(3,19)‐4‐Bromobenzylidene‐isoandrographolide Induces Apoptosis and Causes Loss of Mitochondrial Membrane Potential in MCF‐7 Breast Cancer Cells

Author:

Tamang Nitesh1ORCID,Inabathina Yashwanth2,Mavileti Sai Kiran1,Sripada Lakshminath1ORCID,Nanduri Srinivas3,Golakoti Nageswara Rao1ORCID,Karanam Balasubramanyam2ORCID

Affiliation:

1. Department of Chemistry Sri Sathya Sai Institute of Higher Learning Puttaparthi Andhra Pradesh India

2. Department of Biology and Cancer Research Tuskegee University Tuskegee AL 36088 USA

3. Department of Chemical Sciences National Institute of Pharmaceutical Education and Research, Balanagar 500037 Hyderabad Telangana India

Abstract

AbstractEighteen isoandrographolide analogues were synthesized, characterized and tested for their anticancer activity against 60 cancer cell lines at NCI. Three of the synthesized acetals ((3,19)‐3‐Nitro‐benzylidene‐isoandrographolide (3 p), (3,19)‐4‐Nitrobenzylidene‐isoandrographolide (3 q) and (3,19)‐4‐Isopropyl‐benzylidene‐isoandrographolide (3 r)) are novel. Most of the compounds were found to be active against leukaemia and breast cancer with (3,19)‐3,5‐difluorobenzylidene‐isoandrographolide(3 o) having the best growth inhibition of 76.90 % and 87.54 % against leukaemia (MOLT‐4) and breast cancer (BT‐549) respectively. A single crystal of compound 3 o was grown and it was characterized using single‐crystal X‐ray diffraction studies. Further studies showed that the compound (3,19)‐4‐Bromobenzylidene‐isoandrographolide (IC50 3 μM) was more active than tamoxifen (IC50 12 μM) against MCF‐7 and arrested the cell cycle at G1‐Phase of MCF‐7 and was observed to be inducing apoptosis and loss of mitochondrial membrane potential.

Funder

Vellore Institute of Technology, Chennai

National Institutes of Health

Publisher

Wiley

Subject

General Chemistry

Reference44 articles.

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