Medicinal Chemistry

Camel trypanosomiasis is a major disease of economic importance in Ethiopian Somali Regional State, Ethiopia. Local people use the leaves of Crotalaria albicaulis and Cistanche phelypaea to treat this disease and complement the absence or the limitations of existing anti-trypanosomal chemotherapeutic agents. Thus, the aim of this study was to evaluate the in vivo and in vitro anti-trypanosomal activity of the methanolic crude extracts of leaves of Crotalaria albicaulis and Cistanche phelypaea against Trypanosoma evansi isolate. The fresh leaves of both plants were extracted by percolation technique using methanol. For the in vivo assay, mice infected with T. evansi were administered intraperitoneally daily for 7 days with crude extracts at doses of 100, 200 and 400 mg/ kg body weight. In vitro trypanocidal activity of these extracts was tested in triplicate in 96 well micro titer plates. Diminazene aceturate and dimethyl sulfoxide were used as positive and negative controls, respectively. At 4.0 mg/ ml concentration the methanolic crude extract of C. albicaulis completely ceased motility of the parasite after 40 minutes. The plant also significantly (p<0.05) prolonged infection period in vitro infectivity test. Moreover, at 400 mg/kg dose, the crude extracts of both plants exhibited a mild in vivo anti-trypanosomial activity against T. evansi. This study established that leaves of C. albicaulis has a mild in vivo and in vitro anti-trypanosomal activity and can be considered as a potential source of new drugs for the treatment of Camel trypanosomiasis.

Over the past decade, there has been a rising interest in the use of carboranes as a potential pharmacophoric moiety in the development of new drugs for the treatment of various types of cancer. The unique physical and chemical properties of carboranes make their use attractive in drug development. In several instances, the inclusion of carboranes into a drug structure has increased the agent’s binding affinity, potency, or bioavailability. The purpose of this review is to highlight applications of carboranes to the medicinal chemistry of cancer.

The aim of this research was to determine antibacterial activity and phyto-chemical screening of ethanolic extracts of Zingiber officinale. Fresh rhizomes of Zingiber officinale (Ginger) were collected from Kachia Local Government Area, Kaduna (Kaduna south) state, Nigeria. The antibacterial activity was determined using agar well diffusion method whereas phytochemical screening was carried out to determine the phytochemical composition of the ginger rhizomes. The result of the Phytochemical screening revealed absence of alkaloids and saponins in all the extracts but showed presence of flavonoids, tannins and steroids. The result for the bioassay presented variation in the biological activity of the extracts. All the extracts exhibited antibacterial activity against all the tested bacteria with zones of inhibition diameter ranging from 7.31-18.67 mm. The highest zone was observed in chloroform extracts on Staphylococcus epidermidis at 100 mg/ml while the least zone of inhibition was observed in n-hexane extracts on Pseudomonas aeruginosa at 25 mg/ml. However, both Klebsiella pneumoniae and Pseudomonas aeruginosa were resistant to n-hexane extracts at 25 mg/ml.