Antiviral escin derivatives from the seeds of Aesculus turbinata Blume (Japanese horse chestnut)

Porcine epidemic diarrhea virus (PEDV) causes severe diarrhea and high fatality of piglets, influencing the swine industry. Japanese horse chestnut (seed of Aesculus turbinata) contains many saponin mixtures, called escins, and has been used for a long time as a traditional medicinal plant. Structure-activity relationship (SAR) studies on escins have revealed that acylations at C-21 and C-22 with angeloyl or tigloyl groups were important for their cytotoxic effects. However, the strong cytotoxicity of escins makes them hard to utilize for other diseases and to develop as nutraceuticals. In this research, we investigated whether escin derivatives 1–7 (including new compounds 2, 3, 5 and 6), without the angeloyl or tigloyl groups and with modified glycosidic linkages by hydrolysis, have PEDV inhibitory effects with less cytotoxicity. Compounds 1–7 had no cytotoxicity at 20 μM on VERO cells, while compounds 8–10 showed strong cytotoxicity at similar concentrations on PEDV. Our results suggest that escin derivatives showed strong inhibitory activities on PEDV replication with lowered cytotoxicity. These studies propose a method to utilize Japanese horse chestnut for treating PEDV and to increase the diversity of its bioactive compounds.     

Possible involvement of dopamine and dopamine2 receptors in the inhibitions of gastric emptying by escin Ib in mice

It was previously reported that escin Ib isolated from horse chestnut inhibited gastric emptying (GE) in mice, in which the capsaicin-sensitive sensory nerves (CPSN), the central nervous system and endogenous prostaglandins (PGs) were involved. In the present study, the possible involvement of dopamine and dopamine receptors in the inhibition of GE by escin Ib were investigated in mice. GE inhibition by escin Ib (25 mg/kg, p.o.) was attenuated after pretreatment with a single bolus of DL-alpha-methyl-p-tyrosine methyl ester (400 mg/kg, s.c., an inhibitor of tyrosine hydroxylase), reserpine (5 mg/kg, p.o., a catecholamine depletor), 6-hydroxydopamine (80 mg/kg, i.p., a dopamine depletor). Furthermore, pretreatment with spiperone (0.5-5 mg/kg, s.c., a dopamine2 receptor antagonist), haloperidol (0.5-10 mg/kg, s.c.) and metoclopramide (1-10 mg/kg, s.c.) (centrally acting dopamine2 receptor antagonists) attenuated the effect of escin Ib. Domperidone (0.1-5 mg/kg, s.c., a peripheral-acting dopamine2 antagonist) showed a weak attenuation, but SCH 23390 (1-5 mg/kg, s.c., a dopamine, receptor antagonist) did not. It is postulated that escin Ib inhibits GE, at least in part, mediated by CPSN, to stimulate the synthesis and/or release of dopamine, to act through central dopamine2 receptor, which in turn causes the release of PGs.     

石斛抗氧化活性研究进展

石斛作为传统的中药材,种类繁多,分布广泛,具有增强免疫力、抗氧化、抗肿瘤以及养阴生津等功效.抗氧化活性在石斛的药理功能中占据重要地位,能抑制活性氧对机体的损伤,延缓衰老,预防疾病,大量研究均围绕石斛这一特性展开.本文从抗氧化活性的石斛种、评价方法与有效成分及其作用机制三方面对石斛进行综述,以期为学者的相关研究提供最新参...     

树木形成层活动及其影响因素研究进展

树木生长是森林生态系统固碳的主要方式,树木生长过程受到气候与非气候因素的共同作用。树木径向生长长期定位监测是明确树木生长对气候变化响应的重要研究手段。本文对运用微树芯法的树木形成层活动及径向生长过程研究进行了总结。首先,综述了气候因素对树木形成层活动的影响: 寒冷湿润区温度决定树木生长开始和停止,干旱半干旱区水分和温度共同决定生长开始,水分决定生长停止;生长速率和持续时间共同决定生长量,最大生长速率出现在夏至前后;短期施氮并不能影响树木径向生长动态。其次,探讨了生物因素对树木径向生长过程的调控: 形成层活动开始时间因树种、树龄、竞争关系而有所差异;非结构性碳水化合物的季节动态与径向生长过程相耦合。最后,阐述了气候因素和生物因素交互作用下树木次生生长的响应机制。针对以上进展,本文提出了目前研究尚存在的问题并展望了未来的发展前景,以期为进一步的科学研究提供参考。     

植被活动对气候变化的响应过程研究进展

植被作为陆地生态系统的主体,在以增暖为主要特征的气候变化影响下,植被活动产生了动态的、非线性的响应规律,并体现出水热要素与植被活动多过程的交互作用和复杂影响机制,形成明显的区域分异特征。总结了温度升高和降水变动对植被活动影响研究进展,一定幅度的增温与增雨有利于植被活动增强,但许多研究认为升温超过3℃,或者降水变化50%,将会对植被活动造成不利影响,而其中的关键响应阈值与脆弱性机制仍不明晰;整合分析了气候多要素对植被活动的耦合效应,水、热、光等气候要素相互叠加共同影响植被活动过程,尤其是暖湿的气候组合对植被活动更为有利。综述了植被活动响应气候变化的区域差异性,及其对植被带分布产生的影响,如我国东北地区的植被活动对温度较为敏感,森林界线发生北移,而内蒙古西部地区则受到水分影响,草原有所退化。提出了今后应遵循"过程和格局耦合"思路,集成应用实验、统计和模型等多种方法,增强植被活动响应气候变化的空间分异规律研究。     

功能性壳寡糖的生物学活性

低分子量壳寡糖的生物学活性是最近的研究热点,诸多研究肯定了壳寡糖在抗肿瘤、神经退行性疾病、糖尿病和高血糖及抗氧化等领域的应用价值。壳寡糖的抗肿瘤作用依赖于免疫刺激;抗氧化作用与其分子结构中的羟基和氨基有关;神经保护作用与抗氧化损伤及抑制乙酰胆碱酯酶活性相关。另外,壳寡糖的生物相容性好等特点也暗示了其在药物研究和功能食品开发领域的应用价值。本文综述了壳寡糖在人类重大疾病防治领域的作用及作用机制的研究进展,探索了壳寡糖生物活性的研究方向。