Anti-Cancer Agent: The Labdane Diterpenoid-Andrographolide (original) (raw)
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Cancer letters, 2018
The diterpene lactone andrographolide, isolated from Andrographis paniculata, has been proven to possess several important protective biological activities, including antioxidant, anti-inflammatory, immunomodulatory, antiseptic, antimicrobial, cytotoxic, hypolipidemic, cardioprotective, hepatoprotective, and neuroprotective effects. In addition, it has been reported to play a therapeutic role in the treatment of major human diseases, such as Parkinson's disease, rheumatoid arthritis, and colitis. This systematic review aims to highlight andrographolide as a promising agent in cancer treatment. To this purpose, a number of databases were used to search for the cytotoxic/anticancer effects of andrographolide in pre-clinical and clinical studies. Among 1703 identified literature articles, 139 were included in this review; 109 were investigated as non-clinical, whereas 24, 3, and 3 were pre-clinical, clinical, and non-pre-clinical trials, respectively. Among the model systems, cultu...
Phytochemistry Reviews, 2016
Natural products have been a great source of pharmaceuticals since ages. Vast screening of natural products from different sources has led to the discovery of plethora of chemotherapeutic drugs and other compounds for the betterment of human life. Several bioactive entities have been generated by the structural modifications of the natural products or by using the natives as key models in synthetic chemistry. Nonetheless, a number of natural compounds with potential bioactivities remain unexploited in the medicinal field due to their stringent chemical properties. Andrographis paniculata Nees., a traditional medicinal herb from family Acanthaceae is known for its multiple pharmacological activities. It's major bioactive constituent ''andrographolide'', possesses promising anticancer potential and is one such unexploited treasure. The architecture of the molecule consists of an a-alkylidene c-butyrolactone moiety, two olefin bond [D 8(17) and D 12(13) ], three hydroxyls at C-3, C-19, and C-14 and highly substituted trans decalin. Of the three hydroxyl groups, one is allylic at C-14, and the others are secondary and primary at C-3 and C-19, respectively. By modification of the above structural features a number of andrographolide derivatives have been synthesized. The intricacy of the molecule has always been a constraint in developing a commercialized drug, nevertheless the efforts in this direction via synthetic chemistry are still continuous and prominent. The present review highlights the chemistry and anticancer activity of andrographolide. It discusses the limitations of the molecule as a pharmacological agent. Modifications in the key molecule along different moieties has been discussed which might lead to desirable bioactive molecules. The compiled information will be helpful in further developing specific modifications in andrographolide moiety which will have significant contribution in semi synthesis of anti-cancer agents.
Anti-Cancer Activity of Andrographolide: A Review
Journal of Pharmaceutical Research International, 2021
Andrographolide, is a chemical compound obtained from the Andrographis paniculata (Family- Acanthaceae), maybe a diterpene lactone ring is responsible for various biological activities like anti-inflammation, anti-microbial anti-cancer, anti-obesity, anti-diabetes, anti-oxidant immunomodulatory, antiseptic, hypolipidemic, cardioprotective, hepatoprotective, neuroprotective effects and other biological activities. In Current research activities worldwide to exhibit the beneficial role of Andrographolide are continuously enriching the therapeutic arsenal of this important Phyto molecule. For this purpose, several databases were accustomed explore for the anticancer/cytotoxic effects of the andrographolide in pre-clinical and clinical studies. During this report, an attempt has been given to spotlight the research findings, related to therapeutic potentials and up-to-date development within the pharmacological activities of andrographolide. Andrographolide is often one of the potential...
2021
Andrographolide, an ent-labdane diterpenoid compound that has been isolated from the stem and leaves of Andrographis paniculata (Burm.f.) Nees by Gorter.1 It is proved to exhibit significant biological activities including antioxidant, anti-inflammatory, antimicrobial, antiseptic, hypolipidemic, cytotoxic, hepatoprotective, neuroprotective activities.2 Andrographolide is also accepted as a potent anticancer drug, studied extensively for the treatment of various kinds of cancers like brain, heart, lung, pancreas, prostate, oral, liver, colon, kidney, breast, skin, colorectal, blood, and bone marrow cancers. Mechanism of anticancer activity of andrographolide includes suppression of cyclins and cyclin-dependent kinases, induction of tumour suppressor proteins p53 and p21, increased level of Bax protein and decreased level of Bcl-2 proteins in a leukaemia cell line (HL-60 cells), G0/G1 phase arrest in breast cancer cell line (MCF-7 cells), cell cycle arrest in G2/M phase in human gliob...
Anticancer activity of andrographolide semisynthetic derivatives
Natural product communications, 2010
Andrographolide 1, a diterpene lactone of Andrographis paniculata, displays in vitro and in vivo antitumor activity against breast cancer models and mouse myeloid leukemia (M1) cells. In the present study, we report the semi-synthesis of andrographolide derivatives and their in vitro activity against A549 (ATCC) (NSCL cancer) cell line. Amongst the derivatives tested, compounds 3-5 displayed maximum activity, with IC50 values of 22-31 microg/mL.
The Prowess of Andrographolide as a Natural Weapon in the War against Cancer
Cancers
There has been a paradigm shift in our understanding about the multifaceted nature of cancer, and a wealth of information has revealed that single-target drugs are not good enough to provide satisfactory clinical outcomes and therapeutic effects for complex diseases which involve multiple factors. Therefore, there has been a reignition to search for natural products having premium pharmacological activities aim to efficiently target multiple deregulated cellular signaling pathways. Andrographolide, a diterpene lactone from Andrographis paniculata was brought into to the limelight because of its ability to inhibit cancer cell proliferation and induce apoptosis. Here we reviewed andrographolide on cellular pathways regulation including Wnt/β-catenin, mTOR, VEGF-mediated intracellular signaling, as well as TRAIL-mediated apoptosis to inhibit cancer development.
Semisynthesis and in vitro anticancer activities of andrographolide analogues
Phytochemistry, 2007
The plant Andrographis paniculata found throughout Southeast Asia contains Andrographolide 1, a diterpenoid lactone, which has antitumour activities against in vitro and in vivo breast cancer models. In the present study, we report on the synthesis of andrographolide derivatives, 3,19-isopropylideneandrographolide (2), 14-acetyl-3,19-isopropylideneandrographolide (3) and 14-acetylandrographolide (4), and their in vitro antitumour activities against a 2-cell line panel consisting of MCF-7 (breast cancer cell line) and HCT-116 (colon cancer cell line). Compounds 2 and 4 were also screened at the US National Cancer Institute (NCI) for their activities against a panel of 60 human cancer cell lines derived from nine cancer types. Compound 2 was found to be selective towards leukaemia and colon cancer cells, and compound 4 was selective towards leukaemia, ovarian and renal cancer cells at all the dose-response parameters. Compounds 2 and 4 showed non-specific phase of the cell cycle arrest in MCF-7 cells treated at different intervals with different concentrations. NCI's COMPARE and SOM mechanistic analyses indicated that the anticancer activities of these new class of compounds were not similar to that of standard anticancer agents, suggesting novel mechanism(s) of action. .my (J. Stanslas). www.elsevier.com/locate/phytochem Phytochemistry 68 (2007) 904-912 PHYTOCHEMISTRY
Andrographolide, a potential cancer therapeutic agent isolated from Andrographis paniculata
Journal of Experimental Therapeutics and Oncology, 2003
Andrographis paniculata plant extract is known to possess a variety of pharmacological activities. Andrographolide, the major constituent of the extract is implicated towards its pharmacological activity. We studied the cellular processes and targets modulated by andrographolide treatment in human cancer and immune cells. Andrographolide treatment inhibited the in vitro proliferation of different tumor cell lines, representing various types of cancers. The compound exerts direct anticancer activity on cancer cells by cell-cycle arrest at G0/G1 phase through induction of cell-cycle inhibitory protein p27 and decreased expression of cyclin-dependent kinase 4 (CDK4). Immunostimulatory activity of andrographolide is evidenced by increased proliferation of lymphocytes and production of interleukin-2. Andrographolide also enhanced the tumor necrosis factor-production and CD marker expression, resulting in increased cytotoxic activity of lymphocytes against cancer cells, which may contribute for its indirect anticancer activity. The in vivo anticancer activity of the compound is further substantiated against B16F0 melanoma syngenic and HT-29 xenograft models. These results suggest that andrographolide is an interesting pharmacophore with anticancer and immunomodulatory activities and hence has the potential for being developed as a cancer therapeutic agent.
Andrographolide: A New Plant-Derived Antineoplastic Entity on Horizon
Evidence-Based Complementary and Alternative Medicine, 2011
Plant-derived natural products occupy an important position in the area of cancer chemotherapy. Molecules such as vincristine, vinblastine, paclitaxel, camptothecin derivatives, epipodophyllotoxin, and so forth, are invaluable contributions of nature to modern medicine. However, the quest to find out novel therapeutic compounds for cancer treatment and management is a never-ending venture; and diverse plant species are persistently being studied for identification of prospective anticancer agents. In this regard,Andrographis paniculataNees, a well-known plant of Indian and Chinese traditional system of medicines, has drawn attention of researchers in recent times. Andrographolide, the principal bioactive chemical constituent of the plant has shown credible anticancer potential in various investigations around the globe.In vitrostudies demonstrate the capability of the compound of inducing cell-cycle arrest and apoptosis in a variety of cancer cells at different concentrations. Andro...