In South Africa, the number of people suffering from diabetes is believed to be rising steadily and the current antidiabetic therapies are frequently reported to have adverse side effects. Ethnomedicinal plant use has shown promise for the development of cheaper, cost‐effective antidiabetic agents with fewer side effects. The aim of this study was to investigate the antidiabetic activity and mechanism of action of aqueous leaf extract prepared from Brachylaena elliptica. The potential of the extract for cytotoxicity was evaluated using MTT assay in HepG2 cells. The effects of the plant extract on glucose utilization in HepG2 cells and L6 myotubes, triglyceride accumulation in 3T3‐L1, INS‐1 proliferation, glucose metabolism in INS‐1 cells, and NO production in RAW macrophages were also investigated using cell culture procedures. The inhibitory effects of the extract on the activities of different enzymes including alpha‐amylase, alpha‐glucosidase, pancreatic lipase, dipeptidyl peptidase IV (DPP‐IV), collagenase, and CYP3A4 enzymes were evaluated. The extract also tested against protein glycation using standard published procedure. The plant extract displayed low level of toxicity, where both concentrations tested did not induce 50% cell death. The extract caused a significant increase in glucose uptake in HepG2 liver cells, with efficacy significantly higher than the positive control, berberine. The crude extract also displayed no significant effect on muscle glucose uptake, triglyceride accumulation in 3T3‐L1, glucose metabolism in INS‐1 cells, alpha‐amylase, alpha‐glucosidase, DPP‐IV, lipase, protein glycation, and collagenase compared to the respective positive controls. The extract displayed a proliferative effect on INS‐1 cells at 25 μg/ml when compared to the negative control. The plant also produced a concentration‐dependent reduction in NO production in RAW macrophages and also demonstrated weak significant inhibition on CYP3A4 activity. The findings provide evidence that B. elliptica possess antidiabetic activity and appear to exact its hypoglycemic effect independent of insulin.

Background: Carpobrotus edulis (Mesembryanthemaceae), also known as igcukuma in Xhosa language is a medicinal plant used by the traditional healers to treat common infections in HIV/AIDS patients. Based on this information, we researched on the plant phytoconstituents, as well as its inhibitory effect using aqueous and three different organic solvent extracts in order to justify its therapeutic usage. Methods: Antioxidant activity of the extracts were investigated spectrophotometrically against 1,1- diphenyl-2-picrylhydrazyl (DPPH), 2,2’-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) diammonium salt, hydrogen peroxide (H₂O₂), nitric oxide (NO), and ferric reducing power, Total phenols, flavonoids, flavonols, proanthocyanidins, tannins, alkaloids and saponins were also determined using the standard methods. Results: Quantitative phytochemical analysis of the four solvent extracts revealed a high percentage of phenolics (55.7 ± 0.404%) in the acetone extract, with appreciable amount of proanthocyanidins (86.9 ± 0.005%) and alkaloids (4.5 ± 0.057%) in the aqueous extract, while tannin (48.9 ± 0.28%) and saponin (4.5 ± 0.262%) were major constituents of the ethanol extract. Flavonoids (0.12 ± 0.05%) and flavonols (0.12 ± 0.05%) were found at higher level in the hexane extract in comparison with the other extracts. The leaf extracts demonstrated strong hydrogen peroxide scavenging activity, with the exception of water and ethanol extracts. IC₅₀ values of the aqueous and ethanolic extract against DPPH, ABTS, and NO were 0.018 and 0.016; 0.020 and 0.022; 0.05 and 0.023 mg/ml, respectively. The reducing power of the extract was found to be concentration dependent. Conclusion: The inhibitory effect of the extracts on free radicals may justify the traditional use of this plant in the management of common diseases in HIV/AIDs patients in Eastern Cape Province. Overall, both aqueous and ethanol were found to be the best solvents for antioxidant activity in C. edulis leaves.

The Opuntia spp. have been used in traditional medicine for many centuries. It is used in the management of diseases that involves oxidative stress, especially diabetes, obesity and cancer. Opuntia stricta (Haw) is one of the relatively unknown species in South Africa where it is regarded more as a weed. Because of this, not much is known about its chemical composition. To determine the chemical composition, antioxidant, anti-inflammatory, and cytotoxic activities of Opuntia stricta cladodes. The phytochemical composition of acetone, aqueous and ethanol extract of cladodes of Opuntia stricta (Haw), as well as the vitamins A, C and E of its dried weight cladodes and the antioxidant activities, were evaluated using standard in vitro methods. The anti-inflammatory and cytotoxic activities were evaluated using cell-based assays. The phytochemical composition and vitamins were determined spectrophotometrically, while the antioxidant activities were determined by DPPH, nitric oxide, hydrogen peroxide scavenging activity and phosphomolybdenum (total) antioxidant activity. Anti-inflammatory activity was determined using RAW 264.7 cells, while cytotoxicity was determined using U937 cells. The phytochemical composition showed a significant difference in the various extracts. The total phenolics were higher than other phytochemicals in all the extracts used. All the extracts displayed antioxidant activity, while most of the extracts showed anti-inflammatory activity. Only one extract showed cytotoxicity, and it was mild. The results show that the Opuntia stricta is rich in polyphenolic compounds and has good antioxidant activity as well as anti-inflammatory activities.

The use of medicinal plants for the management of diabetes mellitus is on the rise in the developing countries, including South Africa. There is increasing scientific evidence that supports the claims by the traditional healers. In this review, we compare the families of previously reported anti-diabetic plants in the Eastern Cape by rating the anti-diabetic activity, mode of action and also highlight their therapeutic potentials based on the available evidence on their pharmacology and toxicity. Forty-five plants mentioned in ethnobotanical surveys were subjected to a comprehensive literature search in the available electronic databases such as PubMed, ScienceDirect, Google Scholar and Elsevier, by using “plant name” and “family” as the keywords for the primary searches to determine the plants that have been scientifically investigated for anti-diabetic activity. The search returned 25 families with Asteraceae highly reported, followed by Asphodelaceae and Alliaceae. Most of the plants have been studied for their anti-diabetic potentials in vivo and/or in vitro, with most of the plants having a higher percentage of insulin release and inhibition against carbohydrate digesting enzymes as compared with insulin mimetic and peripheral glucose uptake. Almost all the investigated plants also inhibit oxidative stress as part of their hypoglycemic activity with less toxicity. However, the isolation of their bioactive molecules is still lacking. This review provides a resource to enable thorough assessments of the therapeutic profiles of available medicinal plants used for the management of diabetes in the Eastern Cape, South Africa. Further studies such as the identification of the active ingredients of potent plants still need to be carried out; this may lead to new molecules in drug discovery and development.