Synthesis and biological activity of amide derivatives of nimbolide

Sastry, B. S.; Babu, K. Suresh; Babu, T. Hari; Chandrasekhar, S.; Srinivas, Priya; Saxena, Ajit Kumar; Rao, J. Madhusudana

doi:10.1016/j.bmcl.2006.05.105

Cited by 52 publications

(32 citation statements)

References 10 publications

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“…Recently, we identified nimbolide (5,7,4′-trihydroxy-3′,5′-diprenylflavanone), a limonoid, as one of the major constituents in neem leaf fractions by highperformance liquid chromatography [16]. Although nimbolide was shown to exert cytotoxicity against a panel of cancer cell lines, the effect of nimbolide on markers of cell proliferation and apoptosis has not been investigated [17][18][19].…”

Section: Introductionmentioning

confidence: 97%

Nimbolide a limonoid from Azadirachta indica inhibits proliferation and induces apoptosis of human choriocarcinoma (BeWo) cells

et al. 2008

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We investigated the cytotoxic effects of nimbolide, a limonoid present in leaves and flowers of the neem tree (Azadirachta indica) on human choriocarcinoma (BeWo) cells. Treatment with nimbolide resulted in dose- and time-dependent inhibition of growth of BeWo cells with IC(50) values of 2.01 and 1.19 microM for 7 and 24 h respectively, accompanied by downregulation of proliferating cell nuclear antigen. Examination of nuclear morphology revealed fragmentation and condensation indicating apoptosis. Increase in the generation of reactive oxygen species (ROS) that was reversed by addition of reduced glutathione suggested ROS involvement in the cytotoxicity of nimbolide. A decrease in Bcl-2/Bax ratio with increased expression of Apaf-1 and caspase-3, and cleavage of poly(ADP-ribose) polymerase provide compelling evidence that nimbolide-induced apoptosis is mediated by the mitochondrial pathway. The results of the present study suggest that nimbolide has immense potential in cancer prevention and therapy based on its antiproliferative and apoptosis inducing effects.

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Section: Introductionmentioning

confidence: 97%

Nimbolide a limonoid from Azadirachta indica inhibits proliferation and induces apoptosis of human choriocarcinoma (BeWo) cells

et al. 2008

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“…[27] Nimbolide , a limonoid isolated from Azadirachta indica, is the chief cytotoxic principle in Neem leaf extract being used as a lead compound for anti-cancer analogue design. [28] This clearly indicates the presence of potent bioactives which might be very useful as antiproliferative, antitumor, pesticidal and other bioactive agents. *Diameter below 7 mm is omitted, as diameter of well is 7 mm.…”

Section: Discussionmentioning

confidence: 98%

Evaluation of Brine shrimp lethality and Antimicrobial activity of Azadirachta indica leaf extract on some drug resistance bacteria in Bangladesh

Emran¹,

Shahed²,

Ahmed³

et al. 2011

Pharmacognosy Journal

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a B S t r a c tAzadirachta indica (neem) is very useful traditional medicinal plant in the subcontinent. each part of the tree has some medicinal properties. in this present studies the bioactivity and antimicrobial activity of Azadirachta indica leaf extract was evaluated. For bioactivity, Brine shrimp lethality test was done for A. indica ethanolic leaf extract and determined lc 50 was 37.15 mg/ml indicating that the prepared extract was rich in bioactive compounds. ethanolic leaf extract was also used to evaluate antibacterial activity and the extract exhibited significant activity against the tested bacterial strain. However, inhibitory activity was concentration and test organism dependent. gram-positive bacteria were more sensitive to the extract compare to gram-negative bacteria. all of the tested bacteria showed sensitivity at higher concentration (7mg/ml) but multi drug resistant bacteria Klebsiella pneumoniae was very sensitive even at very low concentration (2mg/ml). Further, the results depict that leaf extracts of Azadirachta indica could be used as a potential source of antimicrobial agents against the bacterial strains tested.

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“…Several groups reported anticancer, anti-inflammatory, and antioxidant activities of neem tree extracts [20,34,54,57] without providing in-depth analysis of the molecular mechanisms leading to NLE-induced inhibition of NF-jB activation. Accordingly, we compared Jurkat cells treated with TNF-a with or without pretreatment by NLE.…”

Section: Resultsmentioning

confidence: 99%

Anti-inflammatory, pro-apoptotic, and anti-proliferative effects of a methanolic neem (Azadirachta indica) leaf extract are mediated via modulation of the nuclear factor-κB pathway

et al. 2010

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Azadirachta indica (neem tree) is used in traditional Indian medicine for its pharmacological properties including cancer prevention and treatment. Here, we studied a neem extract's anti-inflammatory potential via the nuclear factor-jB (NF-jB) signaling pathway, linked to cancer, inflammation, and apoptosis. Cultured human leukemia cells were treated with a methanolic neem leaf extract with or without tumor necrosis factor (TNF)-a stimulation. Inhibition of NF-jB activity was demonstrated by luciferase assay and electrophoretic mobility shift assay (EMSA). Inhibition of viability by neem extracts was assessed by luminescent assays. Western blot analysis allowed assessing the inhibitory effect of the neem extract on TNF-a-induced degradation of inhibitor of jB (IjB) and nuclear translocation of the NF-jB p50/p65 heterodimer. Inhibition of IjB kinase (IKK) activity was shown as well as the effect of neem extract on the induction of apoptotic cell death mechanisms by nuclear fragmentation analysis and flow cytometry analysis. In conclusion, our data provide evidence for a strong effect of the neem extract on proinflammatory cell signaling and apoptotic cell death mechanisms, contributing to a better understanding of the mechanisms triggered by Azadirachta indica.

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Synthesis and biological activity of amide derivatives of nimbolide

Cited by 52 publications

References 10 publications

Nimbolide a limonoid from Azadirachta indica inhibits proliferation and induces apoptosis of human choriocarcinoma (BeWo) cells

Nimbolide a limonoid from Azadirachta indica inhibits proliferation and induces apoptosis of human choriocarcinoma (BeWo) cells

Evaluation of Brine shrimp lethality and Antimicrobial activity of Azadirachta indica leaf extract on some drug resistance bacteria in Bangladesh

Anti-inflammatory, pro-apoptotic, and anti-proliferative effects of a methanolic neem (Azadirachta indica) leaf extract are mediated via modulation of the nuclear factor-κB pathway

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