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Contraceptive Efficacy and Hormonal Profile of Ferujol: a New Coumarin from Ferula jaeschkeana 1

Authors:
  • Saraswati Dental College, Lucknow & CSIR Central Drug Research Institute, Lucknow, India

Abstract

The ethanolic extract of FERULA JAESCHKEANA Vatke as well as its hexane, benzene and chloroform soluble fractions prevented pregnancy in adult female rats when administered orally on days 1-5 POSTCOITUM. Chromatography of these combined fractions, whose TLC pattern was similar, yielded the active compound ferujol. Single oral administration of ferujol on days 1, 2 or 3 POSTCOITUM at 0.6 mg/kg dose prevented pregnancy in rats. None of the fractions nor ferujol, however, exhibited any contraceptive efficacy in hamsters. In ovariectomized immature female rats, ferujol showed potent estrogenic activity at the contraceptive dose, but was devoid of any antiestrogenic activity. Significant uterotrophic effect was discerned even at 1/40th of the contraceptive dose of the compound. Taking 100% increase in uterine weight as the parameter, ferujol was found to be about 10 times less estrogenic than ethynylestradiol. In addition, ferujol induced implantation of blastocysts in mice undergoing experimentally induced delayed implantation, confirming its frank estrogenic activity.
... The estrogenic activity of a polyphenolic extract of the leaves of Epimedium brevicornum and its five fractions was demonstrated by solid-phase extraction using estrogen-responsive bioassay in vitro method of yeast cell assay and the Ishikowa Var-I assay (Naeyer et al., 2004). Ferujol isolated from Ferula jaeschkeana exhibited estrogenic activity in rats (Singh et al., 1985). Carotane sequiterpanes isolated from the rhizomes of F. jaeschkeana administered to ovariectomised immature rats, exhibited estrogenic activity (Singh et al., 1985). ...
... Ferujol isolated from Ferula jaeschkeana exhibited estrogenic activity in rats (Singh et al., 1985). Carotane sequiterpanes isolated from the rhizomes of F. jaeschkeana administered to ovariectomised immature rats, exhibited estrogenic activity (Singh et al., 1985). Oral administration of acetone extract of Foeniculum vulgare seeds to female rats for 10 days lead to vaginal cornification (Malini et al., 1985). ...
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Contraception: An Herbal Medicine Approach of Citrus medica Seeds for Fertility Regulation, this research book focused on the evaluation of contraceptive activities of C. medica seeds on albino rats. Out of the tested three crude extracts, petroleum ether extract found more potential on fertility regulation, judged by phytochemical analysis, acute and chronic toxicity studies, antiimplantation, abortifacient, antiovulatory, estrogenic, progestogenic activities. Results were analysed by gravimetric, histological, histometrical, biochemical, antioxidant assays, hormonal profile by RIA and withdrawal studies with applying statistical analysis Student’s ‘t’ Test and also its TLC fractions were tested and found potential at the dose level of 50 and 100mg/kg/b.w. of fraction II in significantly. Spectroscopic analysis like UV, GCMS, IR and H1 NMR were resulted isolated compound is fatty acid mixture of fraction II, structure not elucidated and characterized due to the nature of fatty acid moiety. Hence, the fraction II is rich in fatty acid and shown contraceptive effects without obtrusive side effects in rats. Therefore, this fraction-II can be subjected for further study to harvest it, as a commercial contraceptive agent in near future.
... Various extracts of the species have been studied for their anti-implantation activity in rats and hamsters along with an assessment of hormonal properties like estrogenic, antiestrogenic, progestagenic and antiprogestagenic actions [8]. The plant is also reported to have contraceptive activity [9]. It contains ferutinol, akichenol, lencerotol, sesquiterpenes and ferujol [7,9]. ...
... The plant is also reported to have contraceptive activity [9]. It contains ferutinol, akichenol, lencerotol, sesquiterpenes and ferujol [7,9]. During survey in Drass, Sonamarg and Kishtwar areas of Jammu and Kashmir (India) the species was found to be growing in disjunct populations on dry slopes. ...
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A protocol for rapid extraction of high quantity and quality of genomic DNA and Random Amplified Polymorphic DNA Polymerase Chain Reaction (PCR) analysis has been optimized for Ferula jaeschkeana Vatke (Apiaceae), an overexploited medicinally important species of Western Himalaya in India. The protocol utilizes preserved leaf material for DNA extraction. Liquid nitrogen was used for grinding the deveined leaf tissue. The isolated DNA was essentially free of polyphenolics, polysaccharides and other major contaminants as revealed by color difference of DNA isolated by the available protocols and the present one. Quantification of the isolated DNA was performed in a UV spectrophotometer (UV1800, Shimadzu) and the purity determined by calculating the ratio of absorbance at 260 nm to that of 280 nm (260/280 = 1.8–2.0). The quality and quantity of DNA was also visualized on 0.8 % agarose gel by comparing band intensity with that of standard amount of lambda DNA (165 μg/ml, Banglore Genei Pvt. Ltd., India). The isolated DNA was diluted to 25 ng/μl which was used for PCR amplification.
... The oleo-gum resin and dried powder of F. jaeschkeana have been used in folk medicine to treat various disorders like chest pain, tumors, ulcers, and chronic wounds (Yaqoob, Nawchoo, & Ahmad, 2016). This plant has not been explored much regarding its chemical constituents (Volatile and non-volatile) and therapeutic potential (Garg, Misra, & Agarwal, 1989;Prakash, Kusum, & Sandhya, 1989;Singh et al., 1985). ...
Article
Ferula assa-foetida is an important species of the genus Ferula, best known for its oleo-gum resin, mainly used as a flavoring agent. Ferula jaeschkeana is another Himalayan medicinal plant of this genus, known for its contraceptive effect but not used in food applications. This study aimed to do a detailed phytochemical analysis of F. assa-foetida growing under controlled conditions in India using GC-MS/headspace and UHPLC-PDA-QTOF-IMS. Further, a comparative analysis of F. assa-foetida was performed with F. jaeschkeana (collected from its natural habitat) and commercial samples of F. assa-foetida oleo-gum resin (collected from the local market). UHPLC-QTOF-IMS profiling of F. assa-foetida led to the identification of foetisulfide C, assafoetidnol A, gumosin, flabellilobin (A/B), and foetisulfide A. In total, 141 metabolites were identified, including vitamins, nucleosides, sulfur compounds, flavonoids, sugars derivatives, and others, using METLIN database. Serine, arginine, asparagine, isoleucine, and phenylalanine were major amino acids quantified among the samples for the nutritional aspect. Characteristic sulfurous compounds (n-propyl-sec-butyl disulfide, trans-propenyl-sec-butyl disulfide, cis-propenyl-sec-butyl disulfide, and bis[1-(methylthio)propyl] disulfide) were identified in all samples except F. jaeschkeana. PCA and cluster analysis showed a significant difference in the volatile constituents of rhizomes of both species. Metabolomics studies also revealed the association of sesquiterpenoid and triterpenoid biosynthesis, phenylpropanoid, flavon, and flavanol biosynthesis. The current study demonstrates, "why only F. assa-foetida is used in culinary applications instead of F. jaeschkeana"?
... There is medical evidence to suggest that giant fennel and its relatives offer contraceptive properties. Several modern studies concluded that three species of Ferula (Ferula assafoetida L., Ferula orientalis L., and Ferula jaeschkeana) exhibit anti-fertility properties in rodents [36][37][38], while the resin of the asafoetida plant has been reported in human tests as acting as a contraceptive and abortifacient [39]. If this is the case, it strengthens our evidence for ancient silphium sharing similar properties. ...
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From luxury spice to medical cure-all, silphium was a product coveted throughout the ancient world and occupied an essential place in the export economy of ancient Cyrene. The mysterious extinction of the silphium plant in the 1st century CE leaves us with little evidence as to the exact nature of this important agricultural product. In this paper, an historical background on the kingdom of Cyrene is provided, evidence for the nature of the silphium plant is reviewed, how and why it was consumed and traded is discussed. Possible causes of extinction are considered in the context of plant genetics, biometrics, and soil geochemistry. Next, we demonstrate how modern medical studies conducted on possible living relatives can inform us about claims made by ancient authors as to the medical uses of the silphium plant, including its use as a contraceptive and abortifacient. Finally, methods for recovering silphium are explored. We show how underwater archaeology and the search for ancient shipwrecks off the northern coast of Libya may offer our best chance for the recovery of botanical remains of ancient silphium, and how ancient DNA may be able to establish the genetic makeup of this elusive plant.
... This method led to several compounds that showed high pharmacological activity or precursors thereof. The phytoestrogen ferujol 24 isolated from Ferula jaeschkeana [51] was synthesized under sonochemical conditions in good yield. In addition, for the first time, simple methylation of compound 25 afforded the anti-virus and anti-platelet aggregation agent collinine (from Zanthoxylum schinifolium). ...
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Esculetin, synonymous with 6,7-dihydroxycoumarin, is the main active ingredient of the traditional Chinese medicine Cortex Fraxini. The twig skin or trunk bark of Cortex Fraxini are used by herb doctors as a mild, bitter liver and gallbladder meridians' nontoxic drug as well as dietary supplement. Recently, with a variety of novel esculetin derivatives being reported, the molecular mechanism research as well as clinical application of Cortex Fraxini and esculetin are becoming more attractive. This mini-review will consolidate what is known about the biological activities, the mechanism of esculetin and its synthetic derivatives over the past decade in addition to providing a brief synopsis of the properties of esculetin.
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The goal of our study is to increase public awareness of natural contraceptives and their powerful advantages over surgical abortion in order to provide people with an alternative method of ending an unwanted or unplanned pregnancy rather than the dreaded surgical procedure. Since ancient times, traditional remedies have been used all across the world to control fertility. Still, the tribal community mostly relies on these herbs for contraception and to cause abortions. The belief in therapeutic approaches has not been diminished despite the tremendous advancement of allopathic treatment because of its negative side effects. Plants and herbs have been used to induce abortions, although there is very little published information on the most regularly used ones. The grail of this paper is to detail the herbal products used to cause abortion.
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The petroleum ether and chloroform extracts of the roots of Cyclea burmanni (Fam. Menispermaceae) have been found to possess significant antifertility effect in rats. Both these extracts exhibited partial and complete resorption of implants at 200 and 400 mg/kg body weight dose levels. In estrogenic activity study, both the extracts increased uterine weight and caused opening and cornification of vagina in immature rats. The present work justifies its effectiveness in preventing pregnancy in all rats when administered at 400 mg/kg p.o.
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Chapter
This review of plant coumarins discovered between 1989 and early 1996 has been compiled on the premise that the reader has access to the two previous reviews in this series by the reviewer, those of 1978 in Vol. 35 (171) and 1991 in Vol. 58 (172). With these other two reviews to hand, the reader will have immediate access to every plant coumarin ever known and should readily be able to determine, for example, if a coumarin just isolated is indeed a new natural plant product.
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Hexane soluble fraction of Lepidium capitatum Hook. f. & Thoms. prevented pregnancy in adult female rats when administered orally at a daily dose of 250 mg/kg on days 1-5 post-coitum. At lower doses, there was a dose dependent inhibition of pregnancy and reduction in implantation number. It failed, however, to prevent pregnancy in hamsters up to 500 mg/kg daily dose. In ovariectomized immature female rats, the extract exhibited potent estrogenic activity at the comparable contraceptive dose, but was devoid of any antiestrogenic activity. Significant uterotrophic effect was discerned even at 1/40th the contraceptive dose. The extract also induced implantation of blastocysts in mice undergoing experimentally induced delayed implantation, confirming its frank estrogenicity. 1 Communication No. 3314
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The uterotrophic, anti-uterotrophic and contraceptive properties of several antifertility agents vere compared in female rats and hamsters. The compounds fell into two distinct groups on the basis of their biological profile in rats: 1. Estrogenic contraceptives, including estradiol-17β (E2), 17α-ethynylestradiol (EE), diethylstilbestrol (DES), ORF 3858 and F 6066; 2. Anti-estrogenic contraceptives, including CN55,945-27, U11,555A, Su 13320 and MER-25. These classifications did not hold true for hamsters. E2 and DES were only 4–5% as active in hamsters as in rats as uterotrophic or contraceptive agents; other estrogens were even less effective. For example, hamsters required 400 to 700 times more ORF 3858 than did rats for uterotrophic and contraceptive activity. Furthermore, enormous doses of all but one of the “anti-estrogenic” compounds failed to antagonize the uterotrophic action of E2 or to impair fertility in hamsters. The data suggest that fertility may be inhibited in rats by administration of estrogens in highly uterotrophic doses or by treatment with compounds which antagonize the endogenous estrogen required for implantation and maintenance of pregnancy. In contrast, hamsters are less sensitive than rats to the contraceptive effects of estrogens and appear to respond minimally to compounds which are anti-estrogenic in rats.