In Vitro Antiproliferative Effects and Phytochemical Characterization of Carissa edulis ((Forssk) Vahl) and Pappea capensis (Eckyl and Zeyh) Extracts.

Cancer mortality is a global concern. The current therapeutic approaches despite showing efficacy are characterized by several limitations. Search for alternatives has led to the use of herbal plants including C. edulis and P. capensis. However, there is limited research on antiproliferative effects of these medicinal plants. The study sought to evaluate antiproliferative effects of the plants against human breast and prostate cancers using cell viability, and gene expression assays to determine modulation of apoptotic genes. Further, Liquid Chromatography Mass Spectrophotometer (LC-MS) and Gas Chromatography Mass Spectrophotometer (GC-MS) analyses were performed to confirm phytocompounds in the extracts. The results indicated that ethylacetate extracts of C. edulis and P. capensis had the highest activity against cancer cells with IC50 values of 2.12 ± 0.02, and 6.57 ± 0.03 µg/ml on HCC 1395 and 2.92 ± 0.17 and 5.00 ± 0.17 µg/ml on DU145, respectively. Moreover, the plants extracts exhibited relatively less cytotoxic activities against Vero cell lines (IC50 > 20 µg/ml). The extracts also exhibit selectivity against the cancer cells (SI > 3). Further, mRNA expression of p53 in the treated HCC 1395 was increased by 7 and 3-fold, whereas by 3 and 2-fold in DU145 cells, upon treatment with ethylacetate extracts of C. edulis and P. capensis, respectively. Similarly, several-fold increases were observed in the number of transcripts of Bax in HCC 1395 and HOXB13 in DU145 cells. Phytochemical analyses detected presence of phytocompounds including flavonoids, phenolics, tocopherols and terpenoids which are associated with anticancer activity. Findings from this study provide a scientific validation for the folklore use of these plants in management of cancer.

Quantitative Phytochemical Profile and In Vitro Antioxidant Properties of Ethyl Acetate Extracts of Xerophyta spekei (Baker) and Grewia tembensis (Fresen).

Overproduction of free radicals in excess of antioxidants leads to oxidative stress which can cause harm to the body. Conventional antioxidants have drawbacks and are believed to be carcinogenic. The present study seeked to confirm folklore use and validate the antioxidant potentials of Grewia tembensis and Xerophyta spekei which have been widely used in the Mbeere community as medicinal plants. Antioxidant properties were determined through scavenging effects of diphenyl-1-picrylhydrazyl (DPPH) and hydrogen peroxide radicals as well as iron chelating effects. The data obtained was assayed in comparison to the standards (Ascorbic acid and EDTA). Ascorbic acid had a significantly greater DPPH radical scavenging property with an inhibitory concentration (IC50) value of 20.54 ± 2.24 µg/mL in comparison to the plant extracts, which had IC50 values of 33.00 ± 1.47 µg/mL, 69.66 ± 1.01 µg/mL and 86.88 ± 2.64 µg/mL for X. spekei, G. tembensis leaf and G. tembensis stem bark extracts, respectively. EDTA demonstrated a significantly greater iron chelating effect having a significantly lesser IC50 value of 25.05 ± 0.79 µg/mL as opposed to 43.56 ± 0.46 µg/mL, 89.78 ± 0.55 µg/mL, and 120.70 ± 0.71 µg/mL for X. spekei, G. tembensis leaf, and G. tembensis stem bark extracts respectively. Additionally, ascorbic acid also exhibited stronger hydrogen peroxide radical scavenging effect than the studied extracts. Generally, X. spekei extract had higher antioxidant activities as compared to both the leaf and stem bark extracts of G. tembensis. The phytochemical screening demonstrated the presence of secondary metabolites associated with antioxidant properties. The present study therefore, recommends ethno medicinal and therapeutic use of G. tembensis and X. spekei in the treatment and management of oxidative stress related infections.

GC-MS Analysis, Antibacterial and Antioxidant Potential of Ethyl Acetate Leaf Extract of Senna singueana (Delile) Grown in Kenya.

Bacterial diseases are a leading cause of mortality and morbidity globally. During bacterial diseases, an elevation of host immune response occurs, which involves the production of free radicals in response to the bacterial infection. The overproduction of free radicals in excess of the antioxidants leads to oxidative stress. Conventional antibiotics are linked to side effects such as hypersensitivity reactions in addition to bacterial pathogens developing resistance against them. Artificial antioxidants are said to be carcinogenic. This study sought to confirm folklore use and validate the antibacterial and antioxidant potential of Senna singueana which has been widely used in the Mbeere community. The in vitro antibacterial potentials of the plant extract were investigated on Bacillus subtilis ATCC 21332, Escherichia coli ATCC 25922, Salmonella typhi ATCC 1408, and Staphylococcus aureus ATCC 25923. Ciprofloxacin (100 µg/ml) drug was used as a standard reference, whereas 5% DMSO was used as a negative reference. The antibacterial tests included disc diffusion and minimum inhibitory and bactericidal concentrations. S. singueana ethyl acetate extract showed broad-spectrum potential against tested bacterial microbes producing mean zones of inhibition (MZI) from 07.67 ± 0.33 to 17.67 ± 0.33 mm. The extract demonstrated a greater effect on Gram-positive than Gram-negative bacterial pathogens. Antibacterial properties of ciprofloxacin were significantly greater in comparison to plant extract in all the dilutions (p < 0.05), while 5% DMSO was inactive against all the tested bacteria. MBC values were greater than MIC values. Antioxidant properties of the extract were determined through scavenging effects of DPPH and hydroxyl radicals (•OH) as well as ferric reducing antioxidant potential (FRAP) assay. S. singueana demonstrated effects against all radicals formed. Additionally, the extract exhibited ferric reducing abilities. The extract also contained various phytocompounds with known antibacterial and antioxidant properties. This study recommends the therapeutic use of S. singueana as an antibacterial as well as an antioxidant agent.

Coenzyme Q10 protected against arsenite and enhanced the capacity of 2,3-dimercaptosuccinic acid to ameliorate arsenite-induced toxicity in mice.

BACKGROUND: Arsenic poisoning affects millions of people. The inorganic forms of arsenic are more toxic. Treatment for arsenic poisoning relies on chelation of extracellularly circulating arsenic molecules by 2,3-dimecaptosuccinic acid (DMSA). As a pharmacological intervention, DMSA is unable to chelate arsenic molecules from intracellular spaces. The consequence is continued toxicity and cell damage in the presence of DMSA. A two-pronged approach that removes extracellular arsenic, while protecting from the intracellular arsenic would provide a better pharmacotherapeutic outcome. In this study, Coenzyme Q10 (CoQ10), which has been shown to protect from intracellular organic arsenic, was administered separately or with DMSA; following oral exposure to sodium meta-arsenite (NaAsO2) - a very toxic trivalent form of inorganic arsenic. The aim was to determine if CoQ10 alone or when co-administered with DMSA would nullify arsenite-induced toxicity in mice. METHODS: Group one represented the control; the second group was treated with NaAsO2 (15 mg/kg) daily for 30 days, the third, fourth and fifth groups of mice were given NaAsO2 and treated with 200 mg/kg CoQ10 (30 days) and 50 mg/kg DMSA (5 days) either alone or in combination. RESULTS: Administration of CoQ10 and DMSA resulted in protection from arsenic-induced suppression of RBCs, haematocrit and hemoglobin levels. CoQ10 and DMSA protected from arsenic-induced alteration of WBCs, basophils, neutrophils, monocytes, eosinophils and platelets. Arsenite-induced dyslipidemia was nullified by administration of CoQ10 alone or in combination with DMSA. Arsenite induced a drastic depletion of the liver and brain GSH; that was significantly blocked by CoQ10 and DMSA alone or in combination. Exposure to arsenite resulted in significant elevation of liver and kidney damage markers. The histological analysis of respective organs confirmed arsenic-induced organ damage, which was ameliorated by CoQ10 alone or when co-administered with DMSA. When administered alone, DMSA did not prevent arsenic-driven tissue damage. CONCLUSIONS: Findings from this study demonstrate that CoQ10 and DMSA separately or in a combination, significantly protect against arsenic-driven toxicity in mice. It is evident that with further pre-clinical and clinical studies, an adjunct therapy that incorporates CoQ10 alongside DMSA may find applications in nullifying arsenic-driven toxicity.

In Vitro Antioxidant Activities of Methanolic Extracts of Caesalpinia volkensii Harms., Vernonia lasiopus O. Hoffm., and Acacia hockii De Wild.

Oxidative stress is the result of the disparity between pro-oxidants and antioxidants in an organism, and it is important in the pathogenesis of several degenerative disorders, such as arthritis, Alzheimer's, cancer, and cardiovascular diseases. Free radicals can damage biomolecules, such as nucleic acids, lipids, proteins, polyunsaturated fatty acids, and carbohydrates, and the DNA leading to mutations. The use of antioxidants is effective in delaying the oxidation of biomolecules. Antioxidants are complexes found in the food that can retard or deter oxidation by preventing the initiation and propagation of oxidizing chain reactions. Medicinal plants have been used for centuries by man to manage diseases and have a host of antioxidant complexes. Traditionally, Caesalpinia volkensii, Vernonia lasiopus, and Acacia hockii have folkloric remedies against associated oxidative stress-mediated complications. However, the upsurge in its use has not been accompanied by scientific validations to support these claims. In this study, in vitro antioxidant activity of Caesalpinia volkensii, Vernonia lasiopus, and Acacia hockii collected from Embu County (Kenya) were determined by radical scavenging activities of 1,1-diphenyl-2-picrylhydrazyl (DPPH) and hydroxyl radical in addition to ferric reducing antioxidant power analyzed against that of L-ascorbic acid as the standard. The obtained results revealed remarkable antioxidant activities of the studied plant extracts as evidenced by the low IC50 and EC50 values. These antioxidant activities could be due to the presence of antioxidants phytochemicals such as flavonoids, phenols, terpenoids, and saponins among others. Therefore, the therapeutic potential of this plant could be due to their antioxidant properties. This study recommends bioassay of the extracts against oxidative stress-related disorders for development of phytomedicine with antioxidant properties.

In Vivo Cognitive-Enhancing, Ex Vivo Malondialdehyde-Lowering Activities and Phytochemical Profiles of Aqueous and Methanolic Stem Bark Extracts of Piliostigma thonningii (Schum.).

Cognitive impairment (CI) is among the leading causes of disability in humans. It is estimated that over 35.6 million people are suffering from Alzheimer's disease- (AD-) associated cognitive deficits globally with these statistics projected to rise over 115.4 million by the year 2050. There is no specific etiology for this cognitive impairment; however, various contributing factors including advancing age (>60 years old), oxidative stress, cerebral injuries, infections, neurologic disorders, and cancer have been implicated. Despite various attempts to manage CI, no curative medicines are yet available. The current drugs used to manage symptoms of AD-associated CI including Donepezil and Rivastigmine among others are only palliative rather than therapeutic. Furthermore, these agents have been associated with undesirable side effects. This calls for alternative and complementary approaches aimed at either preventing or reverting AD-related CI in a curative way without causing adverse events. It is estimated that over 80% of the world's population utilize herbal medicines for basic healthcare as it is considered safe, affordable, and easily accessible as opposed to conventional healthcare. Various parts of P. thonningii are used in traditional medicine to manage various conditions including CI. However, empirical and scientific data to validate these uses is lacking. In this study, the Morris water maze (MWM) experiment was adopted to evaluate the cognitive-enhancing effects of the studied plant extracts. The malondialdehyde (MDA) profiles in the brains of experimental mice were determined using the thiobarbituric acid reactive substances (TBARS) test. Moreover, qualitative phytochemical profiling of the studied plant extracts was performed using standard procedures. The results showed remarkable cognitive-enhancing activities which were reflected in significantly shorter transfer latencies, navigation distances, longer time spent in platform quadrant, and lower MDA levels compared with those recorded for the negative control mice (p < 0.05). Phytochemical screening of the studied plant extracts revealed the presence of antioxidant phytocompounds, which may have played key roles in the extracts' potency. Based on the findings herein, P. thonningii extracts, especially the aqueous ones have a promising potential for the management of AD-associated CI. Further studies aimed at isolating and characterizing specific active compounds for CI from P. thonningii are recommended. Additionally, specific mode(s) of action of active principles should be elucidated. Moreover, toxicity studies should be done on the studied plant extracts to ascertain their safety.