表观遗传修饰剂线性肟酸对桦褐孔菌三萜合成的影响

目的 三萜类化合物是药用真菌桦褐孔菌产生的主要次生代谢产物之一,但其在实验室培养条件下积累量较少。旨在研究组蛋白去乙酰化酶（histone deacetylase,HDAC）活性抑制剂线性肟酸（suberoylanilide hydroxamic acid,SAHA）对桦褐孔菌三萜合成的调控。方法 液体摇瓶发酵法培养桦褐孔菌,并在培养液中添加SAHA。采用荧光定量PCR测定三萜合成相关基因转录水平,香草醛-高氯酸法测定细胞内和发酵液中三萜的含量。结果 SAHA的添加提高了桦褐孔菌体内编码3-羟基-3-甲基戊二酸单酰辅酶A合成酶、3-羟基-3-甲基戊二单酰辅酶A还原酶、甲羟戊酸激酶、二磷酸酯脱羧酶、角鲨烯合成酶和羊毛甾醇合成酶等基因的表达水平。SAHA显著提高了桦褐孔菌菌丝体内和发酵液中三萜的积累量。SAHA诱导下桦褐孔菌菌丝体内三萜积累量达（66.4±5.24）mg/g,明显高于对照组[（22.7±3.3）mg/g],并且胞外三萜的含量由对照组的（30.5±2.7）mg/L提高至（49.3±3.8）mg/L。此外,经SAHA处理后桦褐孔菌胞内三萜清除自由基的能力显著提高。结论 SAHA...     

决明毛状根化学成分的研究

目的 研究决明毛状根的化学成分。方法 应用毛状根培养技术,在实验室摇瓶积累生产决明毛状根干重90g,结果 从中分离得到1个化合物,根据其理化性质和波谱分析。鉴定为betulinic acid（桦木酸）。结论 此化合物为决明毛状根和该属植物中首次分离得到。通过决明毛状根与其干燥种子、根、茎、叶的化学成分在薄层层析上比较。结果表明,决明毛状根培养可代谢产生桦木酸或大幅度提高桦木酸的含量。     

膜荚黄芪叶中三萜皂苷类成分的分离与鉴定

目的：研究膜荚黄芪叶中的三萜皂苷类成分。方法：采用硅胶、十八烷基硅烷键合硅胶(ODS)等色谱方法对膜荚黄芪叶的化学成分进行分离,通过一维核磁共振氢谱(¹D-NMR)和²D-NMR法分析鉴定化合物。结果：从膜荚黄芪叶提取物中共分离出15个化合物,分别鉴定为黄芪叶苷B(1)、黄芪叶苷L(2)、cyclounifolioside D(3)、3-O-[α-L-吡喃鼠李糖基-(1→2)-β-D-吡喃木糖基]-6-O-β-D-吡喃葡萄糖基-24-O-α-L-吡喃阿拉伯糖基-16-乙酰基-3β,6α,16β,24(S),25-五羟基环菠萝蜜烷(4)、黄芪叶苷K(5)、黄芪叶苷A(6)、astraverrucinⅠ(7)、cycloaraloside A(8)、黄芪叶苷D (9)、astralanosaponin D (10)、大豆皂醇E (11)、3β,21α,24-三羟基-齐墩果-12-烯(12)、3β,22β,24,29-四羟基齐墩果-12-烯(13)、豌豆皂苷Ⅰ(14)、大豆皂醇B-3-O-β-D-吡喃葡萄糖醛酸基-(1→2)-β-D-吡喃葡萄糖基-...     

Indian Morinda species: A review

Morinda is a largest genus of Rubiaceae family, and its 11 species are found in India. In India, plant species are known by several common names as great morinda, Indian mulberry, noni, beach mulberry and cheese fruit. Various Morinda products (capsules, tablets, skin products and fruit juices) are available in the market, used by people for treatment of several health complaints. A diversity of phytochemicals including iridoids, flavonoids, flavonoid glycosides, anthraquinones, coumarins, lignanas, noniosides, phenolics and triterpenoids have been reported from Morinda species. Morinda species are used in the treatment of inflammation, cancer, diabetes, psyquiatric disorders, and bacterial and viral infections. The noni fruit juice (Morinda citrifolia) and its products are used clinically in the treatment of cancer, hypertension and cervical spondylosis affecting patients. M. citrifolia fuit juice, with different doses, is used in the maintaining blood pressure and reducing of superoxides, HDL and LDL levels. Similarly, oligosaccharide capsules and tablets of root extract of M. officinalis are recommended as medicine for the treatment of kidney problems and sexual dysfunctions of patients. The toxicological studies revealed that higher doses of fruit juice (4,000 or 5,000 mg/kg) of M. citrifolia for 2 or more months cause toxic effects on liver and kidneys. M. officinalis root extracts (ethanolic and aqueous) are found fully safe during treatment of diseases. A large number of reviews are available on M. citrifolia but very few studies are conducted on other Indian Morinda species. This review reports the comprehensive knowledge on state‐wise distribution, botany, ethnomedicinal uses, phytochemistry, pharmacological activities, clinical applications and toxicological evaluations of 11 species of Morinda found in India.     

Lanostane Tetracyclic Triterpenoids as Important Sources for Anti‑Inflammatory Drug Discovery

Inflammation is a defensive reaction of the human body to numerous detrimental stimuli, including physical trauma, noxious chemicals, as well as microbial agents. Uncontrolled inflammation is the pathological basis of multiple diseases, such as rheumatoid arthritis(RA), neurodegenerative diseases, liver disease, and lung inflammation. Lanostane triterpenoids are natural tetracyclic triterpenoids with significant anti-inflammatory activity. An extensive review of the published literature regarding the phytochemistry and anti-inflammatory pharmacology of lanostane triterpenoids has been performed and analyzed using several search engines, such as SciFinder, Web of Science, Scopus, PubMed, Google Scholar, and ScienceDirect. This review is devoted to naturally occurring lanostane-type triterpenes with anti-inflammatory activity, including their sources, biosynthesis, and mechanism of action. This review also discusses the inflammation-related diseases and the clinical significance of traditional Chinese medicine as multi-target therapeutic agents for the prevention and treatment of inflammatory diseases. In the past 30 years, more than 100 new lanostane-type triterpenes have been reported from the families Schisandraceae, Ganodermataceae, and Polyporaceae. Six compounds, fomitopinic acid A, fomitosides E and F, obtusifoliol, 4α, l4α-dimethyl-5α-ergosta-7,9(11), 24(28)-trien-3 β-ol, and gramisterol exhibited the most potent anti-inflammatory activity against cyclooxygenase-1(COX-1) and COX-2, with IC50 values ranging from 0.087 to 1.15 μM. Some of these compounds exhibited significant activity by mediating the inhibition of the pro-inflammatory cytokines, inducible nitric oxide synthase, and COX-2 expression. This review provides a basis for identifying anti-inflammatory drugs with high selectivity, high potency, and few adverse effects from lanostane-type triterpenes.     

蒙药材多叶棘豆化学成分和药理作用研究进展

蒙药材多叶棘豆为蒙古族习用药材，具有杀"黏"、清热、燥"协日乌素"等功效。本文对多叶棘豆中的黄酮类、三萜类、酰胺类和其他类化学成分及抗氧化和抗菌等药理作用的研究现状进行了概述，为其进一步研究提供参考。     

参与植物三萜生物合成的细胞色素P450酶研究进展

三萜是许多药用植物的活性成分,目前已对其生物合成途径进行了大量研究并取得了重大进展。细胞色素P450(CYP450)主要参与三萜的后修饰过程,对三萜的多样性起着关键作用。目前,已从多种植物中克隆得到与三萜生物合成相关的CYP450基因。对参与三萜生物合成的CYP450的功能研究进行综述,为三萜生物合成途径的解析及CYP450的功能研究提供借鉴。     

Immunomodulatory activities of isolated compounds from the root-bark of Cussonia arborea

Context: Cussonia arborea Hochst. ex A. Rich (Araliaceae) is a folk medicine used to treat various diseases. However, there is no report of the root phytochemistry.

Objective: This study isolates and identifies the immunomodulatory compounds from root-bark of C. arborea.

Materials and methods: The methanol extract (18?g) was subjected to repeated column chromatography resulting in isolation of five compounds (1–5). Structure determination was achieved by analysis of their 1?D and 2?D NMR, and mass spectroscopy. The compounds (100–1.0?μg/mL) were examined immunomodulatory for effect on production of reactive oxygen species (ROS) from whole blood phagocytes and on proliferation of T-cells. The compounds cytotoxicity (100–1.0?μg/mL) was evaluated on NIH-3T3 normal fibroblast cells.

Results: Three pentacyclic triterpenoids [3, 23-dihydroxy-12-oleanen-28-oic acid (1), 3β-hydroxylolean-12-en-28-oic (2) and 23-hydoxy-oxo-urs-12-en-28-oic acid (5)], two phytosterols: [stigmasterol (3)] and [3-O-β-d-glucopyranosyl stigmasterol (4)] were all isolated from the methanol soluble extract. All the tested compounds (1–4) were found to be nontoxic on NIH-3T3 cells. Compound 1 and 2 moderately inhibited the production of ROS (IC₅₀?=?24.4?±?4.3 and 37.5?±?0.1?μg/mL, respectively) whereas compound 2 exhibited the highest inhibitory effect (IC₅₀?=?12.6?±?0.4?μg/mL) on proliferation of phytoheamagglutinin (PHA) activated T-cells.

Conclusions: The isolated compounds (1–5) are reported for the first time from this species. In addition, compound 2 with suppressive potential on production of intracellular ROS and proliferation of T-cells could be of immense value in control of autoimmune diseases as well as in immune compromised patients.     

Anti-inflammatory activity of phenylpropyl triterpenoids from Osmanthus fragrans var. aurantiacus leaves

Osmanthus fragrans var. aurantiacus has been used for the treatment of menopausal pain, foul breath, and intestinal bleeding. Four phenylpropyl triterpenoids, 3-O-trans-p-coumaroyltormentic acid (1), 3β-trans-p-coumaroyloxy-2α-hydroxyl-urs-12-en-28-oic acid (2), 3β-cis-p-coumaroyloxy-2α-hydroxyl-urs-12-en-28-oic acid (3), 3-O-cis-coumaroylmaslinic acid (4), were isolated from the leaves of O. fragrans var. aurantiacus and the inhibitory effect on nitric oxide (NO) production in lipopolysaccharide (LPS)-induced macrophages were evaluated. Among them, compounds 2–4 concentration dependently showed NO production inhibitory effects. To determine the signaling factors involved in the inhibition of NO production by compounds 2–4, we assessed anti-inflammatory activity. Western blot analysis revealed compounds 2–4 significantly decreased the expression of LPS-stimulated protein, inducible nitric oxide synthase (iNOS), cyclooxygenase (COX)-2, nuclear factor-kappa B (NF-κB) and phosphorylated extracellular regulated kinase (pERK)1/2. Also, compounds 2–4 downregulated tumor necrosis factor (TNF)-α, interleukin (IL)-1β, IL-6 and IL-8 levels in LPS-induced macrophages and colonic epithelial cells. This study demonstrated that phenylpropyl triterpenoids 2–4 isolated from O. fragrans var. aurantiacus leaves can be used as potential candidates for the prevention and treatment of inflammatory bowel disease.     

苏木蓝和花木蓝的化学成分研究

目的 研究木蓝山豆根的主要来源植物--苏木蓝lndigofera carlesii和花木蓝I.kirilowii的化学成分.方法 运用溶剂萃取.硅胶柱色谱、大孔树脂柱色谱、重结晶等方法分离纯化,根据NMR、MS谱数据及与对照品共薄层色谱鉴定化合物的结构.结果 从木蓝属两种植物中共分离鉴定了11个化合物,其中从苏木蓝根乙醇提取物中分离鉴定了3个化合物:3-O-α-L-鼠李吡喃糖基-(1→2)-[β-D-半乳吡喃糖基(1→3)]-α-L-阿拉伯吡喃糖基齐墩果酸-28-O-α-L-鼠李吡喃糖基-(1→4)-β-D-葡萄吡喃糖基-(1→6)-β-D-葡萄吡喃糖基酯(工)、木栓酮(Ⅱ)、正丁基-β-D-吡喃果糖苷(Ⅲ);从花木蓝叶乙醇提取物中分离鉴定了2个化合物:八角枫苷A(alangioside A,Ⅳ)、异鼠李素-3-O-芸香糖苷(Ⅴ);从花木蓝根乙醇提取物中分离鉴定了6个化合物:亚油酸乙酯(Ⅵ)、咖啡酸十八、二十、二十二、二十四烷醇酯的混合物(Ⅶ)、1-棕榈酸单甘油酯(Ⅷ)、乙酰齐墩果酸(Ⅸ)、丁香酸葡萄糖苷(Ⅹ)和橙皮苷(Ⅺ).结论 所有化合物均为首次从木蓝属植物中分离得到,其中化合物Ⅰ、Ⅳ分别为三萜皂苷类和紫罗烷(megastig-mane)型倍半萜类化合物,为从木蓝属植物首次报道的两种类型的天然化合物.