Hepatoprotective effects of Astragalus kahiricus root extract against ethanol-induced liver apoptosis in rats / 中国天然药物

The hepatoprotective activity of the ethanol extract of Astragalus kahiricus (Fabaceae) roots against ethanol-induced liver apoptosis was evaluated and it showed very promising hepatoprotective actions through different mechanisms. The extract counteracted the ethanol-induced liver enzymes leakage and glutathione depletion. In addition, it demonstrated anti-apoptotic effects against caspase-3 activation and DNA fragmentation that were confirmed by liver histopathological examination. Moreover, the phytochemical study of this extract led to the isolation of four cycloartane-type triterpenes identified as astrasieversianin II (1), astramembrannin II (2), astrasieversianin XIV (3), and cycloastragenol (4). The structures of these isolates were established by HRESI-MS and 1D and 2D NMR experiments. The antimicrobial, antimalarial, and cytotoxic activities of the isolates were further evaluated, but none of them showed any activity.

effect of calcium channel blockers amlodipine, lacidipine and diltiazem on thermal and visceral pain in mice

The effect of the calcium channel blockers amlodipine, lacidipine and deltiazem was studied after subcutaneous [s.c.] injection in mice using the hot plate and abdominal stretching assays. In the hot-plate test of thermal pain, amlodipine [0.43 and 0.86 mg/kg], lacidipine [0.17 and 0.35 mg/kg] or deltiazem [5.2 and 10.4 mg/kg], produced a dose-related reduction in nociceptive responses. In the acetic acid-induced abdominal constrictions test of visceral pain, amlodipine, lacidipine or deltiazem at the above doses, reduced the number of abdominal constrictions dose-dependently. The inhibition of writhing response by the three drugs was reduced by co-administration of the muscarinic acetylcholine receptor antagonist atropine [1 mg/kg, s.c.], enhanced by co-administration of the alpha-1 adrenoceptor blocker prazosin [1 mg/kg, s.c.], whilst the analgesic effect of lacidipine and deltiazem was reduced by the alpha-2 adrenoceptor blocker yohimbine [5 mg/kg, s.c.]. The analgesic effect of both amlodipine and Iacidipine was unaffected, but that of deltiazem was reduced by the beta adrenoceptor antagonist propranolol [1 mg/kg, s.c.]. The non-selective opioid receptor antagonist naloxone [5 mg/kg, i.p.] enhanced the analgesic effect of amlodipine, but reduced that of deltiazem. Meanwhile, lacidipine anti-nociception was reduced by the non-selective adenosine receptor antagonist theophylline [20 mg/kg, s.c.]. These data suggest that the calcium channel antagonists amlodipine, Iacidipine or deltiazem have analgesic effects in thermal and visceral pain models in mice. Data also indicate that muscarinic acetylcholine receptors mediate at least in part the visceral analgesic effect of these drugs. The antinociceptive effect of lacidipine involves adenosine receptors. The antinociceptive effect of deltiazem involves opioid, alpha-2 and beta adrenoceptors

Effect of Ramipril, Valsartan, Candesartan and Lacidipine on inflammation and gastric ulcer in rats

The present study investigated and compared the effect of the angiotensin converting enzyme inhibitor ramipril and the angiotensin II receptor blockers valsartan and candesartan and the calcium channel blocker lacidipine on inflammation and gastric ulcer in rats. The acute inflammation was induced by intraplantar injection of carrageenan [1%] in the rat hind paw. Gastric ulcer was evoked by s.c. indomethacin [20 mg/kg]. When given s.c. 30 min prior to induction of inflammation, ramipril [0.23 and 0.45 mg/kg], valsartan [7.5 and 15 mg/kg], candesartan [0.72 and 1.44 gm/kg] failed to reduce paw oedema response. Meanwhile, lacidipine at the lower dose of 0.18 mg/kg displayed mild anti-inflammatory activity up to 1 hr, reducing paw odema by 26.7% for 1 hr post-carrageenan, while a higher dose of 0.36 mg/kg inhibited oedema formation by 33.5, 31, 23.6 and 22.3% at 1, 2, 3 and 4 hr post-carrageenan, respectively. The acute gastric mucosal lesions evoked by indomethacin in the rat were aggravated by co-administration of ramipril 0.23 and 0.45 mg/kg, valsartan 7.5 and 15 mg/kg, lacidipne 0.18 and 0.36 mg/kg and candesartan 0.72 mg/kg, but reduced by candesartan 1.44 mg/kg. Findings in the present study do not favor an anti-inflammatory activity for ramipril, valsartan and candesartan, but indicates an antioedema effect for lacidipine at the doses employed. These agents are likely to adversely affect gastric mucosal integrity and enhance the indomethacin-induced gastric injury

Evaluation of the gastric mucosal effects of different antidepressant drugs in the rat

Investigations were performed in the rat to evaluate the effects of different classes of antidepressant drugs on the gastric mucosal damage evoked by indomethacin and on gastric acid secretion. Following pylorus-ligation, indomethacin [20 mg/kg] was given subcutaneously and rats received 2 ml of 0.15 N HCI into their stomachs. Immediately afterwards, the drugs under study were given by the subctaneous route. Rats were killed 4 h after pylorus-ligation, and the number of gastric mucosal lesions were noted, their severity calculated and gastric acid secretory responses determined. The selective 5-hydroxytryptamine [serotonin] reuptake inhibitors [SSRIs] fluoxetine and sertraline caused dose-related increase in the degree of gastric mucosal injury caused by indomethacin. Similar effects were seen on administration of the heterocyclic agent; trazodone. In contrast, the indomethacin-induced lesion scores were remarkably reduced in rats treated with the non-selective noradrenaline and, serotonin reuptake inhibitors; imipramine and amitriptyline. Gastric acid secretion was increased by fluoxetine and sertraline administration, but reduced in rats treated with imipramine or amitriptyline. It is concluded that in the rat, the SSRIs fluoxetine and sertraline and the atypical antidepressant, trazodone, potentiate gastric mucosal damage caused by indomethacin in the presence of acid in the stomach. These results also suggest that changes in gastric acid secretion are involved in the modulatory effects induced by antidepressant drugs on gastric mucosal injury

Pharmaco-chemical investigations of plantago ovata aerial parts

The ethanolic extract of aerial parts of Plantago ovata was successively fractionated into ether, ethyl acetate and n-butanol- ethyl acetate [5:1] soluble fractions. The phenolic fraction of the ether extract afforded the coumarins; imperatorin, xanthotoxin, bergapten, umbeliferone, xanthtoxol and marmesin. The unsaponifiable fraction revealed high percentage of beta-sitosterol and stigmasterol, while the saponifiable part indicated high percentage of palmitolenic and palmitic acids. The ethyl acetate extract afforded a major compound identified as verbascoside and four flavonoids identified as luteolin-7-0-beta-glucopyranoside, luteolin-4-0-beta- glucopyranoside, quercetin 3-0-rhamnoside and the highly methoxylated calycopterin. Also, the n-butanol-ethyl acetate extract showed the same compound verbascoside as a major component. All isolated compounds were identified by chemical and spectral methods of analysis. The analgesic and anti-inflammatory activities of the ethanolic extract fractions [Et2O, EtOAc and n-BuOH-EtOAc] and the major constituent verbascoside were determined on rats