Abstract 3818: Isoandrographolide derivative, (3,19)-4-Bromobenzylidene-isoandrographolide induces apoptosis and causes loss of mitochondrial membrane potential in ER positive Breast cancer

Abstract

Abstract Natural product, Andrographolide.is diterpene lactone extracted from Andrographis paniculata. In traditional form of medicine, it is being used in India, China and Malaysia for treating various diseases. While in the last two decades there are many reports on andrographolides and its derivatives with various biological activities such as anti-cancer and anti-inflammatory. We synthesized compounds along with isoandrographolide were characterized and tested for their anticancer activity against 60 cancer cell line at NCI. Most compounds were found to be active against leukemia and breast cancer with (3,19)-4-Bromobenzylidene-isoandrographolide having best growth inhibition of 76.90% and 87.54% against leukemia (MOLT-4) and breast cancer (BT-549) respectively. Upon further testing compound (3,19)-4-Bromobenzylidene-isoandrographolide was found to be more activate than the tamoxifen against MCF-7. Compound (3,19)-4-Bromobenzylidene-isoandrographolide arrested cell cycle at G1-Phase of MCF-7 and was observed to be inducing apoptosis and loss of mitochondrial membrane potential. We discuss our studies on crystal structure, cell cycle progression assay, apoptotic studies on ER-positive breast cancer MCF-7. Citation Format: Balasubramanyam Karanam, Nitesh Tamang, Yashwanth Inabathina, Sai Kiran Mavileti, Lakshminath Sripada, Srinivas Nanduri, Nageswara Rao Golakoti. Isoandrographolide derivative, (3,19)-4-Bromobenzylidene-isoandrographolide induces apoptosis and causes loss of mitochondrial membrane potential in ER positive Breast cancer. [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2023; Part 1 (Regular and Invited Abstracts); 2023 Apr 14-19; Orlando, FL. Philadelphia (PA): AACR; Cancer Res 2023;83(7_Suppl):Abstract nr 3818.