lesions in the ethanol model by 62, 72 and 96%, and in the indometacin model by 34, 70 and 75%, respectively, as compared with misoprostol (50 g kg −1 , p.o.), the reference compound that caused lesion suppression by 67% in ethanol model and by 72% against indometacin-induced ulceration. The ED50 of DDF in reducing gastric lesions induced by ethanol and indometacin (dose of the DDF that reduced the gastric lesion area by 50% in relation to the control value) was 50.87 and 61 56 mg kg −1 , respectively. Mechanistic studies were carried out at 100 mg kg −1 DDF using the ethanol model. Compared with N-acetylcysteine (750 mg kg −1 , p.o.), a donor of sulfhydryls, DDF only partially replenished the ethanol-induced depletion of gastric mucosal NP-SH. Pretreatment with TRPV1 antagonist capsazepine (5 mg kg −1 , i.p.) or the non-selective cyclooxygenase inhibitor indometacin (10 mg kg −1 , p.o.) effectively blocked the gastroprotective effect of DDF 100 mg kg −1
Lupeol Stearate Accelerates Healing and Prevents Recurrence of Gastric Ulcer in Rodents
2021
The gastric healing and gastric ulcer recurrence preventive effect of Lupeol Stearate (LS) was measured in this study. To evaluate the gastric healing effect, rats were submitted to the 80% acetic acid-induced ulcer model and treated with vehicle (1 ml/kg, p.o.), LS (1 mg/kg, p.o.) or omeprazole (20 mg/kg, p.o.) twice a day for seven days. The gastric injury was evaluated macroscopically, histologically and histochemical; and biochemical parameters were also quantified. To evaluate the effects of LS on gastric ulcer recurrence, mice were ulcerated by gastric instillation of 10% acetic acid and treated with vehicle (1 ml/kg, p.o.), LS (1 mg/kg, p.o.) or ranitidine (20 mg/kg, p.o.) twice a day for ten days. Then, the ulcer recurrence in these animals was induced by IL- 1β (1 µg/kg i.p) at five day after the end of the treatment period. The area of the lesion recurred were measured, as well as the activity of myeloperoxidase and TNF levels. Oral treatment with LS accelerated gastric he...
Biological Activities of Lupeol
This review covers mainly the past 25 years of research on the biological activities of lupeol, a significant lupane-type triterpene represented in the plant, fungi and animal kingdoms. Anticancer, antiprotozoal, chemopreventive and anti-inflammatory properties, plus the mechanisms of action of lupeol are emphasized. Some insights are provided regarding lupeol as a lead scaffold for synthetic chemical attempts to optimize pharmacological potency. Structure-activity relationship is also discussed.
Fundamental & Clinical Pharmacology, 2010
(-)-α-Bisabolol is an unsaturated, optically active sesquiterpene alcohol obtained by the direct distillation essential oil from plants such as Vanillosmopsis erythropappa and Matricaria chamomilla. (-)-α-Bisabolol has generated considerable economic interest, since it possesses a delicate floral odor and has been shown to have anti-septic and anti-inflammatory activity. The aim of this work was to evaluate the gastroprotective action of (-)-α-bisabolol on ethanol and indomethacin-induced ulcer models in mice, and further investigate the pharmacological mechanisms involved in this action. The oral administration of (-)-α-bisabolol 100 and 200 mg/kg was able to protect the gastric mucosa from ethanol (0.2 mL/animal p.o.) and indomethacin-induced ulcer (20 mg/kg p.o.). Administration of l-NAME (10 mg/kg i.p.), glibenclamide (10 mg/kg i.p.) or indomethacin (10 mg/kg p.o.) was not able to revert the gastroprotection promoted by (-)-α-bisabolol 200 mg/kg on the ethanol-induced ulcer. Dosage of gastric reduced glutathione (GSH) levels showed that ethanol and indomethacin reduced the content of non-protein sulfhydryl (NP-SH) groups, while (-)-α-bisabolol significantly decreased the reduction of these levels on ulcer-induced mice, but not in mice without ulcer. In conclusion, gastroprotective effect on ethanol and indomethacin-induced ulcer promoted by (-)-α-bisabolol may be associated with an increase of gastric sulfydryl groups bioavailability leading to a reduction of gastric oxidative injury induced by ethanol and indomethacin.
Journal of Ethnopharmacology, 2010
Ethnopharmacological relevance: Validate the popular use of Plectranthus grandis in gastric disorders through the active components. Aims: Isolation of barbatusin (BB) and 3-hydroxy-3-deoxibarbatusin (BBOH), diterpenes from Plectranthus grandis, and evaluation of their gastroprotective effect and possible mechanisms of action. Materials and methods: Isolation and chemical characterization of diterpenes from Plectranthus grandis by chromatographic and spectroscopic methods and evaluation of gastroprotective action of the diterpenes through ethanol-induced gastric injury in mice model. It was evaluated the effect of capsazepine, indomethacin and the role of nitric oxide and K ATP− channels on the gastroprotective effect of BBOH and BB. Additionally it was measured the concentrations of gastric mucus, non-proteic-sulfhydryl groups and total thiobarbituric acid-reactive substances. Results: Orally administered BBOH and BB at doses of 5 and 10 mg/kg, markedly reduced the gastric lesions by 59 and 96%, and 32 and 76%, respectively, with superior results as compared to N-acetylcysteine (150 mg/kg, i.p.), reference compound that caused 85% lesion suppression. Although BBOH presented a higher gastroprotection than BB they act by similar mechanisms in relation to N-acetylcysteine, and prevent the depletion of gastric mucus, gastric mucosal non-proteic-sulfhydryl groups as well as the increase in thiobarbituric acid-reactive species. Moreover, the gastroprotective effect of BB was effectively blocked in mice pretreated with TRPV1 antagonist capsazepine, by the non-selective cyclooxygenase inhibitor indomethacin, or by the nitric oxide synthase inhibitor l-NAME but not by K + ATP channel inhibitor glibenclamide. In contrast, the gastroprotective effect of BBOH was blocked only by indomethacin and glibenclamide pretreatments. Conclusion: The protective role for BBOH and BB affording gastroprotection against gastric damage induced by ethanol indicates that these compounds contribute for the activity of Plectranthus species. The different modes of action are probably related to differences in their chemical structure.