Antiulcer activity of methanolic extract and fractions of Picralima nitida seeds(Apocynacaea) in rats.

OBJECTIVE: To investigated the antisecrectory activities of the methanol extract, chloroform fraction and methanol fraction of Picralima nitida seeds. METHODS: The methanol extract of Picralima nitida seeds was fractionated into chloroform fraction and methanol fraction. They were evaluated for antiulcer activity and gastric emptying time in rats using aspirin-pylorus-ligation model. RESULTS: Oral administration of the methanol extract, chloroform fraction and methanol fraction at 1 000 mg/kg reduced gastric ulcer by 56.4%, 40.0% and 56.3%, respectively; and the fractions of the extract significantly (P<0.05) reduced gastric emptying time when compared to the control. Gastric acidity was significantly decreased when compared with saline group, 40.25 mEq/L in methanol extract, 50.0 mEq/L in chloroform fraction 51.25 mEq/L in methanol fraction but had no significant effect on the gastric secretion volume. CONCLUSIONS: These findings showed that methanol extract, chloroform fraction and methanol fraction of the seeds of Picralima possessed potent antiulcer properties and some antisecretory properties.

Antisecretory actions of Baccharis trimera (Less.) DC aqueous extract and isolated compounds: analysis of underlying mechanisms.

ETHNOPHARMACOLOGICAL RELEVANCE: Baccharis trimera (Less.) DC. (Asteraceae) is a species native to South America used in Brazilian folk medicine to treat gastrointestinal and liver diseases, kidney disorders and diabetes. Previous studies from this laboratory confirmed the antacid and antiulcer activities of the plant aqueous extract (AE) in rat and mouse models. AIM OF THE STUDY: To investigate the mechanisms involved in the antacid action of AE and isolated compounds from Baccharis trimera. MATERIALS AND METHODS: AE was assayed in vivo in cold-restraint stress gastric ulcers and in pylorus-ligated mice. Nine fractions (F2-F10) previously isolated from AE were assayed in vitro on acid secretion measured as [(14)C]-aminopyrine ([(14)C]-AP) accumulation in rabbit gastric glands, and on gastric microsomal H(+), K(+)-ATPase preparations. Chlorogenic acids (F2, F3, F6, F7), flavonoids (F9), an ent-clerodane diterpene (F8) and a dilactonic neo-clerodane diterpene (F10) have been identified in these fractions. RESULTS: Intraduodenal injection of AE (1.0 and 2.0 g/kg) in 4h pylorus-ligated mice decreased the volume (20 and 50%) and total acidity (34 and 50%) of acid secretion compared to control values. Administered orally at the same doses AE protected against gastric mucosal lesions induced in mice by restraint at 4°C. Exposure of isolated rabbit gastric glands to fractions F8 (10-100 µM) and F9 (10-300 µg/ml) decreased the basal [(14)C]-AP uptake by 50 and 60% of control (Ratio=6.2±1.1), whereas the remaining fractions were inactive. In the presence of the secretagogues F2 and F4 (30-300 µg/ml) decreased the [(14)C]-AP uptake induced by histamine (His) with a 100-fold lower potency than that of ranitidine. F5 and F6 reduced the [(14)C]-AP uptake stimulated by carbachol (CCh), but they were 10 to 20-fold less potent than atropine. F8 (diterpene 2) and F9 (flavonoids) decreased both the His- and CCh-induced [(14)C]-AP uptake, whereas F10 (diterpene 1) was inactive against the [(14)C]-AP uptake stimulated by secretagogues. Diterpene 2 was the most active of all tested compounds being 7-fold less potent than ranitidine and equipotent to atropine in reducing acid secretion in vitro. This compound also reduced the gastric H(+), K(+)-ATPase activity by 20% of control, while the remaining fractions were inactive on the proton pump in vitro. CONCLUSIONS: The results indicate that Baccharis trimera presents constituents that inhibit gastric acid secretion by acting mainly on the cholinergic regulatory pathway. The plant extract also contains compounds that exert moderate inhibition of the histaminergic regulatory pathway of acid secretion and the gastric proton pump. Altogether these active constituents appear to provide effective inhibition of acid secretion in vivo, which may explain the reputed antiulcer activity of the plant extract.

Effects of Nidus Vespae extract and chemical fractions on the growth and acidogenicity of oral microorganisms.

Nidus Vespae is the honeycomb of Polistes Olivaceous (De Geer), P. Japonicus Saussure, and Parapolybiavaria Fabricius. It is known to have a number of pharmacological effects, including antimicrobial, anti-inflammatory, anti-virus, anti-tumor and anesthetic properties. The present study evaluated the antimicrobial activity and acid inhibition properties of extracts and chemical fractions of Nidus Vespae. The raw material was first extracted using 95% ethanol/water. Subsequent fractions were prepared from this extract using cyclohexane/ethyl acetate, petroleum ether/ethyl acetate, and chloroform/methanol. For the antimicrobial activity assays, minimum inhibitory concentrations (MIC) and minimum bactericidal concentrations (MBC) were determined using the microdilution method. The chloroform/methanol (Chl/MeOH) fraction showed the highest antibacterial activities with a MIC of 8-16mg/ml and an MBC of 16-32mg/ml. In addition, the extract and chemical fractions of Nidus Vespae showed a remarkable capacity for inhibiting the acid production of common oral bacteria at sub-MIC concentrations. Sub-MIC levels of the petroleum ether/ethyl acetate fraction significantly inhibited acid production by Streptococcus mutans ATCC 25175. The significant antiacidogenic activity demonstrated by Nidus Vespae shows it to be a promising source of novel anticariogenic agents.