Cytotoxic and Schistosomidal Activities of Extract, Fractions and Isolated Compounds from Zanthoxylum Leprieurii (Rutaceae)

Schistosomiasis is a major and chronic neglected tropical disease. The existing treatment does not kill immature schistosomes and have serious adverse side effect.  It is well known that some parasites are responsible for causing specific cancers in humans including bladder cancer from Schistosoma haematobium infection. So, novel drugs discovery is an urgent need. In this study, were evaluated in vitro the cytotoxic on human hepatocarcinoma (HepG2) and normal cells (Chang liver), and the schistosomicidal properties of crude extract, fractions and isolated compounds (1-Hydroxy-3-methoxy-N-methylacridone (1) described in this species from Cameroon for the first time, Scoparone (2), and Arborinine (3)) from powdered fruits of Zanthoxylum leprieurii (Rutaceae). All fractions: hexanic (FH), methylene chloride (FC), ethyl acetate (FA) and methanolic (FM) killed all the cercariae within 2 hours exposure and presents LC50 values between 2 and 3 μg/ml; Compounds 1 and 3 also displayed a good in vitro schistosomicidal activity against cercariae with LC50 values of 78.78 and 6.98 μg/mL, respectively. For antitumor activity compounds 1-3 and fraction FC presents good activity with IC50 values range 18.27 - 74.61 μg/mL on HepG2 cells, however most of these were more toxic on Chang cells than to HepG2 cells, with only exception for compound 2. The acridone Arborinine (3) can constitute a good lead for the research of schistosomiasis alternative therapy, and the coumarin Scoparone (2) can be used in drug design as scaffold for design new potential anticancer agents

Documenting indigenous knowledge about Africa’s traditional medicine: A myth or a reality?

This article examines the global debates about indigenous knowledge and Africa’s traditional medicine. It explores whether it is possible to document all the elements of indigenous knowledge about Africa’s traditional medicine that is used for the treatment of diverse forms of sickness. Certain types of Africa’s traditional medicines used for the treatment of different forms of sickness encompass associated knowledge in the form of spiritual rituals that may be considered mostly by religious leaders as devilish in nature. It may be difficult to document the spiritual elements of traditional medicine that is deemed devilish as traditional healers consider it top secret. The non-documentation of the spiritual rituals that form part of the traditional medicine is tantamount to documenting certain elements and not the entire process of a particular medicine. The raison d'être for documenting Africa’s traditional medicine stem from the notion that there is an increasing extinction of medicinal plants due to environmental degradation, deforestation, agricultural encroachment, over harvesting and population growth that is associated with the loss of indigenous knowledge on plant use for medicine. Hence there is a need to document medicinal plants with their associated knowledge. The article explores Africa’s traditional medicines that can and cannot be documented in its entirety and proposes measures within Intellectual Property Rights (IPR) in the form of patents through which certain types of traditional medicines used for the treatment of particular illnesses could be documented in their entirety.Keywords: Africa’s traditional medicine, indigenous knowledge, Intellectual Property Rights (IPR) – paten

Rapid in vivo screening method for the evaluation of new anti helicobacter medicinal preparations

The objective of this study was to devise a rapid mouse model for the in vivo screening of new anti Helicobacter pylori products. Six to eight week-old mice pre-treated (7 days) with Amoxicillin/Metronidazole (25 mg/kg) to eliminate all Helicobacter-like organisms were inoculated (4x per week) with 200 µl of a bacterial culture (108 CFU/ml of H. pylori CCUG-39500). Colonisation of mouse stomach was assessed from day 1 to 15 post inoculation by the Gram stain, rapid urease test and antral mucus culture. These findings were used as a mouse model of Helicobacter pylori infection to assess the in vivo anti Helicobacter activities of two plant-derived molecules with proven cytoprotective, ulcer healing and in vitro anti Helicobacter properties (TN, a tabersonine chloride alkaloid from the fruits of Voacanga Africana and PAL, a protoberberine alkaloid ((7,8-dihydro-8-hydroxy-palmatine) from the bark of Enantia chlorantha). For up to 6 days post inoculation, the test organisms were recoverable by culture from 87.5% of the antral mucus samples while 100% of Gram stains were positive. The infection tended to clear naturally from day 9. Fifteen days post infection, only Gram stains were still positive (37.5%). Three-day oral administration of TN, PAL (50 mg/kg) and Metronidazole (25 mg/kg) completely eliminated the bacterial strain from the gastric antral mucus compared with the controls. This 4-week model is proposed as a rapid screening tool for in vivo evaluation of new anti H. pylori products in order to select candidates for detailed investigations. African Journal of Traditional, Complementary and Alternative Medicines Vol. 3(4) 2006: 102-11

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 mu M) 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). Crown Copyright (C) 2010 Published by Elsevier Ltd. All rights reserved

Research Paper - HEALING EFFECT ON CHRONIC GASTRIC ULCERS AND SHORT-TERM TOXICITY PROFILE OF THE LEAF METHANOL EXTRACT OF OCIMUM SUAVE WILD (LAMIACEAE) IN RATS

The gastric cytoprotective actions of the extract of Ocimum suave wild (lamiaceae) have previously been demonstrated. We have investigated here the healing effect of the leaf methanol extract of Ocimum suave against chronic gastric ulcers induced in experimental rats. Chronic gastric ulcers were induced using acetic acid and the induced ulcers treated over a period of two weeks using daily oral doses (125 - 500 mg/kg) of the extract. Possible toxic effects of the extract given in the short term were also investigated. The extract reduced ulcer indices from 50.40 in the 4-day controls to 11.8, 5.8, and 3.6, respectively, for the rats receiving 125, 250 and 500 mg/kg of the extract. The highest dose of the extract (500 mg/kg) showed a highly significant (P < 0.001) reduction of ulceration with a corresponding healing rate of 81.25 per cent. Treatment with the plant extract was also associated with a significant increase in mucus production up to 57 per cent (P < 0.01) for the 500 mg/kg dose. A similar increase in mucus production was not observed with ranitidine although it generated a healing rate of 66 per cent. No apparent toxicity signs were observed through food and fluid intakes, vital organ weights, animal behaviour, stool texture, red and white blood cell counts and histopathological evaluation. The results of the present study show that in addition to the previously demonstrated cytoprotective antiulcer actions of the leaf methanol extract of O. suave, the extract also possesses potent healing effects against chronic gastric ulcers. Enhanced mucus production appears to play a significant role in the mode of action of the extrac

HEALING EFFECT ON CHRONIC GASTRIC ULCERS AND SHORT-TERM TOXICITY PROFILE OF THE LEAF METHANOL EXTRACT OF OCIMUM SUAVE WILD (LAMIACEAE) IN RATS

The gastric cytoprotective actions of the extract of Ocimum suave wild (lamiaceae) have previously been demonstrated. We have investigated here the healing effect of the leaf methanol extract of Ocimum suave against chronic gastric ulcers induced in experimental rats. Chronic gastric ulcers were induced using acetic acid and the induced ulcers treated over a period of two weeks using daily oral doses (125 – 500 mg/kg) of the extract. Possible toxic effects of the extract given in the short term were also investigated. The extract reduced ulcer indices from 50.40 in the 4-day controls to 11.8, 5.8, and 3.6, respectively, for the rats receiving 125, 250 and 500 mg/kg of the extract. The highest dose of the extract (500 mg/kg) showed a highly significant (P < 0.001) reduction of ulceration with a corresponding healing rate of 81.25 per cent. Treatment with the plant extract was also associated with a significant increase in mucus production up to 57 per cent (P < 0.01) for the 500 mg/kg dose. A similar increase in mucus production was not observed with ranitidine although it generated a healing rate of 66 per cent. No apparent toxicity signs were observed through food and fluid intakes, vital organ weights, animal behaviour, stool texture, red and white blood cell counts and histopathological evaluation. The results of the present study show that in addition to the previously demonstrated cytoprotective antiulcer actions of the leaf methanol extract of O. suave, the extract also possesses potent healing effects against chronic gastric ulcers. Enhanced mucus production appears to play a significant role in the mode of action of the extrac

Antitrypanosomal activity of polycarpol from Piptostigma preussi (Annonaceae).

Polycarpol, sitosterol and sitosterol-3-O-beta-D-glucoside isolated for the first time from Piptostigma preussi (Annonaceae) occur regularly in some Annonaceae such as Piptostigma genus. Polycarpol exhibits interesting antitrypanosomal activity with an ED(50) value of 5.11 muM on Trypanosoma brucei cells. Moreover, it inhibits T. brucei glycolytic enzymes GAPDH and PFK with IC(50) values of 650 and 180 muM respectively