NCI in vitro and in silico anticancer screen, cell cycle pertubation and apoptosis-inducing potential of new acylated, benzylidene and isopropylidene derivatives of andrographolide
Andrographolide (AGP) is the main bioactive constituent isolated from the traditional medicinal, Andrographis paniculata which contributes towards its various biological activities, including anticancer property. In this study, a series of new AGP derivatives were semi-synthesised and screened again...
| Main Authors: | , , , , , , |
|---|---|
| Format: | Article |
| Published: |
Elsevier
2014
|
| Online Access: | http://psasir.upm.edu.my/id/eprint/34632/ |
| _version_ | 1848847827803832320 |
|---|---|
| author | Wong, Charng Choon Sagineedu, Sreenivasa Rao Sumon, Shariful Hasan Mohamad Sidik, Shiran Phillips, Roger Lajis, Nordin Stanslas, Johnson |
| author_facet | Wong, Charng Choon Sagineedu, Sreenivasa Rao Sumon, Shariful Hasan Mohamad Sidik, Shiran Phillips, Roger Lajis, Nordin Stanslas, Johnson |
| author_sort | Wong, Charng Choon |
| building | UPM Institutional Repository |
| collection | Online Access |
| description | Andrographolide (AGP) is the main bioactive constituent isolated from the traditional medicinal, Andrographis paniculata which contributes towards its various biological activities, including anticancer property. In this study, a series of new AGP derivatives were semi-synthesised and screened against the NCI in vitro 60 cell lines. From the screening results, we had identified SRS07 as the most potent AGP derivative, against breast and colon cancer cell lines. Subsequently, SRS07 was tested for its capability to induce cell cycle arrest and apoptosis in MCF-7 and HCT116 cancer cells. SRS07 effectively induced G1 cell cycle arrest in both cell lines and ultimately apoptosis by inducing DNA fragmentation in HCT116 cells. The apoptotic cell death induced by SRS07 was confirmed via FITC Annexin-V double staining. Western blot analysis of SRS07-treated HCT116 cells revealed that the compound induced apoptosis be activating caspase 8 which in turn cleaved Bid to t-Bid to initiate cell death cascade. Prediction of the possible mode of action of SRS07 by utilising NCI COMPARE analysis failed to reveal a distinct mechanism category. Hence, it is speculated that SRS07 possesses novel mechanism of action. In conclusion, SRS07 demonstrated superior in vitro anticancer profiles and emerged as a potential lead anticancer candidate. |
| first_indexed | 2025-11-15T09:24:48Z |
| format | Article |
| id | upm-34632 |
| institution | Universiti Putra Malaysia |
| institution_category | Local University |
| last_indexed | 2025-11-15T09:24:48Z |
| publishDate | 2014 |
| publisher | Elsevier |
| recordtype | eprints |
| repository_type | Digital Repository |
| spelling | upm-346322015-12-16T07:19:42Z http://psasir.upm.edu.my/id/eprint/34632/ NCI in vitro and in silico anticancer screen, cell cycle pertubation and apoptosis-inducing potential of new acylated, benzylidene and isopropylidene derivatives of andrographolide Wong, Charng Choon Sagineedu, Sreenivasa Rao Sumon, Shariful Hasan Mohamad Sidik, Shiran Phillips, Roger Lajis, Nordin Stanslas, Johnson Andrographolide (AGP) is the main bioactive constituent isolated from the traditional medicinal, Andrographis paniculata which contributes towards its various biological activities, including anticancer property. In this study, a series of new AGP derivatives were semi-synthesised and screened against the NCI in vitro 60 cell lines. From the screening results, we had identified SRS07 as the most potent AGP derivative, against breast and colon cancer cell lines. Subsequently, SRS07 was tested for its capability to induce cell cycle arrest and apoptosis in MCF-7 and HCT116 cancer cells. SRS07 effectively induced G1 cell cycle arrest in both cell lines and ultimately apoptosis by inducing DNA fragmentation in HCT116 cells. The apoptotic cell death induced by SRS07 was confirmed via FITC Annexin-V double staining. Western blot analysis of SRS07-treated HCT116 cells revealed that the compound induced apoptosis be activating caspase 8 which in turn cleaved Bid to t-Bid to initiate cell death cascade. Prediction of the possible mode of action of SRS07 by utilising NCI COMPARE analysis failed to reveal a distinct mechanism category. Hence, it is speculated that SRS07 possesses novel mechanism of action. In conclusion, SRS07 demonstrated superior in vitro anticancer profiles and emerged as a potential lead anticancer candidate. Elsevier 2014-09 Article PeerReviewed Wong, Charng Choon and Sagineedu, Sreenivasa Rao and Sumon, Shariful Hasan and Mohamad Sidik, Shiran and Phillips, Roger and Lajis, Nordin and Stanslas, Johnson (2014) NCI in vitro and in silico anticancer screen, cell cycle pertubation and apoptosis-inducing potential of new acylated, benzylidene and isopropylidene derivatives of andrographolide. Environmental Toxicology and Pharmacology, 38 (2). pp. 489-501. ISSN 1382-6689; ESSN: 1872-7077 http://www.sciencedirect.com/science/article/pii/S1382668914001707 10.1016/j.etap.2014.07.016 |
| spellingShingle | Wong, Charng Choon Sagineedu, Sreenivasa Rao Sumon, Shariful Hasan Mohamad Sidik, Shiran Phillips, Roger Lajis, Nordin Stanslas, Johnson NCI in vitro and in silico anticancer screen, cell cycle pertubation and apoptosis-inducing potential of new acylated, benzylidene and isopropylidene derivatives of andrographolide |
| title | NCI in vitro and in silico anticancer screen, cell cycle pertubation and apoptosis-inducing potential of new acylated, benzylidene and isopropylidene derivatives of andrographolide |
| title_full | NCI in vitro and in silico anticancer screen, cell cycle pertubation and apoptosis-inducing potential of new acylated, benzylidene and isopropylidene derivatives of andrographolide |
| title_fullStr | NCI in vitro and in silico anticancer screen, cell cycle pertubation and apoptosis-inducing potential of new acylated, benzylidene and isopropylidene derivatives of andrographolide |
| title_full_unstemmed | NCI in vitro and in silico anticancer screen, cell cycle pertubation and apoptosis-inducing potential of new acylated, benzylidene and isopropylidene derivatives of andrographolide |
| title_short | NCI in vitro and in silico anticancer screen, cell cycle pertubation and apoptosis-inducing potential of new acylated, benzylidene and isopropylidene derivatives of andrographolide |
| title_sort | nci in vitro and in silico anticancer screen, cell cycle pertubation and apoptosis-inducing potential of new acylated, benzylidene and isopropylidene derivatives of andrographolide |
| url | http://psasir.upm.edu.my/id/eprint/34632/ http://psasir.upm.edu.my/id/eprint/34632/ http://psasir.upm.edu.my/id/eprint/34632/ |