Anticancer effects of herbal medicine Emelia-M, Mshikazi and Delosma H against human leukaemia cells.

Background: Leukaemia is one of the three major types of blood cancers that lead to the overproduction of abnormal white blood cells. Emelia M (EMB), Mshikazi and Delosma H are herbal medicines that are being used by traditional healers in KwaZulu-Natal, South Africa to treat leukaemia and other diseases. Objectives: To gain insight into the safety (non-toxic effect), anti-cancer activity, mechanisms of action and phytochemical profiles of traditional herbal medicines (Emelia M (EMB), Mshikazi and Delosma H) in South Africa. Methods: The viability of human peripheral blood mononuclear cells (PBMCs), monocytic (THP-1) and T-lymphocyte (Jurkat) cell lines exposed to varying concentrations of aqueous extracts of the three herbal medicines were assessed using adenosine triphosphate (ATP) assay. Results: All three extracts showed a dose-dependent effect on the viability of PBMCs. Cell viability decreased with increasing concentrations of extracts when compared with the untreated cells at 24 and 48 hours. The inhibitory activities (IC50) of the extract were found in the order of Mshikazi > EMB, > Delosma H. All the extracts induced apoptosis with minimal necrosis. Many bioactive compounds that have been previously reported to have anticancer effects were identified in the extracts. Conclusion: Mshikazi extract significantly inhibited the growth of THP-1 and Jurkat cells and induced cell death through apoptosis than the other two extracts.

Unravelling the drugability of MSI2 RNA recognition motif (RRM) protein and the prediction of their effective antileukemia inhibitors from traditional herb concoctions.

MSI2 is a homolog 2 of the Musashi RNA binding proteins (MSI) and is known to contribute to acute myeloid leukaemia (AML) and expressed up to 70% in AML patients. High expression of MSI2 has been found to lead to the lower overall survival of patients with AML. This study proposed the potential antagonists of MSI2 RNA-recognition motifs (MSI2 RRM1) derived from the LC-MS analysis of three traditional herbal samples. The LC-MS analysis of the three traditional herbs concoctions yields a total of 271 unique molecules of which 262 were screened against MSI2 RRM1 protein. After the dynamic study of the selected 8 top molecules from the virtual screening, the five most promising ligands emerged as potential MSI2 antagonists compare to the reference experimental molecule. The results show that the dynamic of MSI2 RRM1 protein is accompanied by a rare even of protein chain dissociation and re-association as evident in both the bound and unbound state of the protein. The unbound protein experience earlier chain dissociation compare to ligand-bound protein indicating that ligand binding to the protein slows down the dissociation time but thereafter increases the frequency of alternation between the protein chain association and dissociation after the first experience. Interestingly, the re-association of the protein chain is also accompanied by full restoration of the ligands to the binding site. The drug candidate Methotrexate (M3) and rescinnamine (M9) are listed among the promising antagonist of MSI2 with unique properties compared to a less promising molecule Ergotamine (M6).Communicated by Ramaswamy H. Sarma.

Phytochemical profile and in vitro antioxidant activity of Emelia M (EMB), Mshikazi and Delosma H herbal medicines as demonstrated in THP-1 and Jurkat leukaemia cell lines.

Background: Three decoctions, namely Emelia M (EMB), Mshikazi and Delosma H are used by traditional health practitioners in KwaZulu-Natal, South Africa to treat and manage leukaemia and related conditions. Objectives: This study evaluated the in vitro antioxidant activity and phytochemical profile of the aqueous extracts of Emelia M (EMB), Mshikazi and Delosma H decoctions. Methods: Antioxidant activity of the extracts was evaluated using1-diphenyl-2-picrylhydrazyl (DPPH), glutathione (GSH), phosphomolybdate and thiobarbituric acid reactive substance (TBARS) assays. Phytochemical screening was used to determine the presence of compounds. Results: The DPPH radical scavenging activity was similar to ascorbic acid for EMB and Delosma H, but not for Mshikazi. At 24 h, EMB increased GSH in both THP-1 and Jurkat cells similar to Delosma H while Mshikazi demonstrated the lowest activity. At 48 h, EMB and Delosma H revealed increased GSH in THP-1 cells with no significant decrease in GSH levels in Jurkat cells. However, EMB showed the lowest lipid peroxidation activity compared to Delosma H and Mshikazi after 24 h treatment of both cells. Phenols, flavonoids, terpenoids, saponins were present in all extracts. Conclusion: Extracts of the three decoctions possess both antioxidant and prooxidant properties through high scavenging activity and increased in lipid peroxidation.