黄花倒水莲化学成分研究

目的：对民族药黄花倒水莲(Polygala fallax HemsI．)的化学成分进行研究。方法：采用MeOH提取，经EtOAc萃取，用柱色谱分离纯化，通过波谱方法鉴定化合物结构。结果：鉴定了8个化合物：1-羟基-2,4-二甲氧基Shan酮(I)，1，2，3-三甲氧基Shan酮(Ⅱ)，1-甲氧基-2，3-亚甲二氧基Shan酮(Ⅲ)，1，7-二羟基-2，3-亚甲二氧基Shan酮(Ⅳ)，6-羟基-1-甲氧基-2，3-亚甲二氧基Shan酮(V)，常春藤皂苷元(Ⅵ)，豆甾醇(Ⅶ)，β-谷甾醇(Ⅷ)。结论：化合物I是新天然产物，化合物V是新化合物，鉴定的8个化合物均为首次从黄花倒水莲中获得。     

(口山)酮对老年小鼠抗氧化酶活性的影响

目的:探讨从穿心草中提取的三种黄酮类化合物(咄)酮(Xanthone,Xan) 对老年小鼠体内抗氧化酶活性的影响.方法:连续20天腹腔注射0.2μmol/L和0.02μmol/L的三种Xan,测定体内超氧化物歧化酶、谷胱甘过氧化物酶和过氧化氢酶的活性.结果:三种Xan均能不同程度地增加老年小鼠体内多种抗氧化酶的含量,作用强度依次为Xan-Ⅰ>Xan-Ⅲ>Xan-Ⅱ.结论:三种Xan对老年小鼠体内抗氧化酶的活性有不同程度的影响,提示Xan对机体的保护作用与其清除氧自由基、提高抗氧化酶的活性有关.     

远志的化学成分研究Ⅲ

目的：研究远志益智安神的有效成分，为开发治疗老年痴呆症的新药及远志的质量控制奠定基础。方法：采用硅胶柱层析和Sephadex LH-20进行纯化，通过各种光谱数据进行结构鉴定。结果：从远志根皮95％乙醇提取物的石油醚萃取物和氯仿萃取物中分离得到了9个化合物，分别鉴定为α-菠甾醇葡萄糖苷(I)，α-菠甾醇葡萄糖苷-6’-0-棕榈酸酯(Ⅱ)，豆甾醇(Ⅲ)，(28Z)-三十四碳烯酸(Ⅳ)，1，7-dimethoxy-2，3-methylenedioxyxanthone(V)，1，2，3，6，7-pentamethoxyxanthone(VI)，1，2，3，7-tetramethoxyxanthone(Ⅶ)，1，3，7-trihydroxyxanthone(Ⅷ)和1，6，7-trihydroxy-2，3-dimethoxyxanthone(IX)。结论：化合物Ⅳ新化合物，化合物I、Ⅱ和Ⅷ为首次从远志属植物中分离得到，化合物Ⅲ和Ⅸ为首次从远志植物中分离得到。     

Xanthone suppresses allergic contact dermatitis in vitro and in vivo

Xanthone is a phenolic compound found in a few higher plant families; it has a variety of biological activities, including antioxidant, anti-inflammatory, and anticancer properties. However, the molecular and cellular mechanisms underlying the activity of xanthone in allergic contact dermatitis (ACD) remain to be explored. Therefore, this study aimed to investigate the regulatory effects of xanthone in ACD in human keratinocytes (HaCaT cell), and human mast cell line (HMC-1 cell) in vitro and in an experimental murine model. The results demonstrated that treatment with xanthone reduced the production of pro-inflammatory cytokines and chemokines including interleukin (IL)-1β, IL-6, IL-8, and expression of chemokines thymus and activation-regulated chemokine (TARC) and macrophage-derived chemokine (MDC) in tumor necrosis factor (TNF)-α and interferon (IFN)-γ-stimulated HaCaT cells. Xanthone also suppressed the production of pro-inflammatory cytokines, chemokines, and allergic mediators in phorbol myristate acetate/A23187 calcium ionophore (PMACI)-stimulated HMC-1 cells. Xanthone significantly suppressed the phosphorylation of mitogen-activated protein kinases (MAPKs) and nuclear factor-kappa B (NF-κB) and activation of caspase-1 signaling pathway in vitro model. Additionally, xanthone administration alleviated 2,4-dinitrofluorobenzene (DNFB)-induced atopic dermatitis like-skin lesion by reducing the serum levels of immunoglobulin E (IgE), histamine, and pro-inflammatory cytokines and suppressing MAPKs phosphorylation. Xanthone administration also inhibited mortality due to compound 48/80-induced anaphylactic shock and suppressed the passive cutaneous anaphylaxis (PCA) reaction mediated by IgE. Collectively, these results suggest that xanthone has a potential for use in the treatment of allergic inflammatory diseases.     

呫吨酮类衍生物抗肿瘤活性研究进展

呫吨酮是含氧杂环化合物的重要组成部分.此类化合物的生物活性与其三环骨架和骨架上取代基团的性质和位置有关.该文总结了一系列天然与合成的呫吨酮类衍生物的抗肿瘤活性,并且阐述了部分重要的抗肿瘤机制,详细介绍了一些呫吨酮类衍生物的抗肿瘤及其对靶点的作用,尤其是对蛋白激酶C调变作用的研究;还列举了部分具有癌症治疗效果的呫吨酮类化合物,包括DMXAA、普梭草素、芒果苷、降阿赛里奥、曼果斯廷等.     

Biological investigation of phenyl benzoate,benzophenone, and xanthone compounds

In the present study, we evaluated the antitumor, anti-tyrosinase, anti-pancreatic lipase, antibacterial, antifungal, and anti-α‐glycosidase activities for all or a subset of 20 known compounds. They included 8 phenyl benzoates, 10 benzophenones, and 2 xanthones. Phenyl benzoate compounds 1–8 did not exhibit evident antitumor activity, which was consistent with existing theories. Compounds 16, 17, and 18 exhibited moderate anti-tyrosinase activity. In addition, compounds 11 and 18 exhibited moderate inhibitory activity against Candida albicans, and compound 20 exhibited stronger anti-α-glycosidase activity than quercetin, with an IC₅₀ of approximately 2.45 μM. These results demonstrated that compounds 11, 16–18, and 20 were promising leads for further structural modification.     

民族药紫红獐牙菜中酮成分的分离与鉴定

目的：提取分离和鉴定民族药紫红獐牙菜中的口山酮成分。方法：采用常压及加压硅胶柱层析等方法进行提取分离，用ＵＶ、ＩＲ、１Ｈ－ＮＭＲ、ＭＳ波谱技术及有关理化性质进行分析鉴定。结果：从紫红獐牙菜乙醇提取物中的乙酸乙酯萃取部分分离鉴定出７个单体化合物，化合物Ⅰ为８－０－β－Ｄ－吡喃葡萄糖－１，３，５－三羟基口山酮；Ⅱ为１，５，８－三羟基－３－甲氧基口山酮；Ⅲ为１，３，５，８－四羟基口山酮；Ⅳ为８－０－β－Ｄ－吡喃葡萄糖－１，５－二羟基－３－甲氧基口山酮；另３个化合物正在鉴定中。结论：对该民族药中的有效成分之一———口山酮类成分进行了系统提取分离与鉴定     

氧杂蒽酮类衍生物的合成

本文合成了14个1,3-二羟基氧杂蒽酮衍生物(Ⅱ～Ⅴ,Ⅷ,Ⅸ)。1,3-二羟基氧杂蒽酮与环氧氯丙烷在哌啶存在下反应,产生化合物(Ⅲ)及(Ⅳ)。(Ⅳ)与胺反应可得化合物(Ⅴ)。大鼠被动皮肤过敏试验(PCA)表明化合物(Ⅱ_c)有63%的保护作用(5 mg/kg静脉注射)。     

New xanthone glycosides from Securidaca inappendiculata

Three new xanthone glycosides, securixanside A ( 1 ), securixanside B ( 2 ), and securixanside C ( 3 ) were isolated from the stems of Securidaca inappendiculata . These compounds were characterized by spectrometric and chemical methods, including FABMS and one- and two-dimensional NMR experiments.     

A new compound from Gentianopsis paludosa

A new compound, named gentianopfluorenone (1), along with three known compounds,1-O-β-d-glucopyranosyl-5-hydroxy-3-methoxyxanthone (2), 1-O-[β-d-xylopyranosyl-(1 → 6)-β-d-glucopyranosyl]-7,8-dihydroxy-3–methoxyxanthone (3), and apigenin (4), were isolated from the whole herb of Gentianopsis paludosa. On the basis of spectral and chemical evidence, the structure of 1 was elucidated as 4,4a,6-trihydroxy-5-methoxy-fluoren-2,9-dione. Compounds 2–4 were isolated from the plant for the first time.