ObjectiveTo evaluate the antimicrobial and toxicological effects of aqueous garlic (Allium sativum) bulbs extract in wister rat using biochemical and hematological parameters.MethodsA total of 20 wister rats were assigned into four (A–D) groups of five animals each. Group A served as the control and was administered 1 mL of distilled water. Groups B–C were given 300, 600 and 1200 mg/kg body weight of garlic (Allium sativum) bulbs extract for 5 weeks.ResultsGarlic bulbs extract produced significant inhibitory activities against all bacteria tested at concentrations of 120 and 160 mg/mL. However, at concentration of 80 mg/mL, the extract had no inhibitory activities against Klebsiella pneumoniae and Salmonella typhi. The minimal inhibitory concentration and minimal bactericidal concentration ranged between 80–120 mg/mL and 120–160 mg/mL respectively. Toxicological study revealed that the extract did not cause any significant (P > 0.05) alteration to serum aspartate transaminase, alkaline phosphatase activities, total bilirubins, Na, K, creatinine, red blood cell, hematocrit, hemoglobin, mean corpuscular hemoglobin concentration, granulocyte and organs-body weight ratio. However, serum alanine transaminase activities, total proteins, direct bilirubins, Cl− concentrations and body weight gain were significantly (P < 0.05) lowered while the concentrations of urea, albumin, white blood cell, mean corpuscular hemoglobin and mean corpuscular volume count were raised significantly (P < 0.05) in rats dosed with 600 and 1200 mg/kg of the extract. However, at a dose of 300 mg/kg only, the concentrations of Cl−, urea and albumin were mildly altered.ConclusionsThe extract caused selective changes in some biochemical parameters of organ function; however, since only mild alteration was observed at a dose of 300 mg/kg, the garlic bulb may be considered to be relatively safe and could be explored as an oral remedy at this dose

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.

The potential pharmaceutical application of nanoparticles has led to the toxicity within the male reproductive system. In the present study, the effects of silver nanoparticles (Ag-NPs) on hematological parameters, free radical generation, antioxidant system, sperm parameters, and organ histo-morphometry in male rats were investigated. Ag-NPs were produced by the reduction of silver ions, while the formation of which was monitored by UV–visible spectrophotometry. Zeta potential, transmission, and scanning electron microscopies were applied for the characterization of AgNPs. A total of 30 rats were divided into 6 groups and were sub-dermally exposed to Ag-NPs at the dosage of 0 (control), 10, and 50 mg/kg bodyweight (bw) doses for either 7 or 28 days. Ag-NP administration altered hematological indices and caused dose-dependent decreases in sperm motility, velocity, kinematic parameters, concentrations of luteinizing hormone, follicle-stimulating hormone, and testosterone. In the epididymis and testis, the concentrations of malondialdehyde and peroxide increases while superoxide dismutase, catalase, reduced glutathione, and total thiol group decreases. These findings suggest that Ag-NP triggered hormonal imbalance and induce oxidative stress in testis and epididymis; which negatively affect sperm parameters of male rats.

Free radicals are highly reactive molecules generated during oxidation reactions which in turn initiate chain reactions resulting to cellular damage. There is substantial evidence implicating free radicals especially reactive oxygen species (ROS) in the etiology of more than one hundred degenerative disorders in humans including, arthritis, atherosclerosis, ischemia and reperfusion injury of many tissues, gastritis, diabetics, central nervous system injury, acquired immunodeficiency syndrome (AIDS) and cancer. Scientific evidence postulates that bioactive compounds especially from natural products are capable of providing protection against free radicals. Consequently, few decades have witnessed a surfeit of research geared towards validating the antioxidant and hepatoprotective potential of the natural products. In this review, African natural products whose antioxidants activities were scientifically validated either in their crude extracts and/or derived products have been discussed. A total 1076 plants species representing 287 family, 132 isolated compounds and 7 insect/mollusk secreation were found. The plant species from the following families; Fababceae, Asteraceae, Lamiaceae, Moraceae, Euphorbiaceae, Combretaceae and Malvaceae have received more scientific attention than others. Analysis of the reports revealed that Combretum apiculatum, Telfaria occidentalis, Acalypha racemosa, Garcinia lucida were the most active plant extracts from African flora. The most active ROS-detoxifying phytochemicals were moracin T, U, S and R (84–87), oleanolic acid (54), 5,7,4′–trihydroxy–3,8,3′,5′–tetramethoxyflavone (89), 5,7,3′–trihydroxy-3,8,4′,5′–trimethoxyflavone (88), luteolin (3′,4′,5,7–tetrahydroxy flavone) (117) and genistein (4′,5,7–trihydroxyisoflavone) (116). The significant antioxidant potential demonstrated by some crude extracts and their constituent compounds render them good candidates for the development of new drugs. Although, the study of the mechanisms of actions as well as clinical validation of some of these isolated compounds is lacking. It is hoped that pertinent scientist and stakeholders will look further into some of these compounds for detailed authentification and subsequent commercialization.

The present study examined the protective effects of curcuminoid isolates from Curcuma longa against carbon tetrachloride (CCL₄)-induced hepatic injury in rats. The hepatoprotective effect of the crude extract (150, 300 and 600 mg/kg bw) and curcuminoids (75, 150 and 300 mg bw) was evident by significant increases in the serum antioxidative defence capacities (super oxide dismutase, reduced glutathione, catalase) and reduction in biomarker enzymes of liver integrity (aspartate transaminase, alanine transaminase and alkaline phosphatase) in comparison to the results obtained in the CCL₄-untreated animals. Some of these parameters were completely restored by pre-treatments with curcuminoids. Similarly, the curcuminoids increases the concentrations of total proteins, albumins and ameliorated histological changes observed in CCL₄ injured rats. Therefore, curcuminoid could be considered a novel candidate for the development of new drug against liver diseases.

Signal transducer and activator of transcription 3 (STAT3) is a transcriptional regulator of a number of biological processes including cell differentiation, proliferation, survival, and angiogenesis, while cyclin-dependent kinases (CDKs) are a critical regulator of cell cycle progression. These proteins appear to play central roles in angiogenesis and cell survival and are widely implicated in tumor progression. In this study, we used the well-characterized US National Cancer Institute 60 (NCI60) human tumor cell lines to screen the in vitro anti-cancer activities of our novel small molecule derivatives (NSC765690 and NSC765599) of salicylanilide. Furthermore, we used the DTP-COMPARE algorithm and in silico drug target prediction to identify the potential molecular targets, and finally, we used molecular docking to assess the interaction between the compounds and prominent potential targets. We found that NSC765690 and NSC765599 exhibited an anti-proliferative effect against the 60 panels of NCI human cancer cell lines, and dose-dependent cytotoxic preference for NSCLC, melanoma, renal, and breast cancer cell lines. Protein–ligand interactions studies revealed that NSC765690 and NSC765599 were favored ligands for STAT3/CDK2/4/6. Moreover, cyclization of the salicylanilide core scaffold of NSC765690 mediated its higher anti-cancer activities and had greater potential to interact with STAT3/CDK2/4/6 than did NSC765599 with an open-ring structure. NSC765690 and NSC765599 met the required safety and criteria of a good drug candidate, and are thus worthy of further in-vitro and in-vivo investigations in tumor-bearing mice to assess their full therapeutic efficacy.