Baroi, S., Saha, A., Ritesh Bachar, R., and Bachar, S.C. Cannabinoid as Potential Aromatase Inhibitor Through Molecular Modeling and Screening for Anti-Cancer Activity. Dhaka Univ. J. Pharm. Sci. 19(1): 47-58, 2020 (June 28, 2020.) doi: 10.3329/dujps.v19i1.47818
Breast cancer is the most prevalent type of cancer, with over 234,000 cases reported in the U.S. in 2015. Estrogen dependent carcinomas are among the most common types of breast cancer.
Aromatase is an enzyme that converts cholesterol to estradiol E2, the most biologically active form of estrogen.
The 2020 virtual screening technique and docking study looked at cannabinoids that may serve as potential inhibitors of aromatase, thus limiting the estrogen biosynthesis pathway. The study used cannabis sativa molecules to develop aromatase inhibitors via computer-based techniques in a lab-based studies. The study examined 61 cannabinoid compounds as potential anticancer drugs after ADEMT checking. ADEMT is chemical absorption, distribution, metabolism, excretion, and toxicity; these are key factors that must be checked in drug studies. A high-quality drug candidate should show an anticancer potential and appropriate ADMET properties at a level of therapeutic dosing.
Cannabinoids as Aromatase Inhibitors for Anti-Cancer Activity: Study Findings
The study identified three molecules as the most likely candidates to be further studied for their anti-tumor effects on hormone targeted breast cancer. These candidates include cannabidiorcol (CBD-C1), and cannabiripsol (CBR). And cannabitriol (CBT). These three compounds were found to have significant cytotoxic activity with the potential to be developed as very strong aromatase inhibitors.
The study revealed preliminary findings that show that some cannabinoids and compounds should be included in future studies on aromatase inhibitors for anti-cancer activity and cancer treatment modalities. Link to article: https://doi.org/10.3329/dujps.v19i1.47818