New Sesquiterpenes from Ferula jaeschkeana

Phytochemical studies of the FERULA JAESCHKEANA rhizomes resulted in the isolation of two new carotane sesquiterpenes; feruone and the 5alpha-( P-hydroxybenzyl)ester of ferutriol.     

Contraceptive and Hormonal Properties of Achyranthes aspera in Rats and Hamsters1.

N-Butanol fraction of aerial parts of ACHYRANTHES ASPERA Linn. prevented pregnancy in adult female rats when administered orally at 75 mg/kg dose on days 1-5 POST-COITUM, but was ineffective in hamsters upto 300 mg/kg dose. In ovariectomized immature female rats, the extract exhibited potent estrogenic activity at the contraceptive dose but was devoid of any antiestrogenic activity. 100% uterine weight gain was achieved at 1/15th of the contraceptive dose. Significant uterotrophic effect was discerned even at 1/20th of the contraceptive dose. Taking 100% increase in uterine weight as the parameter, estrogenic activity of the extract was found to be 1/2750 that of ethynylestradiol.     

Dihydroayapin,a New Coumarin Compound from Dendrobium Densiflorum

Abstract

A new coumarin named dihydroayapin (1) together with seven known compounds were isolated from the stems of Dendrobium densiflorum. On the basis of physicochemical and spectral evidences, the structure of 1 was established as 6,7-methylenedioxy-3,4-dihydrobenzopyran-2-one.     

New sesquiterpene coumarins from the roots of Ferula flabelliloba

Three new sesquiterpene coumarins, namely, farnesiferone B (1), flabellilobin A (2) and flabellilobin B (3), together with nine known compounds, ligupersin A, 7-epi-gamma-eudesmol, persicasulfide A, conferdione, umbelliprenin, conferone, feselol, lehmferin and farnesiferol B were isolated from the roots of Ferula flabelliloba Rech. f. & Aell. (Apiaceae). The structures of these compounds were elucidated by various 1- and 2-D NMR techniques as well as HREIMS.     

Contraceptive agents from cycloaddition reactions of diarylcyclopropenones and diarylthiirene 1, 1-dioxides.

The potential for compounds with antifertility activity from the reactions of diphenylcyclopropernone (1) and 2, 3-diphenylthiirene 1, 1-dioxide (2) with enamines is described. In certain instances, a marked dissociation of antifertility from estrogenic activity was possible. Two series were studied extensively, one was stilbene amides (7) and the other stilbene amino ketones (8). The latter series (8) afforded several materials from which, on further biological work-up, was singled out compound 21 as a potent antifertility agent in rats and hamsters.     

Effect of ultrasound on extraction and stability of polyphenols from Berberis jaeschkeana C.K. Schneid fruits: A comparative study

The extraction of bioactive compounds from plant sources has always posed the question of stability, which largely depends on the extraction conditions. This study is, therefore, designed to evaluate the stability of polyphenolics from Berberis jaeschkeana fruit extracted under optimal ultrasonic-assisted extraction (UAE) conditions, and make comparisons with conventional extraction (CE). Ultrasonic temperature, solvent concentration and sample-to-solvent ratio were found to significantly affect the extraction yield. Under the optimal UAE conditions, significantly higher polyphenolic contents and antioxidant activity were recorded than CE. The stability of polyphenols varied in UAE and CE conditions, and compounds, such as rutin, vanillic acid, 3-hydroxybenzoic acid and trans cinnamic acid, showed higher stability under UAE, while caffeic, chlorogenic, p-coumaric and 4-hydroxybenzoic acid were completely degraded under ultrasonication. The results revealed that the stability of polyphenolic compounds under UAE depend on the physio-chemical properties of the individual polyphenolic compounds, extraction type and process factors.     

The Estrogen Activity of the Sum of Terpenoid Alcohol Esters Isolated from Ferula kuhistanica and Ferula Tenuifida

Pharmaceutical Chemistry Journal -     

Coumarin incorporated triazoles: a new class of anticonvulsants

A series of coumarin incorporated 1,2,4- triazole compounds (1-14) were evaluated for their possible anticonvulsant and neurotoxic properties, log P values, pharmacophoric mapping and three dimensional structure analysis. Compound (6) with para-fluoro substitution showed significant anticonvulsant activity.     

复方左炔诺孕酮片避孕有效性与安全性的Meta分析

目的 系统评价复方左炔诺孕酮片——左炔诺孕酮/炔雌醇100/20 μg（levonorgestrel/ethinyl estradiol 100/20 μg,LNG/EE 100/20 μg）避孕的有效性及安全性。方法 计算机检索中国知网、维普、万方、Pubmed、Web of science、EMbase以及Cochrane图书馆等数据库,査找有关复方左炔诺孕酮片（LNG/EE 100/20 μg）用于避孕的随机对照试验（RCT）,检索时间均从建库至2015年8月30日。对资料进行数据提取和质量评价,釆用RevMan 5.3软件进行Meta分析。结果 纳入7项研究,共1 786例患者。Meta分析结果显示,与复方左炔诺孕酮片（LNG/EE 150/30 μg）等几个复方口服避孕药相比,复方左炔诺孕酮片（LNG/EE 100/20 μg）在避孕有效率[OR=1.08,95% CI（0.29,4.04）,P=0.91]和不良事件发生率[OR=0.99,95% CI（0.81,1.21）,P=0.92]方面差异均无统计学意义,周期控制有效率差异有统计学意义[OR=1.75,95% CI（1.28,2.38）,P=0.000 4],复方左炔诺孕酮片（LNG/EE 100/20 μg）对周期控制的效果更优。结论 根据现有的临床数据,复方左炔诺孕酮片（LNG/EE 100/20 μg）避孕有效率与不良事件发生率与复方左炔诺孕酮片（LNG/EE 150/30 μg）等几个复方口服避孕药相当,而周期控制有效率效果明显。由于纳入的随机对照试验样本量小,部分文献质量偏低,本评价结果还需通过严格设计的大样本临床试验加以验证。     

Controlled Release of a Contraceptive Steroid from Biodegradable and Injectable Gel Formulations: In Vitro Evaluation

Purpose. The purpose of this study was to investigate the effects of formulation factors including varying wax concentration, drug loading and drug particle size, on drug release characteristics from both pure oil and gel formulations prepared with a combination of derivatized vegetable oil (Labrafil 1944 CS) and glyceryl palmitostearate (Precirol ATO 5), using levonorgestrel as a model drug. Methods. The effects of varying drug loadings, different drug particle sizes, and wax (Precirol) concentrations on in-vitro drug release rates were evaluated, and the mechanisms of drug release from the gels were determined. Results. Zero-order drug release rates from the 10% Precirol gel formulations containing 0.25, 0.50 and 2.00% w/v drug loadings were lower than those observed for oil formulations containing identical drug loadings. Higher zero-order release rates were observed from formulations containing smaller drug particles suspended in both oil and gel formulations. The mechanism of drug release from gels containing less than 0.25% w/w drug was diffusion-controlled. Increasing the wax concentrations in the gels from 5% w/w to 20% w/w significantly decreased the diffusivity of the drug through the gel formulations and markedly increased the force required to inject the gels from two different sizes of needles. Conclusions. This study shows how modification of the physicochemical properties of the gel formulations by changing the drug particle size, wax concentration and drug loading, affects drug release characteristics from the system.     

Letter: Contraceptive practice and unplanned pregnancy in students.

The conclusion from a study of Australian university students that the proportion of university women experiencing sexual intercourse and the proportion of sexually active university women using contraceptives were greater than that found in Britain and America is challenged from the British experience. In Cambridge, England, the proportion of sexually experience undergraduate and secretarial female students was 57%, compared with 62% in the Australian study. When analyzed by age, the Australian study indicated that 15% of the women had engaged in sexual congress by the age of 16, and 95% had done so by the age of 19. These figures approximated those for non-university students in Britain. However, 89% of the British undergraduates and 72% of non-university students had used a reliable method of contraception on every occasion of sexual intercourse, compared with 49% in the Australian study. Also, 74% of the British undergraduates used oral contraceptives (OC), while only 30% used OCs in the Australian study. Nonetheless, only 60% of the experienced British women and 35% of the men felt that contraceptive advice was adequately available. Apprehension that OCs are regarded as the only reliable method of contraception available is expressed in light of circumstances in which OCs may not be suitable or available.     

Acute toxicity of ferulenol, a 4-hydroxycoumarin isolated from Ferula communis L

The acute LD50s of ferulenol were determined in albino mice by single po or ip as 2,100 and 319 mg/kg bw, respectively. Ferulenol had a higher LD50 compared to warfarin and thus has a lower acute toxicity. Three days after ferulenol administration, dosed animals showed hypoprothrombinemia with internal and external hemorrhages similar to those described in ferulosys and anti-vitamin K experimental poisonings. Male mice were more sensitive to intoxication by ferulenol than were females.     

Identification of Isocoumarin and Coumarin from Leaves of Hydrangea Macrophylla

目的 研究八仙花叶的化学成分.方法 采用多种色谱方法(硅胶柱色谱﹑ODS柱色谱和HPLC柱色谱)分离纯化,依据理化性质、波谱数据分析进行结构鉴定.结果 从八仙花叶中分离得到 2个异香豆素和3个香豆素类化合物,分别鉴定为①绣球酚,②绣球酚-4′-O-β-D-葡萄糖苷,③7-羟基香豆素,④香豆素-7-O-β-D-葡萄糖苷,⑤8-甲氧基香豆素-7-O-β-D-葡萄糖苷.结论 本文为八仙花的进一步研究提供有效的物质基础,并首次报导了绣球酚的光谱数据,为其活性的深入研究提供了保证.     

八仙花叶中异香豆素和香豆素成分的结构鉴定

目的研究八仙花叶的化学成分。方法采用多种色谱方法(硅胶柱色谱﹑ODS柱色谱和HPLC柱色谱)分离纯化,依据理化性质、波谱数据分析进行结构鉴定。结果从八仙花叶中分离得到2个异香豆素和3个香豆素类化合物,分别鉴定为①绣球酚,②绣球酚-4’-O-β-D-葡萄糖苷,③7-羟基香豆素,④香豆素-7-O-β-D-葡萄糖苷,⑤8-甲氧基香豆素-7-O-β-D-葡萄糖苷。结论本文为八仙花的进一步研究提供有效的物质基础,并首次报导了绣球酚的光谱数据,为其活性的深入研究提供了保证。     

A New Non-Glycosidic Iridoid and a New Bisiridoid from Argylia radiata1

From ARGYLIA RADIATA a non-glycosidic iridoid, the (4a S, 7 S, 7a S)-7-hydroxy-7-methyl-1,4a,5,6,7,7a-heptahydrocyclopenta[ C]pyran-3(4 H)-one, and a bisiridoid, derived from the junction of catalpol and 7-deoxyloganic acid, were isolated.     

Efficacy and tolerability of intramuscular interferon beta-1a compared with subcutaneous interferon beta-1a in relapsing MS: results from PROOF

ABSTRACT

Objective: Benefits from interferon beta (IFNβ) treatment in patients with multiple sclerosis are affected by many factors, including sustained clinical efficacy, acceptable tolerability, adherence to therapy, and the development of neutralizing antibodies (NAbs). The Prospective and Retrospective Long-Term Observational Study of Avonex and Rebif (PROOF) was designed to compare the relative efficacy and tolerability of the two IFNβ-1a products for up to 5 years.

Methods: PROOF compared the relative efficacy and tolerability of intramuscular (IM) IFNβ-1a (Avonex) 30?µg once weekly (n= 69) and subcutaneous (SC) IFNβ-1a (Rebif) 44?µg three times per week (n= 67). The duration of the retrospective portion of the study was 12–24 months. Due to slow enrollment, PROOF ended earlier than planned and the final duration of the prospective portion of the study was 6 months. Therefore, between 18 and 30?months of efficacy and tolerability data were available for analysis.

Results: After controlling for baseline disability level, Expanded Disability Status Scale (EDSS) scores revealed no statistically significant differences between the treatment groups during the prospective portion of the study, with sustained disability progression similar in both groups (25.8% IM IFNβ-1a 30?µg once weekly vs. 26.7% SC IFNβ-1a 44?µg three times per week). Relapse rates were similar in the groups, as were MRI endpoints of brain parenchymal fraction, T1 lesion volume, T2 lesion volume, number of new/enlarging T2 lesions, and gadolinium-enhancing (Gd+) lesion volume and count. Treatment groups differed in frequency of NAbs, with 19% of patients treated with SC IFNβ-1a 44?µg three times per week NAb+ compared with none treated with IM IFNβ-1a 30?µg once weekly. More NAb+ patients compared with NAb– patients had disability progression (40.0% vs. 27.8%, p= NS), new or enlarging T2 lesions at the end of treatment (63.6% vs. 40.7%, p= 0.003), and Gd+ lesions after 12–24 months of treatment (36.4% vs. 15%, p= 0.001). The IFNβ-1a products had comparable tolerability. However, fewer patients treated with IM IFNβ-1a 30?µg once weekly had injection-site reactions (2.9% vs. 6.0%). Limitations of this study include its design and sample size, both of which hinder detection of differences in efficacy between IFNβ-1a treatments.

Conclusions: The results of the present study show that the two IFNβ-1a products have comparable efficacy and differing immunogenicity.