New Series of Imidazoles Showed Promising Growth Inhibitory and Curative Potential Against Trypanosoma Infection.

The Trypanosoma spp. cause animal and human trypanosomiasis characterized with appreciable health and economic burden mostly in developing nations. There is currently no effective therapy for this parasitic disease, due to poor drug efficacy, drug resistance, and unwanted toxicity, etc. Therefore, new anti-Trypanosoma agents are urgently needed. This study explored new series of imidazoles for anti-Trypanosoma properties in vitro and in vivo. The imidazoles showed moderate to strong and specific action against growth of T. congolense. For example, the efficacy of the imidazole compounds to restrict Trypanosoma growth in vitro was ≥ 12-fold specific towards T. congolense relative to the mammalian cells. Additionally, the in vivo study revealed that the imidazoles exhibited promising anti-Trypanosoma efficacy corroborating the in vitro anti-parasite capacity. In particular, three imidazole compounds (C1, C6, and C8) not only cleared the systemic parasite burden but cured infected rats after no death was recorded. On the other hand, the remaining five imidazole compounds (C2, C3, C4, C5, and C7) drastically reduced the systemic parasite load while extending survival time of the infected rats by 14 days as compared with control. Untreated control died 3 days post-infection, while the rats treated with diminazene aceturate were cured comparable to the results obtained for C1, C6, and C8. In conclusion, this is the first study demonstrating the potential of these new series of imidazoles to clear the systemic parasite burden in infected rats. Furthermore, a high selectivity index of imidazoles towards T. congolensein vitro and the oral LD50 in rats support anti-parasite specific action. Together, findings support the anti-parasitic prospects of the new series of imidazole derivatives.

Drug leads agents from methanol extract of Nigerian bee (Apis mellifera) propolis.

BACKGROUND: Propolis is a bee (Apis mellifera) product of plant origin with varied chemical composition depending on the ecology of the botanical origin. It has been reported in literature to possess various therapeutic effects both traditionally, clinical trial, and animal study. OBJECTIVES: In the present study bioactive principle in methanol extract of Nigerian bee (A. mellifera) propolis was determined by gas chromatography-mass spectrometry (GC/MS) study. MATERIALS AND METHODS: The methanol extract of Nigerian bee (A. mellifera) propolis was characterized for its chemical composition by preliminary phytochemicals screening and GC/MS analysis using standard procedures and methods. RESULTS: Phytochemical screening revealed the presence of flavonoids, saponins, alkaloids, tannins, cardiac glycosides, anthraquinones phlobatannins, and steroids while GC/MS chromatogram revealed nineteen peaks representing 60 different chemical compounds. The first compounds identified with less retention time (RT) (13.33s) were methyl tetradecanoate, tridecanoic acid, methyl ester, decanoic acid, methyl ester while squalene, all-trans-squalene, 2,6,10-dodecatrien-1-ol, 3,7,11-trimethyl-, (E,E)- and farnesol isomer a took longest RT (23.647s) to identify. Methyl 14-methylpentadecanoate, hexadecanoic acid methyl ester, methyl isoheptadecanoate, and methyl tridecanoate were the most concentrated constituent as revealed by there peak height (26.01%) while eicosanoic acid was the least concentrated (peak height 0.81%) constituent of Nigerian bee propolis. CONCLUSION: The presence of these chemical principles is an indication that methanol extract of Nigeria bee propolis, if properly screened could yield a drug of pharmaceutical importance.

Potential antimalarials from African natural products: A reviw.

Malaria remains an overwhelming infectious disease with significant health challenges in African and other endemic countries globally. Resistance to antimalarial drugs has become one of the most momentous challenges to human health, and thus has necessitated the hunt for new and effective drugs. Consequently, few decades have witnessed a surfeit of research geared to validate the effectiveness of commonly used traditionally medicines against malaria fever. The present review work focuses on documenting natural products from African whose activity has been reported in vivo or in vitro against malaria parasite. Literature was collected using electronic search of published articles (Google Scholar, PubMed, Medline, Sciencedirect, and Science domain) that report on antiplasmodial activity of natural products from differernts Africa region. A total of 652 plant taxa from 146 families, 134 isolated antimalarial compounds from 39 plants species, 2 herbal formulations and 4 insect/products were found to be reported in literature from 1996 to 2015. Plants species from family Asteraceae (11.04%), Fababceae (8.128%), Euphorbiaceae (5.52%), Rubiaceas (5.52%), and Apocyanaceae (5.214%), have received more scientific validation than others. African natural products possess remarkable healing properties as revealed in the various citations as promising antimalarial agents. Some of these natural products from Africa demonstrate high, promising or low activities against Plasmodium parasite. This study also shows that natural products from Africa have a huge amount of novel antimalarial compounds that could serve as a leads for the development of new and effective antiplasmodial drugs. However, in a view of bridging the gap in knowledge, clinical validation of these natural products are of paramount importance.