Cytotoxicity of naturally occurring phenolics and terpenoids from Kenyan flora towards human carcinoma cells

Background: Cancer constitutes a major hurdle worldwide and its treatment mainly relies onchemotherapy.Objectives: The present study was designed to evaluate the cytotoxicity of eleven naturally occurringcompounds including six phenolics amongst them were 4 chalcones and 2 flavanones as well as 5 terpenoids (3 clerodane and 2 trachylobane diterpenoids) against 6 human carcinoma cell lines and normalCRL2120 fibroblasts.Materials and methods: The neutral red uptake (NR) assay was used to evaluate the cytotoxicity of thecompounds, whilst caspase-Glo assay was used to detect caspase activation. Cell cycle and mitochondrialmembrane potential (MMP) were all analyzed via flow cytometry meanwhile levels of reactive oxygenspecies (ROS) was measured by spectrophotometry.Results: Chalcones: 20,40-dihydroxy-60-methoxychalcone (1); 40,60-dihydroxy-20,50-dimethoxychalcone(2); 20,40,60-trihydroxy-50-methoxychalcone (3); 20,60-diacetate-40-methoxychalcone (4), trachylobanediterpenoids: 2,6,19-trachylobanetriol; (ent-2a,6a)-form (10) and 2,18,19-trachylobanetriol; (ent-2a)-form (11) as well as doxorubicin displayed IC50 values below 110 mM in the six tested cancer cell lines. TheIC50 values of the most active compounds were between 6.30 mM and 46.23 mM for compound 1respectively towards breast adenocarcinoma MCF-7 cells and small lung cancer A549 cells and between0.07 mM and 1.01 mM for doxorubicin respectively against SPC212 cells and A549 cells. Compounds 1induced apoptosis in MCF-7 cells mediated by increasing ROS production and MMP loss.Conclusion: Chalcones 1e3 are potential cytotoxic phytochemicals that deserve more investigations todevelop novel anticancer drugs against human carcinoma.© 2018 Transdisciplinary University, Bangalore and World Ayurveda Foundation. Publishing Services byElsevier B.V. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).

In vivo Evaluation of Anti-malarial Activity of Stem and Root Extracts of Erythrina abyssinica

Aims: The aim of the study was to determine the in vivo anti-malarial activity of stem and root extracts of E. abyssinica using the 4-day suppressive in vivo anti-malarial test. Methodology: Female mice weighing approximately 20±2 g were intra-peritoneally injected with mice passaged Plasmodium berghei parasites. The extracts were then administered orally 2 h post-infection and, subsequently, daily for 4 days. On the 4th day, blood smears were prepared from all the mice, stained with giemsa and parasitaemia as well as chemosuppression determined. Results: Comparatively, the root extracts exhibited higher chemosuppression than stem extracts and the level of chemosuppression was dose dependent being the highest at 50 mg/kg and lowest at 12.5 mg/kg. Survival time in extract treated and chloroquine treated groups was 2 to 3 fold higher than the –ve control. Conclusion: These findings suggest that the root extracts are more efficacious in suppressing the development of full blown malaria compared to stem extracts and may be a useful candidate in managing malaria in future.