In vitro evaluation of aliphatic fatty alcohol metabolites of Perseaamericana seed as potential antimalarial and antimicrobial agents.

Perseaamericana Mill (Lauraceae) is a local medicinal plant used in Nigerian ethnomedicine as antimalarial. The aqueous decoction of the root part is a potent remedy against bacterial infections. Hence, the need to investigate the phytochemical and biological activities (antimicrobial and antiplasmodial) of the root back of Perseaamericana. Chromatographic and spectroscopic techniques were used in the identification and purification of metabolites, which were assayed for antimalarial and antimicrobial activities using Plasmodium falciparum and a panel of microorganisms. From the seeds of P. americana, five known 1, 2, 4-dihydroxy derivatives aliphatic alcohols, called avocadenols were isolated and identified by spectroscopic methods including 1D- and 2D NMR, and comparison with reported data in literature. Antifungal activity for 1, 2, 4-Trihydroxyheptadec-6-en-16-yne (5) (IC50< 8 µg/mL) against all the fungal strains and S. areus, and antimalarial activity for compounds 1, 2, 4-Trihydroxyheptadec-16-ene (1) and 1, 2, 4-tetrahydroxyheptadecane-6, 16-diene(2) (IC50 = 1.6 and 1.4 µg/mL for the D6 clone, respectively, and 2.1 and 1.4 µg/mL for the W2 clone, respectively) was observed. The fatty alcohols 1, 2, 4-tetrahydroxyheptadecane-6, 16-diene(2); 1, 2, 4-Trihydroxyheptadec-16-yne(3) and 1, 2, 4-Trihydroxyheptadecane(4) also exhibited promising in vitro antibacterial activity against a panel of pathogenic bacteria S. areus, methicillin resistant S. areus and E. coli at IC50 values of 21.1, 8, 200 µg/mL), (3.259, 86.32 µg/mL) and (17.18, 8.26 and 200 µg/mL), respectively. The results of this study provide evidence that the fatty alcohols are a promising class of antimalarial and antimicrobial agents.

Proliferative effects of five traditional Nigerian medicinal plant extracts on human breast and bone cancer cell lines.

ETHNOPHARMACOLOGICAL RELEVANCE: The medicinal plants Hunteria umbellata (HUL), Cola lepidota (CCL), Persea americana leaf (PAL), Root bark of Persea americana (RPA) and Plukenetia conophora (PCL) are used in Nigerian traditional medicine for the treatment of cancer and cancer related diseases. AIM OF THE STUDY: To scientifically evaluate the cell proliferative and apoptotic effects of the plants extracts using breast and osteocarcinoma cell lines, and also to identify the possible components via LC-MS to have a kind of chemical fingerprint. MATERIALS AND METHODS: The antiproliferative and apoptotic effects of methanolic extracts (10 µg/ml) of the five medicinal plants were subjected to in vitro evaluation using four cancer cell lines (breast-MCF-7 and BT-20; Osteocarcinoma-MG-63 and Saos-2) measured by flow cytometry. Non-tumorigenic controls MCF-12A and primary isolated osteoblasts (POB) were chosen to eliminate negative influence on healthy tissue. RESULTS: Of the five extracts RPA demonstrated a significant (P<0.05) anti-proliferative activity against estrogen receptor positive breast cancer cell lines (MCF-7). The proliferative phase was decreased by 18%, whereas, a significant increase in cell proliferation (about 27%) was observed for RPA at a concentration of 10 µg/ml. PCL, CCL, HUL and PAL did not show marked inhibition of the proliferation of cell line MCF-7. CONCLUSION: These results give suggestive evidence that the plant extracts exhibit some correlation between the claimed ethnomedicinal uses and the cell proliferative activity. RPA extract includes chemical compounds with estrogen-like activity and validates its potential use as anticancer agent, particularly against breast carcinoma; provided important information potentially helpful in drug designing and discovery. Further studies will involve the isolation of anti tumour compounds in RPA by LC-MS and detailed mechanism of anticancer activities.

Phytochemical components of Hunteria umbellata (K. Schum) and its effect on isolated non-pregnant rat uterus in oestrus.

Hunteria umbellate plant is used by West African traditional midwives as phytomedicine in herbal remedies to treat pregnancy related ailment and most especially to augment or induce labour in gravid uterus. The purpose of this study was to investigate this claim with view to validating scientifically the ethno - medicinal usage. The phytochemical analysis of the crude medicinal plant extract revealed the presence of saponin, saponin glycosides, steroid, tannins, volatile oils, phenols and copious amount of alkaloids. The aqueous extract obtained by maceration technique was subjected to pharmacological testing in vitro on a piece of isolated rat uterus previously pretreated with stilbesterol, suspended in De Jalon at 37 degrees C and aerated with 95% Oxygen and 5% CO(2). The oxytocic activity of the aqueous pulp extract of the pulp of Hunteria umbellata was compared with uterine stimulant like oxytocin. The extract affected the contractility of the uterus significantly (P<0.05) in a dose dependent manner. The effect of 10mg/ml extract was blocked by 0.1 ml of 0.1mg/ml atropine. The extract also potentiated the response shown by various doses of oxytocin. This preliminary investigation revealed that Hunteria umbellata has oxytocic effect thus justifying the use by the traditional birth attendants.

Phytochemical and active column fractions of Pyrenacantha staudtii leaf extracts on isolated rat uterus.

Four methanolic leaf fraction extracts of Pyrenacantha staudtii obtained from accelerated gradient chromatography (AGC) were tested on the isolated rat uterus. Various fractions--M1, M2, M3 and M4 through bioassay guided isolation were obtained. Fractions M(2) and M(4), containing saponins and alkaloids respectively, significantly (P<0.05) exerted high smooth muscle relaxant activity on the uterus. Fractions M(1) and M(3) containing fatty acids and tannins respectively did not exhibit significant effect on the isolated rat uterus. The results indicate the presence of active principles in the leaf extracts of P. staudtii which may be responsible for some of the applications in traditional medicines as remedy against threatened abortion and dysmenorrheal.