苹果短枝型品种叶片脱落酸含量的研究

苹果短枝型品种叶片脱落酸含量的研究牛自勉，房耀仁（山西省农科院果树所，太谷０３０８００）（北京林业大学，北京１０００８３）ＳＴＤＤＹＯＮＴＨＥＡＢＳＣＩＳＩＣＡＣＩＤＩＮＬＥＡＦＯＦＳＰＵＲ－ＴＹＰＥＶＡＲＩＥＴＹＯＦＡＰＰＬＥ￥ＮｉｕＺｉ－ｍｉａｎ...     

杉木人工林取代天然次生阔叶林对土壤生物活性的影响

对我国亚热带南、中、北3个区带杉木人工林与天然次生阔叶林表层土壤化学性状、土壤生物活性特征进行研究.结果表明,杉木人工林取代天然次生林阔叶林后表层土壤总有机碳含量下降31.51%～58.24%,土壤全氮、全磷、pH值以及土壤C/N、C/P比亦呈下降趋势;杉木人工林取代天然次生阔叶林后表层土壤细菌、真菌数量减少;土壤脲酶、蔗糖酶、过氧化氢酶和脱氢酶活性下降,而土壤多酚氧化酶活性增加8%～40%;杉木人工林与天然次生林阔叶林相比,土壤呼吸强度下降51.15%～54.48%.相关分析发现,土壤总有机碳与土壤多酚氧化酶活性呈负相关(R=-0.723,n=18),与土壤全氮、全磷及其它土壤酶活性呈正相关.杉木人工林取代天然次生林阔叶林使林内表层土壤质量恶化.杉木人工林土壤有机质丢失是导致杉木人工林土壤养分减少、土壤生物活性下降的重要原因.     

植物多糖的凹形结构与生物活性关系

简述了植物多糖的生物活性与结构 ,讨论了植物多糖的生物活性与结构的关系 ,提出了凹形结构是多糖产生生物活性的基础     

非天然氨基酸及非天然蛋白合成的研究进展

非天然氨基酸是天然氨基酸的衍生物,其具有重要的生理和药理功能.由非天然氨基酸合成的非天然蛋白同样具有特别的功能与活性.非天然氨基酸插入蛋白质中的研究为新型生物材料和蛋白质药物等的合成和应用提供了新的指导方向.基于此,本文综述了非天然氨基酸的生物合成方法,分析了非天然氨基酸生物合成目前存在的难点,总结了非天然氨基酸插入蛋...     

抗单纯疱疹病毒的天然产物研究现况

单纯疱疹病毒(HSV)是一种发病率极高,在全世界分布广泛的疱疹病毒,易引起多种人类皮肤疾病,严重危害人类的身体健康和生命安全。目前临床上常用核苷类抗病毒药物对单纯疱疹病毒感染进行治疗,但存在着许多明显的缺点,如：生物利用度低,溶解度小,临床多见不良反应且容易导致病毒耐药等。与核苷抗病毒药物相比,天然产物具有作用时间长、低毒、病毒不易产生耐药性等显著优点。随着对天然产物研究的深入,大量研究和实验证明：从植物或动物中提取的天然产物对于单纯疱疹病毒感染的治疗有着广阔的前景,天然产物成了寻找新型抗疱疹病毒药物的重要来源。将对近年来天然产物抗HSV研究状况进行整理、总结和分析,为将来天然产物抗HSV感染研究提供参考和对比。     

具有生物活性的天然三萜化合物的研究进展

三萜类化合物是广泛存在于自然界的一类有机化合物,其中很多具有一定的生物活性。该文着重综述了近五年来具有抗炎、抗菌、抗肿瘤生物活性的天然游离三萜化合物的研究进展。     

生物转化对天然药物进行结构修饰的研究进展

利用生物转化对天然药物进行结构修饰,是筛选活性化合物的有效途径之一。本文根据生物体系中酶的多样性和特异性以及生物转化具有副产物少、选择性和专一性强等特点,系统性的综述了近几年来在天然药物资源开发利用研究中生物转化进行结构修饰的常见反应类型:羟基化、糖基化、水解和环氧化反应等,并简述了生物转化法在开发具有活性的新药物和改变天然药物活性如改变细胞毒性、增强抗耐药性、减小毒副作用或提高生物利用率等方面的实际应用。     

天然多糖羧甲基化对其生物活性影响的研究进展

多糖由于具有抗氧化、抗肿瘤、调节免疫、降血糖等生物活性而受到诸多领域的关注。多糖的结构与其生物活性相关,经过化学修饰会增强其生物活性或产生新的活性。本文就天然多糖的羧甲基化修饰及对其生物活性的影响进行综述,以期为多糖的研发与应用提供理论参考。     

Synthesis of (R)- and (S)- muscone

(R)-(-)-Muscone (3-methylcyclopentadecanone, 1) the key perfumery component isolated from the male musk deer, Moschus moschiferus,* was synthesized from the easily available chiral building block, (R)-3-tert-butoxycarbonyl-2-methylpropanoic acid (2), by employing ring-closing olefin metathesis (RCM). Antipode (+)-1 was also synthesized in a similar manner from tert-butyl (S)-3-methoxycarbonylbutanoate (10). *(a) Walbaum, H. J. J. Prakt. Chem., 73, 488 (1906); (b) Ruzicka, L., Further considerations on the constitution of muscone. Helv. Chim. Acta, 9, 715, 1008-1017 (1926).     

Facile entry to (-)-(R)- and (+)-(S)-mexiletine

The title compounds, 1a and 1b, have been synthesized in a three-step sequence starting from (-)-(S) and (+)-(R)-propylene oxide, respectively, in acceptable overall yields. The enantiomeric excess values for 1a and 1b were 96% and 93% respectively, as assessed by HPLC analysis on a chiral stationary phase of the corresponding N-acetyl derivatives. The synthetic route herein presented may represent a facile entry to highly enriched mexiletine enantiomers, alternative to those previously reported in the literature.     

Synthesis and antioxidant evaluation of (S,S)- and (R,R)-secoisolariciresinol diglucosides (SDGs)

Secoisolariciresinol diglucosides (SDGs) (S,S)-SDG-1 (major isomer in flaxseed) and (R,R)-SDG-2 (minor isomer in flaxseed) were synthesized from vanillin via secoisolariciresinol (6) and glucosyl donor 7 through a concise route that involved chromatographic separation of diastereomeric diglucoside derivatives (S,S)-8 and (R,R)-9. Synthetic (S,S)-SDG-1 and (R,R)-SDG-2 exhibited potent antioxidant properties (EC₅₀ = 292.17 ± 27.71 μM and 331.94 ± 21.21 μM, respectively), which compared well with that of natural (S,S)-SDG-1 (EC₅₀ = 275.24 ± 13.15 μM). These values are significantly lower than those of ascorbic acid (EC₅₀ = 1129.32 ± 88.79 μM) and α-tocopherol (EC₅₀ = 944.62 ± 148.00 μM). Compounds (S,S)-SDG-1 and (R,R)-SDG-2 also demonstrated powerful scavenging activities against hydroxyl [natural (S,S)-SDG-1: 3.68 ± 0.27; synthetic (S,S)-SDG-1: 2.09 ± 0.16; synthetic (R,R)-SDG-2: 1.96 ± 0.27], peroxyl [natural (S,S)-SDG-1: 2.55 ± 0.11; synthetic (S,S)-SDG-1: 2.20 ± 0.10; synthetic (R,R)-SDG-2: 3.03 ± 0.04] and DPPH [natural (S,S)-SDG-1: EC₅₀ = 83.94 ± 2.80 μM; synthetic (S,S)-SDG-1: EC₅₀ = 157.54 ± 21.30 μM; synthetic (R,R)-SDG-2: EC₅₀ = 123.63 ± 8.67 μM] radicals. These results confirm previous studies with naturally occurring (S,S)-SDG-1 and establish both (S,S)-SDG-1 and (R,R)-SDG-2 as potent antioxidants and free radical scavengers for potential in vivo use.     

Efficient synthesis of the ketone body ester (R)-3-hydroxybutyryl-(R)-3-hydroxybutyrate and its (S,S) enantiomer

The ketone body ester (R)-3-hydroxybutyryl-(R)-3-hydroxybutyrate and its (S,S) enantiomer were prepared in a short, operationally simple synthetic sequence from racemic β-butyrolactone. Enantioselective hydrolysis of β-butyrolactone with immobilized Candida antarctica lipase-B (CAL-B) results in (R)-β-butyrolactone and (S)-β-hydroxybutyric acid, which are easily converted to (R) or (S)-ethyl-3-hydroxybutyrate and reduced to (R) or (S)-1,3 butanediol. Either enantiomer of ethyl-3-hydroxybutyrate and 1,3 butanediol are then coupled, again using CAL-B, to produce the ketone body ester product. This is an efficient, scalable, atom-economic, chromatography-free, and low cost synthetic method to produce the ketone body esters.     

Practical access to the proline analogs (S,S,S)- and (R,R,R)-2-methyloctahydroindole-2-carboxylic acids by HPLC enantioseparation

An efficient methodology for the preparation of the α‐tetrasubstituted proline analog (S,S,S)‐2‐methyloctahydroindole‐2‐carboxylic acid, (S,S,S)‐(αMe)Oic, and its enantiomer, (R,R,R)‐(αMe)Oic, has been developed. Starting from easily available substrates and through simple transformations, a racemic precursor has been synthesized in excellent yield and further subjected to HPLC resolution using a cellulose‐derived chiral stationary phase. Specifically, a semipreparative (250 mm × 20 mm ID) Chiralpak® IC column has allowed the efficient resolution of more than 4 g of racemate using a mixture of n‐hexane/tert‐butyl methyl ether/2‐propanol as the eluent. Multigram quantities of the target amino acids have been isolated in enantiomerically pure form and suitably protected for incorporation into peptides. Chirality, 2011. © 2011 Wiley‐Liss, Inc.     

Synthesis and biochemical evaluation of highly enantiomerically pure (R,R)- and (S,S)-alexidine

Alexidine is in everyday human use as oral disinfectant and contact lens disinfectant. It is used as a mixture of stereoisomers. Since all of alexidine’s known biological targets are chiral, the biological activity of any of its chiral stereoisomers could be significantly higher than that of the mixture of stereoisomers. This makes a synthetic methodology for obtaining the individual enantiomers of the chiral diastereoisomer highly desirable. Here, we describe the first synthesis of both enantiomers of alexidine in high enantiomeric purity, and demonstrate their activity against the protein–protein interaction between the anti-apoptotic protein Bcl-x_L and the pro-apoptotic protein Bak.     

Total synthesis of (R,R,R)- and (S,S,S)-schweinfurthin F: differences of bioactivity in the enantiomeric series

Total synthesis of the (R,R,R)- and (S,S,S)-enantiomers of the natural product schweinfurthin F has been completed. Comparisons of spectral data and optical rotations with those reported for the natural product, as well as a variety of bioassay data, allow assignment of the natural material as the (R,R,R)-isomer.     

A useful route to (R)- and (S)-tert-leucine

Resolution of 1-(2-furyl)-2,2-dimethylpropylamine, an intermediate on a synthetic route to tert-leucine, followed by oxidation of the respective enantiomers, constitutes an interesting and useful strategy to (R)- and (S)-tert-leucine.     

Stereoselective effects of (R)- and (S)-carvedilol in humans

Carvedilol is currently used as the racemic mixture, (R,S)-carvedilol, consisting of equal amounts of (R)-carvedilol, an alpha-blocker, and (S)-carvedilol, an alpha- and beta-blocker, which have never been tested in their optically pure forms in human subjects. We performed a randomized, double-blind, placebo-controlled, crossover study in 12 healthy male volunteers. Subjects received single oral doses of 25 mg (R,S)-carvedilol, 12.5 mg (R)-carvedilol, 12.5 mg (S)-carvedilol, and placebo at 8 AM as well as at 8 PM. Exercise was performed at 11 AM, and heart rate and blood pressure were measured at rest and after 10 min of exercise. Urine was collected between 10 AM and 6 PM, as well as between 10 PM and 6 AM, and the amounts of urinary 6-hydroxy-melatonin sulfate (aMT6s) were determined by RIA. Compared to placebo, (R)-carvedilol increased heart rate during exercise (+4%, P < 0.05) and recovery (+10%, P < 0.05); (S)-carvedilol decreased heart rate during exercise (-14%, P < 0.05) and recovery (-6%, P < 0.05), and systolic blood pressure during exercise (-12%, P < 0.05); (R,S)-carvedilol decreased heart rate during exercise (-11%, P < 0.05), and systolic blood pressure at rest (-7%, P < 0.05) and during exercise (-10%, P < 0.05). None of the agents had any significant effect on the release of aMT6s. Our results indicate that only (S)-carvedilol causes beta-blockade, whereas (R)-carvedilol appears to increase sympathetic tone, presumably as a physiological reaction to the decrease of blood pressure caused by alpha-blockade. None of the drugs had any influence on melatonin release. The weak clinical net effect of beta-blockade of (R,S)-carvedilol at rest might be one reason why this drug causes fewer side effects than other beta-blockers, such as a reduction of nocturnal melatonin release.     

Synthesis of (3R,10R)- and (3S,10S)-Diastereomers of 3,10-Dimethylspermine

Russian Journal of Bioorganic Chemistry - A simple and practical 10-step synthesis is reported for previously unknown diastereomers of C?methylated spermine (Spm) analogue,...