FL同时测定中药厚朴中厚朴酚与和厚朴酚含量

利用厚朴酚与和厚朴酚光酸性的不同,建立同时检测厚朴药材中这2种主要组分的荧光方法.通过对5份样品的测定发现,与色谱方法一样,甲醇提取液不需要进一步纯化处理,可以直接用于论文建立的荧光法对厚朴酚与和厚朴酚的测定.通过与HPLC方法的对照,证明荧光光谱法的精密度和准确度皆能满足分析要求.     

厚朴酚合成方法的改进研究

本实验中,将2,2＇-联苯二酚与1-溴丁烷经Williamson反应后,利用该反应产物溴化钠在酸性条件下与溴酸钠反应生成初生态的溴作为溴源,溴代反应得到5,5＇-二溴-2,2＇-二丁氧基联苯.中间产物5,5＇-二溴-2,2＇-二丁氧基联苯制成Grignard试剂后与烯丙基溴反应生成5,5＇-二烯丙基-2,2＇-二丁氧基...     

Semi-Synthesis and In Vitro Anti-Cancer Evaluation of Magnolol Derivatives

Magnolol (MAG), a biphenolic neolignan, has various biological activities including antitumor effects. In this study, 15 MAG derivatives were semi-synthesized and evaluated for their in vitro anticancer activities. From these derivatives, compound 6a exhibited the best cytotoxic activity against four human cancer cell lines, with IC₅₀ values ranging from 20.43 to 28.27 μM. Wound-healing and transwell assays showed that compound 6a significantly inhibited the migration and invasion of MDA-MB-231 cells. In addition, Western blotting experiments, performed using various concentrations of 6a, demonstrated that it downregulates the expression of HIF-1α, MMP-2, and MMP-9 in a concentration-dependent manner. Overall, these results suggest that substituting a benzyl group having F atoms substituted at the C2 position on MAG is a viable strategy for the structural optimization of MAG derivatives as anticancer agents.     

HPLC法研究三种皮类药材不同贮藏期药效成分的含量变化

目的 利用高效液相色谱法探究杜仲、厚朴和黄柏三种皮类药材不同贮藏期药效成分的含量变化。方法 分别采用回流、超声和闪式三种方式对同批贮存一年以及贮存五年的杜仲、厚朴和黄柏三种皮类药材进行提取,并利用高效液相色谱法对提取液中有效成分进行定量分析。结果 与贮藏期一年的药材相比,经过5年的贮存,三种皮类药材的药效物质含量均随着贮藏期延长或多或少的降低,其中杜仲皮中桃叶珊瑚苷的含量减少70%以上;厚朴皮中厚朴酚及和厚朴酚的含量减少1%以下;黄柏皮中盐酸小檗碱的含量减少10%以上。结论 三种皮类药材的药效物质在贮藏期变化总体有相似的规律,贮藏时间对杜仲皮皮中桃叶珊瑚苷的含量影响较大,对厚朴皮中厚朴酚与和厚朴酚的含量影响最小,而对黄柏皮中盐酸小檗碱的含量影响较小。研究结果为三种皮类药材的质量控制提供了科学依据。     

二阶导数同步荧光光谱法同时直接测定厚朴酚及和厚朴酚

研究了厚朴酚与和厚朴酚及其混合溶液的二阶导数同步荧光光谱,结果两者的二阶导数同步荧光光谱得到完全分离,消除了彼此间的干扰,据此建立了一种二阶导数同步荧光光谱法同时直接测定混合物中厚朴酚与和厚朴酚的新方法.厚朴酚与和厚朴酚的线性范围分别为2.8～500.0 μg/L和4.3～560.0 μg/L;检出限分别为0.84和1.30 μg/L,回收率分别为94.65%～105.58%和95.09%～104.51%; 相对标准偏差均低于4.08%.本方法用于同时直接测定厚朴药材及其提取物中厚朴酚与和厚朴酚含量,结果令人满意.     

新型厚朴酚2-甲亚胺衍生物的合成及其生物活性

以厚朴酚为原料,通过Reimer-Tiemann法,在其苯环羟基邻位引入甲酰基后,分别与甘氨酸、谷氨酸、精氨酸及对氨基苯磺酰胺反应合成了4个单取代、1个二取代新型厚朴酚2-甲亚胺衍生物(3a~3d和4),其结构经UV-Vis, ¹H NMR, IR, MS和元素分析表征。生物活性研究结果表明： 2-(N-甘氨酸)-厚朴酚甲亚胺(3a)对成肌细胞的毒性较大;2-［N-(4-氨磺酰苯基)］-厚朴酚甲亚胺(3d)浓度为64 μmol·L^-1时,对CYP2D6和CYP1A2的抑制率分别为42.9%和36.8%。     

吐温-80和脂质体对厚朴酚荧光光谱的影响

分析厚朴酚在吐温-80胶束和脂质体溶液中荧光光谱的变化,发现：1）浓度为2mmol·L^-1的吐温-80胶束对厚朴酚有荧光增敏作用,厚朴酚存在于吐温-80的疏水核中,其荧光光谱发生了明显的红移;2）在4mg·mL^-1的脂质体溶液中,厚朴酚的荧光光谱变得复杂,谱图信息反映厚朴酚同时存在于水相和双脂层膜相中,且在二者之间存在分配平衡,通过测定λ365、λ397处的荧光光谱随厚朴酚浓度的变化,得到了厚朴酚在脂质体膜相和水相中的分配平衡关系;3）脂质体溶液中加入吐温-80,厚朴酚在双脂层膜相中的分布增加,其荧光光谱发生了红移．     

厚朴果实中厚朴酚、和厚朴酚的提取工艺比较

目的：测定厚朴果实中厚朴酚、和厚朴酚的含量,并对厚朴果实中酚类成分的提取方法进行探索和优化,为厚朴果实入药提供依据和参考。方法用醇提法、碱提法和超声辅助提取法提取厚朴果实中的酚类成分,采用薄层扫描法测定其中的厚朴酚、和厚朴酚的含量;并采用控制单一变量法优化乙醇提取工艺。结果厚朴果实中两种酚的含量是厚朴皮的1/4左右,提示厚朴果实具有入药的潜性;乙醇提取法的工艺优化结果显示最佳提取参数是60℃下、80%体积的乙醇提取三次（2、1.5、1 h）。结论醇提法、碱提法和超声提取法对酚类物质提取率没有显著影响,提示在选择提取方法时我们可以根据实际情况和成本来选择恰当的提取方法。     

Magnolol as a Potential Anticancer Agent: A Proposed Mechanistic Insight

Cancer is a serious disease with high mortality and morbidity worldwide. Natural products have served as a major source for developing new anticancer drugs during recent decades. Magnolol, a representative natural phenolic lignan isolated from Magnolia officinali, has attracted considerable attention for its anticancer properties in recent years. Accumulating preclinical studies have demonstrated the tremendous therapeutic potential of magnolol via a wide range of pharmacological mechanisms against cancer. In this review, we summarized the latest advances in preclinical studies investigating anticancer properties of magnolol and described the important signaling pathways explaining its underlying mechanisms. Magnolol was capable of inhibiting cancer growth and metastasis against various cancer types. Magnolol exerted anticancer effects through inhibiting proliferation, inducing cell cycle arrest, provoking apoptosis, restraining migration and invasion, and suppressing angiogenesis. Multiple signaling pathways were also involved in the pharmacological actions of magnolol against cancer, such as PI3K/Akt/mTOR signaling, MAPK signaling and NF-κB signaling. Based on this existing evidence summarized in the review, we have conclusively confirmed magnolol had a multi-target anticancer effect against heterogeneous cancer disease. It is promising to develop magnolol as a drug candidate for cancer therapy in the future.     

厚朴酚的提取及分析方法

厚朴酚是中药材厚朴的主要有效成分,具有抗菌、抗焦虑、抗抑郁等广泛药理作用,受到化学研究者的广泛关注.用索氏提取法、快速溶剂萃取法、超临界CO2萃取法、超声提取法等提取方法以及紫外分光光度法、荧光分光光度法、高效液相色谱法分析方法进行研究.研究认为厚朴酚具有抗菌、抗病毒、抗氧化、抗肿瘤、抗哮喘等多种药理学作用药理作用,并将日益引起国内外的广泛重视.要使厚朴酚的药理作用更加体现出,那么厚朴酚的厚朴酚的提取、分析方法也就不是只需要一种方法就能独立完成,需要多种方法相互结合使用,既使生产经济又能保证厚朴酚的天然无污染.通过有进一步研究,能够寻找更加完善的新技术,使厚朴酚在临床、制药、化妆品等方面得到更好的应用.