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Synthesis and biological evaluation of andrographolide analogues as anti-cancer agents

Preet, Ranjan ; Chakraborty, Biswajit ; Siddharth, Sumit ; Mohapatra, Purusottam LU ; Das, Dipon ; Satapathy, Shakti Ranjan LU ; Das, Supriya ; Maiti, Nakul C ; Maulik, Prakas R and Kundu, Chanakya Nath , et al. (2014) In European Journal of Medicinal Chemistry 85. p.95-106
Abstract

A new family of andrographolide analogues were synthesized and screened in vitro against kidney (HEK-293) and breast (MCF-7) cancer cells. The anti-cancer effects of the active analogues (2b, 2c and 4c) were determined by multiple cell based assays such as MTT, immunostaining, FACS, western blotting and transcriptional inhibition of NF-κB activity. Importantly, these compounds were found to possess higher anti-cancer potency than andrographolide and low toxicity to normal (VERO and MCF-10A) cells. Increased level of Bax/Bcl-xL ratio, caspase 3, and sub G1 population, higher expression level of tumor suppressor protein p53 and lower expression level of NF-κB suggested potent apoptotic property of the active analogues. Data revealed that... (More)

A new family of andrographolide analogues were synthesized and screened in vitro against kidney (HEK-293) and breast (MCF-7) cancer cells. The anti-cancer effects of the active analogues (2b, 2c and 4c) were determined by multiple cell based assays such as MTT, immunostaining, FACS, western blotting and transcriptional inhibition of NF-κB activity. Importantly, these compounds were found to possess higher anti-cancer potency than andrographolide and low toxicity to normal (VERO and MCF-10A) cells. Increased level of Bax/Bcl-xL ratio, caspase 3, and sub G1 population, higher expression level of tumor suppressor protein p53 and lower expression level of NF-κB suggested potent apoptotic property of the active analogues. Data revealed that the andrographolide derivative-mediated cell death in cancer cells was p53 dependent.

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publishing date
type
Contribution to journal
publication status
published
keywords
Animals, Antineoplastic Agents/chemical synthesis, Caspase 3/metabolism, Cell Line, Tumor, Chemistry Techniques, Synthetic, Diterpenes/chemical synthesis, Glutathione/metabolism, Half-Life, Humans, Hydrolysis, NF-kappa B/metabolism, Transcription, Genetic/drug effects
in
European Journal of Medicinal Chemistry
volume
85
pages
95 - 106
publisher
Elsevier Masson SAS
external identifiers
  • pmid:25078313
  • scopus:84905171913
ISSN
0223-5234
DOI
10.1016/j.ejmech.2014.07.088
language
English
LU publication?
no
additional info
Copyright © 2014 Elsevier Masson SAS. All rights reserved.
id
10bfba75-5e0b-4f9f-b114-8fa40d411c47
date added to LUP
2025-01-30 10:33:08
date last changed
2025-06-20 14:37:53
@article{10bfba75-5e0b-4f9f-b114-8fa40d411c47,
  abstract     = {{<p>A new family of andrographolide analogues were synthesized and screened in vitro against kidney (HEK-293) and breast (MCF-7) cancer cells. The anti-cancer effects of the active analogues (2b, 2c and 4c) were determined by multiple cell based assays such as MTT, immunostaining, FACS, western blotting and transcriptional inhibition of NF-κB activity. Importantly, these compounds were found to possess higher anti-cancer potency than andrographolide and low toxicity to normal (VERO and MCF-10A) cells. Increased level of Bax/Bcl-xL ratio, caspase 3, and sub G1 population, higher expression level of tumor suppressor protein p53 and lower expression level of NF-κB suggested potent apoptotic property of the active analogues. Data revealed that the andrographolide derivative-mediated cell death in cancer cells was p53 dependent.</p>}},
  author       = {{Preet, Ranjan and Chakraborty, Biswajit and Siddharth, Sumit and Mohapatra, Purusottam and Das, Dipon and Satapathy, Shakti Ranjan and Das, Supriya and Maiti, Nakul C and Maulik, Prakas R and Kundu, Chanakya Nath and Chowdhury, Chinmay}},
  issn         = {{0223-5234}},
  keywords     = {{Animals; Antineoplastic Agents/chemical synthesis; Caspase 3/metabolism; Cell Line, Tumor; Chemistry Techniques, Synthetic; Diterpenes/chemical synthesis; Glutathione/metabolism; Half-Life; Humans; Hydrolysis; NF-kappa B/metabolism; Transcription, Genetic/drug effects}},
  language     = {{eng}},
  month        = {{10}},
  pages        = {{95--106}},
  publisher    = {{Elsevier Masson SAS}},
  series       = {{European Journal of Medicinal Chemistry}},
  title        = {{Synthesis and biological evaluation of andrographolide analogues as anti-cancer agents}},
  url          = {{http://dx.doi.org/10.1016/j.ejmech.2014.07.088}},
  doi          = {{10.1016/j.ejmech.2014.07.088}},
  volume       = {{85}},
  year         = {{2014}},
}