IN VITRO ALPHA-GLUCOSIDASE INHIBITORY ACTIVITY OF EGYPTIAN PLANT EXTRACTS AS AN INDICATION FOR THEIR ANTIDIABETIC ACTIVITY

Objective: Diabetes mellitus is a highly prevalent chronic disease in Egypt leading to high socioeconomic problems, especially in the cities due to the unhealthy life style. Although many drugs are available, they have many side effects. Furthermore, the body arouses resistance after a while for the drug so it should be changed every once in a while. Plants could be a good source for drugs. In Egypt, we have a rich flora which has not been subjected to systematic screening for antidiabetic activity.Methods: The aim of this work was to screen 264 plant extracts for their in vitro α-glucosidase inhibitory activity. Those extracts which gave more than 70% inhibition were screened on different concentrations and their inhibitory concentrations giving 50% activity (IC50) were calculated.Results: Out of all the tested extracts, 63 gave more than or equal 70% inhibition on α-glucosidase at the tested concentration (25 ppm). After the calculation of the IC50 values, 10 extracts were chosen for further study having 5 ppm and less IC50.Conclusion: The most active plant extract is Pinus roxburghii Sarg. branches (IC50 is 2.47 ppm)

Targeted Nano-Drug Delivery of Colchicine against Colon Cancer Cells by Means of Mesoporous Silica Nanoparticles

Antimitotics are important anticancer agents and include the natural alkaloid prodrug colchicine (COL). However, a major challenge of using COL as an anticancer drug is its cytotoxicity. We developed a novel drug delivery system (DDS) for COL using mesoporous silica nanoparticles (MSNs). The MSNs were functionalized with phosphonate groups, loaded with COL, and coated with folic acid chitosan-glycine complex. The resulting nanoformulation, called MSNsPCOL/CG-FA, was tested for action against cancer and normal cell lines. The anticancer effect was highly enhanced for MSNsPCOL/CG-FA compared to COL. In the case of HCT116 cells, 100% inhibition was achieved. The efficiency of MSNsPCOL/CG-FA ranked in this order: HCT116 (colon cancer) > HepG2 (liver cancer) > PC3 (prostate cancer). MSNsPCOL/CG-FA exhibited low cytotoxicity (4%) compared to COL (~60%) in BJ1 normal cells. The mechanism of action was studied in detail for HCT116 cells and found to be primarily intrinsic apoptosis caused by an enhanced antimitotic effect. Furthermore, a contribution of genetic regulation (metastasis-associated lung adenocarcinoma transcript 1 (MALAT 1), and microRNA (mir-205)) and immunotherapy effects (angiopoietin-2 (Ang-2 protein) and programmed cell death protein 1 (PD-1) was found. Therefore, this study shows enhanced anticancer effects and reduced cytotoxicity of COL with targeted delivery compared to free COL and is a novel method of developing cancer immunotherapy using a low-cost small-molecule natural prodrug