A new C21 steroidal compound from the whole herb of Pachysandra terminalis Sieb. et Zucc

2020 ◽  
Vol 91 ◽  
pp. 104056
Author(s):  
Yangyang Zhang ◽  
Yuze Li ◽  
Yue Xu ◽  
Hao Fan ◽  
Wenli Huang ◽  
...  
Keyword(s):  
Steroidal Compound

Steroid Template Associated Peptides: Design, Synthesis and 2D NMR Characterization of a Novel Protected 18-Phe,19-Gly-Containing Steroidal Compound.

ChemInform ◽  
2007 ◽  
Vol 38 (51) ◽  
Author(s):  
Mira S. Bjelakovic ◽  
Natalija M. Krstic ◽  
Nenad Juranic ◽  
Milan M. Dabovic ◽  
Svetislav V. Gojkovic ◽  
...  
Keyword(s):  
2D Nmr ◽  
Design Synthesis ◽  
Nmr Characterization ◽  
Steroidal Compound

Cyclophenil, a non-steroidal compound with a higher central than peripheral oestrogenic activity: study of its effects on uterine growth and on some central parameters in castrated female rats

1984 ◽  
Vol 107 (3) ◽  
pp. 340-345 ◽  
Author(s):  
F. Celotti ◽  
N. Avogadri ◽  
R. C. Melcangi ◽  
S. Milani ◽  
P. Negri-Cesi
Keyword(s):  
Prolactin Secretion ◽  
The Other ◽  
Female Rats ◽  
Reliable Estimate ◽  
Growth Test ◽  
Oestradiol Benzoate ◽  
Enzymatic Systems ◽  
Uterine Growth ◽  
Steroidal Compound

Abstract. The oestrogenic activity of cyclophenil, a non-steroidal compound which has structural analogies with both stilbene and triphenylethylene, has been reevaluated utilizing both central and peripheral parameters. The central parameters considered were LH, FSH, prolactin secretion and two enzymatic systems known to be oestrogen-sensitive: hypophyseal 5α-reductase and hypothalamic aromatase. The uterine growth test was used to determine oestrogenic peripheral activity. The compound was administered at various doses in comparison with oestradiol benzoate (EB) to long-term castrated female rats. Cyclophenil has an activity 1/8110 times that of EB on uterine growth, and 1/1660 and 1/550 times that of EB in inhibiting LH and FSH. respectively. The hypophyseal 5α-reductase(expressed as DHT formation) was inhibited 1710 times less by cyclophenil than by EB. The other parameters considered were unsuitable to provide a statistically reliable estimate of the potency ratios between the two compounds. The data show that cyclophenil is an oestrogenic compound with peculiar characteristics. This substance is more effective in expressing its oestrogenic activity in central structures than in the peripheral ones.

Aromatase inhibitors in human breast cancer

1989 ◽  
Vol 95 ◽  
pp. 283-291 ◽  
Author(s):  
R. C. Coombes ◽  
R. C. Stein ◽  
M. Dowsett
Keyword(s):  
Breast Cancer ◽  
Aromatase Inhibitors ◽  
Overall Response Rate ◽  
Dose Schedule ◽  
Complete Regression ◽  
Human Breast ◽  
Irreversible Inhibitor ◽  
Clinical Toxicity ◽  
Clinical Responses ◽  
Steroidal Compound

SynopsisThe results of a phase I/II study in advanced breast cancer in postmenopausal women of the aromatase inhibitors 4-hydroxyandrostenedione (40HA), miconazole and CGS16949A are described. 40HA, a steroidal compound which is an irreversible inhibitor of aromatase, has been administered to 131 patients by weekly (500 mg) or fortnightly (250 mg) i.m. injections, and daily (500 mg) by mouth. The overall response rate (complete regression (CR) and partial regression (PR)) was 33%; all three dose schedules had similar clinical efficacy. Oestradiol levels were suppressed to a mean of 37–45% of pretreatment values with oral and with weekly i.m. 40HA; suppression was marginally suboptimal with 250 mg i.m. fortnightly. 40HA was well tolerated, especially when administered by fortnightly injections; this dose schedule is to be preferred to weekly injections.Significant oestradiol suppression and clinical responses did not occur with the imidazole antifungal, miconazole, which was administered to twenty-two patients at doses of 500–1000 mg daily. The non-steroidal aromatase inhibitor, CGS16949A, induced comparable oestradiol suppression to 40HA at doses of 0.6–4 mg daily; 0.6 mg daily appears to be suboptimal. Five of thirty-one patients treated had objective responses, and disease stabilised for at least six months in nine patients. Some suppression of aldosterone occurred with doses of 2 and 4 mg daily, but clinical toxicity of the compound was minor.

scholarly journals A review on the pharmaceutical activity of Solanum surattense

2021 ◽  
Vol 7 (3) ◽  
pp. 038-044
Author(s):  
Pradeep Kumar
Keyword(s):  
Ascorbic Acid ◽  
Medicinal Plants ◽  
Medicinal Plant ◽  
Molecular Level ◽  
Therapeutic Effects ◽  
Review Of The Literature ◽  
Solanum Surattense ◽  
Traditional Medicinal Plants ◽  
Pharmaceutical Activity ◽  
Steroidal Compound

The traditional medicinal plants are believed to be an impotent source of phytochemicals with potential therapeutic effects, and caring for different diseases. The plant Solanum surattense has active phytochemicals like saponins, alkaloid, phenols, solamargine, solasurine, solasonine, gum, ascorbic acid, sterols, torvoside K, torvoside L, khasianine, glycosides, flavonoids, aculeatiside A, solamargine, glycoalkaloid, steroidal compound, steroidal alkaloids, polyphenol (caffeic acid), coumarins (esculentin and aesculin), steroids (carpesterol, campesterol, daucosterol, stigmasterol, cycloortanol, and cholesterol), triterpinins, and sapogenin. This medicinal plant is widespread in pharmaceutics and still presents a large source of active phytochemicals with different activity such as antimicrobial, anti-larvicidal, anthelmintic, antimalarial, antioxidant, antidiabetic, anti-asthmatic, and anti-cancerous. This review of the literature revealed new researches on the phytochemicals of S. surattense that how the active phytochemicals are performed different activities on the molecular level in vital aspects.

scholarly journals Quantitative standardization of pharmacologically active components from antiplasmodial plant Solanum nudum Dunal (wild and in vitro)

2022 ◽  
Vol 21 (1) ◽  
pp. 41-50
Author(s):  
Ana Maria Mesa-Vanegas ◽  
◽  
Esther Julia Naranjo-Gomez ◽  
Felipe Cardona ◽  
Lucia Atehortua-Garces ◽  
...  
Keyword(s):  
Pacific Coast ◽  
Inhibitory Concentration ◽  
Quality Parameter ◽  
Antimalarial Treatment ◽  
Active Components ◽  
Steroidal Compound ◽  
Pharmacologically Active ◽  
Article Study ◽  
Over Time

Solanum nudum Dunal (Solanaceae) is most commonly known and used by the population of the colombian Pacific coast as an antimalarial treatment. This article study into optimization and quantitative analysis of compounds steroidal over time of development of this species when grown in vitro and wild. A new steroidal compound named SN6 was elucidated by NMR and a new method of quantification of seven steroidal compounds (Diosgenone DONA and six steroids SNs) using HPLC-DAD-MS in extracts of cultures in vitro and wild was investigated. Biology activity of extracts was found to a range of antiplasmodial activity in FCB2 and NF-54 with inhibitory concentration (IC50) between (17.04 -100 μg/mL) and cytotoxicity in U-937 of CC50 (7.18 -104.7 μg/mL). This method creates the basis for the detection of seven sterols antiplasmodial present in extracts from S. nudum plant as a quality parameter in the control and expression of phytochemicals.

VII. ON THE MECHANISM OF ANTI-ANDROGENIC ACTION OF 16β-ETHYL-17β-HYDROXY-4-OESTREN-3-ONE (TSAA-291)

1979 ◽  
Vol 92 (3_Supplb) ◽  
pp. S100-S107 ◽  
Author(s):  
Ryo Nakayama ◽  
Michio Masuoka ◽  
Kentaro Hiraga ◽  
Takuichi Miki
Keyword(s):  
Drug Design ◽  
Hydroxy Group ◽  
Steric Hindrance ◽  
Ventral Prostate ◽  
Complete Elimination ◽  
Structure Activity ◽  
Rat Ventral Prostate ◽  
Androgenic Activity ◽  
Drug Designing ◽  
Steroidal Compound

ABSTRACT The mechanism of anti-androgenic action of a steroidal compound, TSAA-291, was summarized and discussed in reference to its drug-designing and structure-activity relationship. The target of the drug-design was to obtain a substance which is inactive in androgenic activity and is capable of antagonistically competing with androgen for the receptor. With this intention, the androgen molecule was rendered with a steric hindrance influencing upon the functional 17β-hydroxy group. Introduction of a bulky group at the steroidal position-13 or -16 led to anti-androgenic properties. Intense steric hindrance by introducing an enormously bulky group or complete elimination of the 17β-hydroxy group rather decreased the anti-androgenic activity. Of these anti-androgens thus synthesized, TSAA-291 proved to be the most active in the anti-androgen assay and also antagonistic against the uptake of [3H]testosterone by the rat ventral prostate.

Tristar fenugreek

2007 ◽  
Vol 87 (4) ◽  
pp. 901-903 ◽  
Author(s):  
S. N. Acharya ◽  
S. Blade ◽  
Z. Mir ◽  
J. R. Moyer
Keyword(s):  
Seed Yield ◽  
Biomass Yield ◽  
Forage Yield ◽  
Research Centre ◽  
Attractive Alternative ◽  
Forage Legume ◽  
Short Term ◽  
Trigonella Foenum Graecum ◽  
Southern Alberta ◽  
Steroidal Compound

Tristar is an annual forage legume cultivar of fenugreek (Trigonella foenum-graceum). This cultivar was developed at the Agriculture and Agri-Food Canada (AAFC) Research Centre, Lethbridge, AB. Tristar biomass yield was 2 and 11% higher than the check cultivar Amber under dryland and irrigated conditions, respectively. This cultivar produced 26% more seed yield than Amber under irrigated condition in southern Alberta. Tristar will be an attractive alternative to alfalfa in short-term rotations as it produces as much biomass as two cuts of alfalfa and unlike alfalfa is bloat free and contains the steroidal compound diosgenin. Key words: Fenugreek, Trigonella foenum-graecum, annual legume, forage yield, forage quality

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