Comprehensive Profile Of Madhuca Longifolia In Pharma And Food Industry

: Madhuca longifolia (J.Koenig) J.F.Macbr. belongs to the family Sapotaceae, also commonly known as mahua or butternut tree. Each part of the plant is known for its unique medicinal properties. This review aims to enhance the existence of application and extend the therapeutic potential of Madhuca species in Pharmaceuticals, cosmeceuticals, agriculture and the food industry. Madhuca longifolia and all its products are widely used as a traditional and herbal medicine system. Even though they are used traditionally by a population of local areas, the potential of therapeutic existence is still uncovered. This systematic review is an exhaustive compilation of detailed data on phytochemistry, wide ethnopharmacological uses, medicinal properties and commercial application of mahua in different sectors. With the potential of spasmogenic, oxytocic, uterotonic, anti-bacterial, anti implantation, anti-tumor, anti-progestational, antiestrogenic activity against menorrhagia and anti-cancer, and many more. M. longifolia is also used in stomach ache, snake bite, scorpion bite, bone fractures, treatment of piles, joint pains, increase lactation, etc. It can contribute towards the development of the pharmaceutical sector and food industry too. Positively it will provide a path for future research for the development of herbal drugs and other products for agriculture and the food industry.

In vitro evaluation of estrogenic, antiestrogenic and antitumor effects of amentoflavone

Apigenin, a flavonoid, is reported to act as an estrogen receptor (ER) agonist and inhibit aromatase enzyme. However, amentoflavone, a biflavonoid bearing two apigenin molecules, has not been evaluated for its endocrine modulatory effects. Besides, it is highly consumed by young people to build muscles, enhance mood and lose weight. In the present study, apigenin was used as a reference molecule and ER mediated as well as ER-independent estrogenic/antiestrogenic activity of amentoflavone was investigated. Antitumor activity of amentoflavone was also investigated in both ER positive (MCF-7 BUS) and triple-negative (MDA-MB-231) breast cancer cells and its cytotoxicity was evaluated in human breast epithelial cells (MCF-10A). Our data confirmed ER agonist, aromatase inhibitory and cytotoxic effects of apigenin in breast cancer cells, where no ER mediated estrogenic effect and physiologically irrelevant, slight, aromatase inhibition was found for amentoflavone. Although selective cytotoxicity of amentoflavone was found in MCF-7 BUS cells, it does not seem to be an alternative to the present cytotoxic drugs. Therefore, neither an adverse effect, mediated by an estrogenic/antiestrogenic effect of amentoflavone nor a therapeutical benefit would be expected from amentoflavone. Further studies could be performed to investigate its in vivo effects.

Polarity Difference and the Presence of Phytoestrogen Compounds Affecting Estrogenic Activity of Peperomia pellucida Extracts

Peperomia pellucida (L.) Kunth has been studied as an anti-osteoporotic agent. However, there is no report about its estrogenic activity, which is important for its anti-osteoporotic activity. Thus, the aim of this research was to study the estrogenic potency of P. pellucida extracts. The estrogenic activity of P. pellucida extracts (n-hexane, ethyl acetate, ethanol, and water extracts) was studied using E-screen assay and confirmed with a molecular docking simulations. Further, the presence of phytoestrogen compounds was identified using thin layer chromatography (TLC), TLC densitometry, and high performance liquid chromatography. The n-hexane, ethyl acetate, and ethanol extracts at a concentration of 0.1 μg mL-1 exhibited a partial agonist effect, whereas the water extract showed full agonisteffect at the similar concentration. This activity was produced through a classical ligand-dependent mechanism similar to estradiol. N-hexane and ethyl acetate extracts showed antiestrogenic activity. The TLC chromatogram evidently depicted the presence of quercetin and stigmasterol in the n-hexane and ethyl acetate extracts. Apigenin and apigetrin at concentrations of 0.239±0.076 and 1.063±0.156 μg mg-1 extract, respectively, were present in the water extract. A docking study on estrogen receptors confirmed that apigetrin prefer to produce estrogenic activity, whereas the other compounds can produce both estrogenic and antiestrogenic activity. Hence, we suggest that the bioactive compounds in the water extract are flavonoids, such as apigenin and apigetrin. In summary, the water extract is recommended to be used as an estrogenic agent.

Antifertility effect of curcumin, an indigenous medicine in rats

Background: Curcumin is an active constituent, obtained from rhizome of Curcuma longa linn, known to have broad medicinal properties, was studied for its effect on fertility in female rats. Curcumin has anti-ovulatory effect probably by its antiestrogenic activity through suppression of negative feedback of estrogen on pituitary.Methods: Inbred Charles Foster female albino rats (150-180 gm) were used for study. They were divided into different groups and treated with curcumin (25 mg/kg. and 50 mg/kg body weight) as per schedule. The antigonadotropic, antiestrogenic, anti-implantation and abortifacient effect on curcumin treated albino rats were demonstrated.Results: The results showed significant reduction in the number of implants and size of litters in curcumin treated rats compared to normal control group. The results were compared with Tamoxifen (10mg/ kg bodyweight) a known antifertility drug, which further substantiated the antifertility effects of curcumin.Conclusions: The results indicated the ways in which curcumin exerts antifertility effects and thus can play a vital role in fertility control.

Antiestrogenic Activity and Possible Mode of Action of Certain New Nonsteroidal Coumarin-4-acetamides

The preparation of certain 2-(2-oxo-2H-chromen-4-yl)-N-substituted acetamides IIIa–h was planned as a step in the development of new modified nonsteroidal antiestrogens. The purity of target compounds IIIa–h was checked by thin-layer chromatography (TLC), and their structures were confirmed using various spectroscopic tools including IR, 1H-NMR, 13C-NMR, and MS spectroscopy. Viability tests were applied using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay to evaluate the cytotoxic effect of the synthesized compounds against two breast cancer cell lines, MCF-7 and MDA-MB-231. Compound IIIb proved the most active against MCF-7 cells, with an IC50 value of 0.32 μM. The results of an analysis of in vitro antiestrogenic activity indicated that only compound IIIb exhibited antiestrogenic activity; its IC50 value of 29.49 μM was about twice as potent as that of the reference compound, MIBP. The aromatase activity was evaluated for the synthesized target compounds IIIa–g and the intermediates Ib and IIa. A significant aromatase inhibition was observed for the intermediate Ib and compound IIIe, with IC50 values of 14.5 and 17.4 μM, respectively. Compound IIIb, namely 7-methoxy-4-(2-oxo-2-(piperidin-1-yl)ethyl)-2H-chromen-2-one, could be used as an antiestrogen and/or cytotoxic agent with selective activity against tumor cells.

Cycloartane and Stigmastane Type Triterpenoids from Pothos scandens Inhibit Estradiol (E2) Induced Proliferations in Breast Cancer Cells

Four cycloartane type triterpenoids and three stigmastane type steroids were isolated from the methanolic extract of stem and root part of Pothos scandens L. (Araceae), a Bangladeshi medicinal plant by high performance liquid chromatographic technique. The compounds were characterized as 24-methylenecycloartanol (1), 24-methylenecycloartenone (2), 24-en-cycloartenone (3), 24-methylenecycloartanyl ferulate (4), stigmast-4-en-3-one (5), stigmast-4,22-diene-3-one (6) and β-sitosterol glucoside (7) through extensive 1D and 2D NMR spectroscopic studies. All the isolates were evaluated for their estrogenic/antiestrogenic activity using the estrogen-responsive breast cancer cell lines, MCF-7 and T47D. The results showed that all the compounds possess mild to strong antiestrogenic activity in both cell lines which was compared to positive control tamoxifen. 24- Methylenecycloartanol (1), which contains a hydroxyl group in its C-3 position, inhibited 90% of estradiol (E2)- induced cell proliferation in MCF-7 and T47D cell lines at a concentration of 0.01 μM only. 24- Methylenecycloartanyl ferulate (4) and stigmast-4,22-diene-3-one (6) showed 90% of estradiol (E2)-induced cell proliferation in T47D cell only at a concentration of 0.01 μM whereas 10.0 μM was required for 24- methylenecycloartanyl ferulate (4) for the same activity in MCF-7 cells. This is the first report of isolation of these compounds from the plant along with their antiestrogenic property. Dhaka Univ. J. Pharm. Sci. 18(1): 93-102, 2019 (June)

ISOLATION, CHARACTERIZATION AND ANTIFERTILITY ACTIVITY OF THE ACTIVE MOIETY FROM THE STEM OF MUSA PARADISIACA L.

Bioactive principles from the hyroalcoholic (50%) extract of Musa paradisiaca L. stem were isolated and characterized to evaluate antifertility activity in female albino rats. Oral acute toxicity study was done with crude extract for 24h. The hydro alcoholic extract of M. paradisiaca stem was subjected to silica gel column chromatography using gradient solvent system DCM: Eth, Mth: Eth and Mth., ten different fraction were collected. The yield of fraction Mu-HA- Mps was 580 mg, further fractionated for purification by using solvent DCM-MeOH (3:2) to yield compound Mu-HA-Mps (20.22 %w/w). Isolated compound Mu-HA-Mps was subjected to evaluation of its antifertility potential by antiovulatory and estrogenic activity. The isolated compound Mu-HA-Mps was found to exhibit significant antiovulatory and antiestrogenic activity at doses of 100 and 200 mg/kg body weight. Isolated compound Mu-HAMps was subjected to structure elucidation by UV, IR, NMR and MASS spectral analytical methods. The results of the present study provide evidence of anti-fertility activity of isolated compound Mu-HA-Mps as claimed in the traditional use. The hydroalcoholic extract of Musa paradisiaca L. furnished a compound whose structure was established as 4’-methoxy-7-hydroxyisoflavone on the basis of physical and spectral basis and could be a good source of drug for birth control.