Barthelemy Nyasse

Antitrypanosomal alkaloids from Polyalthia suaveolens (Annonaceae): Their effects on three selected glycolytic enzymes of Trypanosoma brucei

In continuation of our study on medicinal plants of Cameroon, stem barks of Polyalthia suaveolens were phytochemically studied. This investigation yielded a new indolosesquiterpene alkaloid, named polysin (1) and four hitherto known alkaloids (2-5). Polysin (1) appeared as a competitive reversible inhibitor (K(i)=10 microM) of phosphofructo kinase (PFK) of Trypanosoma brucei with respect to fructose-6-phosphate (K(i)/K(M)=0.05) and could be used in the design of new trypanocidal drugs. The other isolated compounds (2-5) also exhibited interesting inhibitory effects on selected glycolytic enzymes (PFK, glyceraldehyde-3-phosphate dehydrogenase and aldolase).

Antibacterial activity of selected Cameroonian dietary spices ethno-medically used against strains of Mycobacterium tuberculosis

ETHNOPHARMACOLOGICAL RELEVANCE Tuberculosis (TB) is considered as a re-emerging disease and one of the most important public health problems worldwide. The use or (in most cases) misuse of existint anti-tuberculosis drugs over the years has led to an increasing prevalence of resistant strains, establishing an urgent need to search for new effective agents. Spices are largely used ethno-medically across Africa. AIM OF THE STUDY The present study aimed to evaluate the in vitro antimycobacterial activities of a total of 20 methanol crude extracts prepared from 20 Cameroonian dietary spices for their ability to inhibit the growth of or kill Mycobacterium tuberculosis strains H(37)Rv (ATCC 27294) and H(37)Ra (ATCC 25177). MATERIALS AND METHODS The antituberculosis screening was performed using the Microplate Alamar Blue Assay (MABA) method to determine the minimum inhibitory concentration (MIC) and the minimum mycobactericidal concentration (MBC). RESULTS Fifteen (15) plant extracts out of 20 showed varied levels of antimycobacterial activity against the strains M. tuberculosis H(37)Rv and H(37)Ra, with MICs in the range of 2.048-0.016 mg/ml. The extract of Echinops giganteus exhibited the most significant activity with a MIC value of 32 μg/ml and 16 μg/ml, respectively against H(37)Ra and H(37)Rv. To the best of our knowledge, the antimycobacterial activity of the tested spices has not been reported before and therefore our results can be evaluated as the first report about the antimycobacterial properties. CONCLUSIONS The results of this study suggest that Echinops giganteus and Piper guineense could be important sources of bactericidal compounds against M. tuberculosis and could probably be promising candidates that can be further investigated.

Gastric cytoprotective anti-ulcer effects of the leaf methanol extract of Ocimum suave (Lamiaceae) in rats.

The anti-ulcerogenic potential of the leaf methanol extract of Ocimum suave (Lamiaceae) was investigated using four methods of gastric lesion induction in experimental Wistar rats (150-200 g): (1) HCl/ethanol-induced gastric lesions, (2) Absolute ethanol-induced gastric lesions, (3) Indomethacin-HCl/ethanol-induced gastric lesions, (4) Pylorus ligation-induced gastric lesions. Administration of the extract of O. suave to the rats by oral route (75-500 mg/kg) dose-dependently prevented the formation of acute gastric lesions induced using the four experimental techniques. The dose-dependent reduction of lesion formation was in all cases accompanied by significant increases in gastric mucus production. At the dose of 250 mg/kg there was complete inhibition of gastric lesions induced using the HCl/ethanol solution. Pre-treatment, by intraperitoneal route, with indomethacin significantly reduced the ability of the extract to inhibit the formation of HCl/ethanol-induced lesions. When the rats were subjected to pylorus ligation, the dose of 500 mg/kg completely inhibited lesion formation but did not have any effect on gastric acid secretion compared with the controls. The mucus secretion promoting effect of the extract was most significant when the gastric environment was highly acidic. These results suggest that a new anti-ulcer therapy regimen may be formulated which does not require the use of antacids and anti-secretory agents.

Antifilarial activity in vitro of polycarpol and 3-O-acetyl aleuritolic acid from cameroonian medicinal plants against Onchocerca gutturosa.

Previous results have revealed the antifilarial activities of crude extracts and pure compounds from some Cameroonian medicinal plants against Onchocerca volvulus and Onchocerca gutturosa. In our efforts to find new filaricidal agents against adult male O. gutturosa worms, we have isolated and screened three compounds: polycarpol and polyveoline from Polyalthia suaveolens (Annonaceae) and 3-O-acetyl aleuritolic acid from Discoglypremna caloneura (Euphorbiaceae). Only polycarpol and 3-O-acetyl aleuritolic acid exhibited significant inhibitory activities on the vitality of adult male worms of O. gutturosa using Amocarzine as positive control compound. The motility reduction values were 28.6 and 57.1%, and the inhibition of MTT reduction values 80.0 and 64.8% respectively.

Prophylactic and healing properties of a new anti-ulcer compound from Enantia chlorantha in rats.

Decoctions prepared from Enantia chlorantha are used in the traditional treatment of some forms of ulcers. We have tested the anti-ulcer actions of a novel protoberberine-type alkaloid (7,8,-dihydro-8-hydroxypalmatine (1)) obtained from the bark of E. chlorantha using the HCl/ethanol, absolute ethanol and pylorus ligation techniques. The healing effect on chronic acetic acid-induced gastric ulcer was also tested. 1 (50 and 100 mg/kg) dose-dependently inhibited the formation of gastric ulcers induced by HCl/ethanol (35-52% inhibition), absolute ethanol (46-53% inhibition) and pylorus ligation (38-62% inhibition). The prophylactic actions were associated with significant increases in gastric mucus production compared with the controls. The significant inhibition of pylorus-ligated ulcers occurred at gastric acid concentrations (83 mEq/l) previously known to induce severe gastric ulceration in rats. The ulcer-healing test showed significant macromorphological and histological acceleration of healing following 10-day treatment with 1 (40 - 80 mg/kg). The results show that 1 has no anti-secretory effects. The prophylactic anti-ulcer effects are associated with enhanced mucus production, which is an important factor in the mechanism of the local healing process of chronic gastric ulcers.

A 7,8-dihydro-8-hydroxypalmatine from Enantia chlorantha

7,8-dihydro-8-hydroxypalmatine, a novel protoberberine-type alkaloid, along with palmatine, has been isolated and characterized from an anti-HIV active extract from Enantia chlorantha. The structures of the two compounds were elucidated by spectroscopic analyses and from chemical evidence.

Anti-ulcer actions of the bark methanol extract of Voacanga africana in different experimental ulcer models in rats.

The antiulcerogenic effects of the bark methanol extract of Voacanga africana were studied using various experimental ulcer models in rats. The effects of the extract on the volume of gastric juice, gastric pH, acid output, mucus production and peptic activity were recorded, as well as the preventive action against lesions caused by HCl/ethanol and indomethacin. Oral administration of the extract (500-750 mg/kg) inhibited the formation of gastric lesions induced by HCl/ethanol (40-63% inhibition). The inhibitory effect against HCl/ethanol was significantly (P<0.01) suppressed by pre-treatment of the rats with indomethacin (30 mg/kg, i.p.). The extract significantly reduced gastric lesion formation in pylorus ligated rats, but this was not associated with an increase in gastric mucus production or with a reduction in acid content, volume of gastric secretion or pepsin activity of the gastric juice.

Anti-ulcer compound from Voacanga africana with possible histamine H2 receptor blocking activity

Voacanga africana is used in Cameroonian ethnomedicine for the treatment of peptic ulcers. We have tested the cytoprotective, anti-secretory and ulcer healing actions of an alkaloid (TN) obtained from the fruit extract. Oral administration of TN (50-100 mg/kg) dose-dependently prevented ulcer formation by HCl/ethanol (36-75%), absolute ethanol (43-75%), HCl-ethanol/indomethacin (58-84%), Pylorus ligation (31-100%), cold restraint stress (68-100%) and histamine (49-100%). The inhibitory effect at 50 and 100 mg/kg against HCl/ethanol was not suppressed by pre-treatment with indomethacin (20 mg/kg, i.p.). TN reduced Shay-ligated gastric acid secretion from 77 mEq/l in the controls to 46 and 25 mEq/l for the 50 and 100 mg/kg doses. Augmented histamine-induced gastric acid secretion was reduced from 84 mEq/l in the controls to 45 and 21 mEq/l for the two doses of TN, with total inhibition of gastric and duodenal ulcers by the 50 mg/kg dose. Healing rate of chronic acetic acid-induced ulcers was 62 and 83%, respectively, for the dose of 50 and 100 mg/kg of TN compared with the controls. TN has gastric anti-secretory effects similar to histamine receptor blockers. Its cytoprotective and ulcer healing properties are related to its ability to strengthen gastric mucosal defenses through enhanced gastric mucus production.

Aporphine alkaloids from Enantia chlorantha

Abstract Two novel aporphine alkaloids, named 6a,7-dehydro-1,2-dimethoxy-7-hydroxy- N -methylaporphine (1) and 6a,7-dehydro-1,2-dimethoxy-7-hydroxyaporphine (2) , have been isolated from the stem bark of E. chlorantha .

In vitro inhibitory effects of palmatine from Enantia chlorantha on Trypanosoma cruzi and Leishmania infantum.

In an attempt to establish the components responsible for the use of Enantia chlorantha against cutaneous leishmaniasis in local traditional medicine, a well-known palmatine has been isolated in substantial amounts from a methanolic bark extract of this plant species. Palmatine therein obtained exhibited a significant inhibitory activity on growth of both Trypanosoma cruzi (IC50 0.068 µM) and Leishmania infantum (IC50 0.79 µM).