Abubakar Babando Aliyu

Anti-trypanosomal activity of African medicinal plants: A review update

ETHNOPHARMACOLOGICAL RELEVANCE African trypanosomiasis is one of the neglected tropical diseases caused by different species of trypanosomes that affect both human and livestock with devastating consequences in the continent. Most of the affected populations commonly use traditional medicinal plants for the treatment of the disease. Consequently, this prompted ethnopharmacological research activities on the anti-trypanosomal activity of a number of these African medicinal plants in order to validate their ethnomedicinal use. Furthermore, such studies could lead to the identification of chemical leads for the development of newer anti-trypanosomal agents from those plants. This review aims to provide updated information on the ethnopharmacological evidence of African medicinal plants with anti-trypanosomal activity. METHODS Literature was collected via electronic search (PubMed, Sciencedirect, Medline and Google Scholar) from published articles that report on the in vitro or in vivo anti-trypanosomal activity of plants that were collected from different parts of Africa. RESULTS African medicinal plants investigated for in vitro and in vivo anti-trypanosomal activity from January 1993 to October 2013 are systematically compiled and all the in vivo studies are critically discussed. A total of 264 plant species belonging to 79 families were investigated for anti-trypanosomal activity. However, only 48 bioactive anti-trypanosomal compounds were successfully isolated in pure forms. Furthermore, some of the plants were investigated for possible ameliorative effects on the trypanosome-induced pathological changes out of which 18 plants were reported to be effective while a few others were not. In spite of interesting preclinical ethnopharmacological evidence for anti-trypanosomal activity, not a single African medicinal plant was investigated in a clinical study. CONCLUSION Several African medicinal plants have demonstrated promising anti-trypanosomal effects but the studies on the anti-trypanosomal potentials of these plants are not taken beyond proof of concept stage. It is hoped that the article would stimulate future clinical studies because of the paucity of knowledge in this area.

Senna occidentalis leaf extract possesses antitrypanosomal activity and ameliorates the trypanosome-induced anemia and organ damage.

The in vitro and in vivo antitrypanosomal effects of the ethanol extract of Senna occidentalis leaf were investigated. The crude extract exhibited an in vitro activity against Trypanosoma brucei brucei as it completely eliminated parasites’ motility within 10 minutes postincubation with 6.66 mg/ml of effective extract concentration. The extract was further used to treat experimentally T. brucei brucei infected rats at concentrations of 100 and 200 mg/kg body weight, beginning on day 5 post infections (p.i.). At the termination of the experiment on Day 11 p.i., the extract significantly (P < 0.05) kept the parasitemia lower than was recorded in the infected untreated rats. All the infected animals developed anemia, the severity of which was significantly (P < 0.05) ameliorated by the extract treatment. The infection caused significant (P < 0.05) increases in serum alanine and aspartate aminotransferases as well as serum urea and creatinine levels. However, treatment of infected animals with the extract significantly (P < 0.05) prevented the trypanosome-induced increase in these biochemical indices. Furthermore, the T. brucei infection caused hepatomegaly and splenomegaly that were significantly (P < 0.05) ameliorated by the extract administration. It was concluded that orally administered ethanol extract of S. occidentalis leaf possessed anti-T. brucei brucei activity and could ameliorate the disease-induced anemia and organ damage.

Phenolics-rich fraction of Khaya senegalensis stem bark: Antitrypanosomal activity and amelioration of some parasite-induced pathological changes

Abstract Context: The stem bark of Khaya senegalensis A. Juss (Meliaceae) is currently used for the treatment of trypanosomiasis by traditional practitioners in Nigeria. Objectives: The present study investigated the anti-Trypanosoma brucei brucei activity of phenolics-rich fraction of K. senegalensis (pfks) and its ameliorative effects on trypanosome-induced pathological changes. Materials and methods: The fraction was initially analyzed by gas chromatography-mass spectrometry (GC-MS). A 60 min time course experiment was conducted with various concentrations of the fraction using a 96-well microtiter plate technique and was further used to treat T. brucei infected rats at 100, 200 and 300 mg/kg body weight (BW). Indices of anemia as well as hepatic and renal functions were analyzed in all experimental animals at the end of the experiment. Results: The GC-MS analysis of the pfks revealed that the most abundant phytochemicals are phloroglucinol (40.56%) and 3,4-(dihydroxyphenyl) acetic acid (41.76%). The fraction showed a concentration dependent in vitro antitrypanosomal activity. Interestingly, the fraction completely eliminated the parasites from the bloodstream of infected rats without relapse during the experimental period at the dose of 300 mg/kg BW and also kept the parasites consistently lower at 100 and 200 mg/kg BW than that was recorded in the untreated infected rats. Furthermore, the severity of T. brucei-induced anemia and hepatic damage was significantly (p < 0.05) ameliorated in the 300 mg/kg BW treatment group whereas the parasite-induced renal damage was significantly (p < 0.05) ameliorated in all treatment groups. Conclusion: Data from this study may suggest that phenolics play an important role in the antitrypanosomal activity of K. senegalensis.

A systematic review of pentacyclic triterpenes and their derivatives as chemotherapeutic agents against tropical parasitic diseases.

Parasitic infections are among the leading global public health problems with very high economic and mortality burdens. Unfortunately, the available treatment drugs are beset with side effects and continuous parasite drug resistance is being reported. However, new findings reveal more promising compounds especially of plant origin. Among the promising leads are the pentacyclic triterpenes (PTs) made up of the oleanane, ursane, taraxastane, lupane and hopane types. This paper reviews the literature published from 1985 to date on the in vitro and in vivo anti-parasitic potency of this class of phytochemicals. Of the 191 natural and synthetic PT reported, 85 have shown high anti-parasitic activity against various species belonging to the genera of Plasmodium, Leishmania, Trypanosoma, as well as various genera of Nematoda. Moreover, structural modification especially at carbon 3 (C3) and C27 of the parent backbone of PT has led to improved anti-parasitic activity in some cases and loss of activity in others. The potential of this group of compounds as future alternatives in the treatment of parasitic diseases is discussed. It is hoped that the information presented herein will contribute to the full exploration of this promising group of compounds as possible drugs for parasitic diseases.

Saponins-rich fraction of Calotropis procera leaves elicit no antitrypanosomal activity in a rat model

OBJECTIVE To examine the in vitro and in vivo anti-Trypanosoma evansi (T. evansi ) activity of saponins-rich fraction of Calotropis procera (cpsf) leaves as well as the effect of the fraction on the parasite-induced anemia. METHODS A 60-minutes time course experiment was conducted with various concentrations of the fraction using a 96-well microtiter plate technique, and subsequently used to treat experimentally T. evansi infected rats at 100 and 200 mg/kg body weight. Index of anemia was analyzed in all animals during the experiment. RESULTS The cpsf did not demonstrate an in vitro antitrypanosomal activity. Further, the cpsf treatments did not significantly (P>0.05) keep the parasites lower than the infected untreated groups. At the end of the experiment, all T. evansi infected rats developed anemia whose severity was not significantly (P>0.05) ameliorated by the cpsf treatment. CONCLUSIONS It was concluded that saponins derived from Calotropis procera leaves could not elicit in vitro and in vivo activities against T. evansi.

Chemical composition and antimicrobial activity of hexane leaf extract of Anisopus mannii (Asclepiadaceae).

Objective: The aim was to determine the chemical constituents and antimicrobial activity of the hexane leaf extract of Anisopus mannii against a wide range of human pathogenic microorganisms. Methods: The chemical constituents of the hexane leaf extract was determined using gas chromatography-mass spectrometry (GC-MS) analysis; and the antimicrobial activity was evaluated on “standard strains”, clinical susceptible and resistant bacterial and fungal isolates using the disc diffusion and broth microdilution methods. Results: GC-MS analysis of the hexane leaf extract revealed 32 compounds, representing 73.8% of the identified components. The major compounds were hexadecanoic acid, ethyl ester (34%), oxirane, hexadecyl- (11%) and 9, 12, 15-octadecatrienoic acid, ethyl ester, (Z, Z, Z) (9.6%). Results from the antimicrobial activity demonstrated higher inhibition zones against Bacillus cereus (29 mm), followed by Streptococcus pyogenes (28 mm). Other notable inhibitions were observed with Enterococcus faecalis (27 mm), Proteus vulgaris (26 mm) and MRSA (25 mm). The MIC values ranged from 0.625 mg/mL to 1.25 mg/mL while the MBC/MFC values ranged from 2.5 mg/mL to 5.0 mg/mL. Conclusion: These results support the traditional use of the plant and demonstrate the huge potential of A. mannii as a source of antimicrobial compounds.

Effects of α-tocopherol on the in vivo antitrypanosomal effects of phenolics-rich fraction of Khaya senegalensis stem bark

Abstract Objective To investigate the effects of combined administration of a low dose of a phenolics-rich fraction of Khaya senegalensis (PFKS) stem bark with α-tocopherol on Trypanosoma brucei brucei (T. brucei brucei) infection. Methods Rats were divided into five groups of six animals, namely, normal control, uninfected but treated with PFKS and α-tocopherol, infected control, infected and treated with PFKS and α-tocopherol (ITTF) and infected treated with diminazine aceturate. Rats in infected control, ITTF and infected treated with diminazine aceturate were infected with T. brucei brucei while the animals in uninfected but treated with PFKS and α-tocopherol and ITTF were treated with a combination of PFKS (100 mg/kg body weight) and α-tocopherol (100 mg/kg body weight) for 8 days. At the end of the experiment, indices of anemia as well as hepatic and renal functions were analysed. Results The combined treatment significantly (P Conclusions Combination of a low dose of PFKS stem bark and α-tocopherol could be a therapeutically active regimen against animal trypanosomiasis.

A new Antimicrobial Prenylated Benzo-lactone from the Rhizome of Cissus cornifolia

Background: Medicinal plants remain one of the largest reservoirs of new bioactive compounds. In this study, a new prenylated benzo-lactone (4, 6-dihydroxy-5-methoxy-3-(1, 2, 3, 4, 5-pentahydroxypentyl)-2-benzofuran-1(3H)-one) was isolated from the acetone extracts of the rhizome of Cissus cornifolia. The antimicrobial activity of the compound was evaluated against some microorganisms including Staphylococcus aureus, Salmonella typhi, and Candida albicans. Materials and Methods: The acetone extracts of the rhizome of C. cornifolia was separated and purified by various chromatographic techniques. The structure of the isolated compound was characterized by analysis of spectral data including one and two-dimensional nuclear magnetic resonance. Results: The isolated compound was characterized as (4, 6-dihydroxy-5-methoxy-3-(1, 2, 3, 4, 5-pentahydroxypentyl)-2-benzofuran-1(3H)-one), it showed activity against 6 out of 10 tested clinical isolates of some microorganisms including S. aureus, S. typhi, and C. albicans. The inhibition zones ranged between 17 mm and 25 mm. The inhibition zones observed compare favorably with the positive control used. Conclusion: The compound could serve as a lead for the development of more potent antimicrobial agent. To the best of our knowledge, this is the first report of the isolation and characterization as well as antimicrobial screening of the compound.