Contraceptive and hormonal properties of the stem bark of Dysoxylum binectariferum in rat and docking analysis of rohitukine, the alkaloid isolated from active chloroform soluble fraction

Keshri, Govind; Oberoi, Ravi Mohan; Lakshmi, Vijai; Pandey, Kartikey; Singh, Man Mohan

doi:10.1016/j.contraception.2007.07.009

Cited by 29 publications

(10 citation statements)

References 20 publications

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“…Phytochemical screenings of the aqueous and methanol extract of F. asperifolia have revealed the presence of alkaloids and saponins. Data from the literature indicate that these two well-known compounds possess uterine stimulating effects [29–31]. It could therefore be understood that the presence of these biological principles in the extracts of F. asperifolia, especially its aqueous extract, may account for the observed uterine contractile activity.…”

Section: Discussionmentioning

confidence: 99%

Evaluation of In Vitro Uterotonic Activities of Fruit Extracts of Ficus asperifolia in Rats

Watcho

Ngadjui

Nkeng-Efouet

et al. 2011

Evidence-Based Complementary and Alternative Medicine

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The aim of the present study was to determine the uterotonic activities of Ficus asperifolia and investigate its mechanism. The effects of aqueous and methanol extracts of the dried fruits of F. asperifolia (0.05–1.60 mg mL−1) were evaluated on estrogenized isolated rat uterus in the presence and absence of atropine (1.73–55.27 nM), pyrilamine maleate (1.25 × 10−3 to 40 × 10−3 M), indomethacin (0.06 × 10−5 to 2.00 × 10−5 M) or hexamethonium (0.66 × 10−4 to 21.43 × 10−4 M). Aqueous (EC50, 0.36 mg mL−1) and methanol (EC50, 0.22 mg mL−1) extracts as well as oxytocin (EC50, 0.02 nM), acetylcholine (EC50, 7.87 nM) and histamine (EC50, 0.76 nM) evoked concentration-dependent contractions of the uterus. Atropine, pyrilamine maleate and indomethacin concentration dependently blocked the response of the uterus to acetylcholine (IC50, 4.82 nM), histamine (IC50, 2.49 nM) and oxytocin (IC50, 0.07 nM), respectively, and to aqueous extract. Hexamethonium produced graded decreases in oxytocin-induced uterine contractions (IC50, 0.37 μM), but did not prevent the contractile effects of the aqueous extract (IC50, 9.88 μM). These results suggest that F. asperifolia-induced uterotonic effect is related to the release of prostaglandins and contraction of the myometrial cells through muscarinic, oxytocic and H1 histamine receptors. These data further give added value to the ethnic use of F. asperifolia for its abortificient and contraceptive properties.

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Section: Discussionmentioning

confidence: 99%

Evaluation of In Vitro Uterotonic Activities of Fruit Extracts of Ficus asperifolia in Rats

Watcho

Ngadjui

Nkeng-Efouet

et al. 2011

Evidence-Based Complementary and Alternative Medicine

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“…Later the alkaloid was also reported from Dysoxylum binectariferum (Meliaceae) and Schumanniophyton problematicum (Rubiaceae) (Naik et al 1988;Houghton and Hairong 1987;Houghton and Woldemariam 1993;Yang et al 2003Yang et al , 2004. The compound is reported to possess anti-inflammatory, anti-fertility, anti-implantation, anti-cancer and immuno-modulatory properties (Naik et al 1988;Mohana Kumara et al 2010;Keshri et al 2007;Ismail et al 2009). Several semi-synthetic analogs of rohitukine have been developed of which flavopiridol (also known as HMR 1275 or Alvocidib) is well known (De Souza 1993).…”

Section: Introductionmentioning

confidence: 87%

Fusarium proliferatum, an endophytic fungus from Dysoxylum binectariferum Hook.f, produces rohitukine, a chromane alkaloid possessing anti-cancer activity

Kumara

Zuehlke

Priti

et al. 2011

Antonie van Leeuwenhoek

119

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Rohitukine is a chromane alkaloid possessing anti-inflammatory, anti-cancer and immuno-modulatory properties. The compound was first reported from Amoora rohituka (Meliaceae) and later from Dysoxylum binectariferum (Meliaceae) and Schumanniophyton problematicum (Rubiaceae). Flavopiridol, a semi-synthetic derivative of rohitukine is a potent CDK inhibitor and is currently in Phase III clinical trials. In this study, the isolation of an endophytic fungus, Fusarium proliferatum (MTCC 9690) from the inner bark tissue of Dysoxylum binectariferum Hook.f (Meliaceae) is reported. The endophytic fungus produces rohitukine when cultured in shake flasks containing potato dextrose broth. The yield of rohitukine was 186 μg/100 g dry mycelial weight, substantially lower than that produced by the host tissue. The compound from the fungus was authenticated by comparing the LC-HRMS and LC-HRMS/MS spectra with those of the reference standard and that produced by the host plant. Methanolic extract of the fungus was cytotoxic against HCT-116 and MCF-7 human cancer cell lines (IC(50) = 10 μg/ml for both cancer cell lines).

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“…[65] Rohitukine showed many bioactivities including anti-inflammatory and immunomodulatory effects,[61] inhibition of in vitro adipogenesis, and arrest of mitotic clonal expansion with dyslipidemia in vivo. [6869] The alkaloid showed anti-fertility activity and efforts are made to enhance anti-implantation activity through structural modification[70] but showed toxicity at a moderate level against human HL-60 promyelocytic leukemia and HCT-166 colon cancer cells. [67] The distinctive chemical structure of rohitukine [Figure 1b] presents a framework for derivatization and chemical synthesis of new novel molecules.…”

Section: Introductionmentioning

confidence: 99%

Anticancer alkaloids from trees: Development into drugs

Isah¹

2016

Phcog Rev

117

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Trees have made an enormous phytochemical contribution in anticancer drugs' development more than any other life form. The contributions include alkaloids that are biosynthesized in various ways and yield. Lead alkaloids isolated from the trees are taxol and camptothecins that currently have annual sales in billion dollars. Other important alkaloids isolated from these life forms include rohitukine, harringtonine, acronycine, thalicarpine, usambarensine, ellipticine, and matrines. Studies on their mechanism of action and target on the DNA and protein of cancerous cells aided the development of potent hemisynthesized congeners. The molecules and their congeners passed/are passing a long period of historical development before approved as antineoplastic drugs for cancer chemotherapy. Some of them did not find the application as anticancer drugs due to ineffectiveness in clinical trials; others are generating research interest in the antineoplastic activity at the present and have reached clinical trial stages. Potentials in antineoplastic molecules from trees are high and are hoped to be commensurate with cancer types afflicting human society in the future.

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Contraceptive and hormonal properties of the stem bark of Dysoxylum binectariferum in rat and docking analysis of rohitukine, the alkaloid isolated from active chloroform soluble fraction

Cited by 29 publications

References 20 publications

Evaluation of In Vitro Uterotonic Activities of Fruit Extracts of Ficus asperifolia in Rats

Evaluation of In Vitro Uterotonic Activities of Fruit Extracts of Ficus asperifolia in Rats

Fusarium proliferatum, an endophytic fungus from Dysoxylum binectariferum Hook.f, produces rohitukine, a chromane alkaloid possessing anti-cancer activity

Anticancer alkaloids from trees: Development into drugs

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