环烯醚萜类化合物治疗氧化应激诱发疾病的研究进展

目的：综述环烯醚萜类化合物对氧化应激诱发的相关疾病可能的治疗机理。方法：查阅、总结国内外发表的氧化应激诱导的相关疾病的成因和环烯醚萜化合物调节相关疾病的可能机理的报道。结果：氧化应激可以引起广泛的细胞内损伤,从而诱发神经系统疾病、肿瘤和糖尿病等相关疾病。环烯醚萜类化合物可通过调节机体抗氧化应激的能力,预防和减缓相关疾病的发生和发展。结论：环烯醚萜类化合物降低机体氧化应激水平,对于开发此类化合物的新药具有广泛前景。     

环烯醚萜类化合物的研究进展

以近5 a来国内外发表的文献为依据,从结构分类和生物活性两方面综述环烯醚萜类化合物的研究进展.环烯醚萜类化合物结构繁多,具有多种生物活性. 环烯醚萜化合物具有很高的研究价值.     

环烯醚萜类化合物近年研究进展

目的 介绍环烯醚萜类化合物研究概况和近年研究进展。方法 以近年来国内外发表的文献为依据,从结构分类、半合成及生物活性方面综述环烯醚萜类化合物近年研究进展。结果 环烯醚萜类化合物具有多种生物活性。结论 环烯醚萜是一类很有研究价值的化合物。     

中药环烯醚萜类化合物研究进展

环烯醚萜类化合物是植物中存在的一大类化合物,具有多种药理活性,是许多中药的主要有效成分。对环烯醚萜类化合物的结构、分布、药理活性及提取、分离、定量测定方法等方面进行了综述,以期为环烯醚萜类化合物的进一步研究开发提供参考。     

10批栀子中环烯醚萜苷类成分含量测定

目的 测定不同产地的10批栀子药材中栀子苷、京尼平龙胆二糖苷及总环烯醚萜苷含量。方法 采用HPLC测定栀子苷、京尼平龙胆二糖苷含量;采用紫外分光光度法测定总环烯醚萜苷含量。结果 江西产栀子中环烯醚萜苷类成分含量高。结论 不同产地栀子药材中环烯醚萜苷类成分含量有所差别。     

巴戟天属植物中环烯醚萜类化合物研究进展

摘要：环烯醚萜类化合物广泛存在于巴戟天属植物中,具有抗抑郁、镇痛抗炎、骨保护、抗衰老、抗肿瘤、保护心血管和抗菌等作用。本文总结了巴戟天属植物中环烯醚萜类化合物的种类、结构、药理活性及含量检测方法,对分析巴戟天属植物中环烯醚萜类成分的物质基础和作用机制具有重要的意义。     

独一味总环烯醚萜苷分离纯化工艺的优化

目的 优化独一味总环烯醚萜苷的制备工艺,获取纯度相对较高的总环烯醚萜苷。方法 以甲醇-水为流动相,梯度洗脱方式建立分离分析独一味总环烯醚萜苷的高效液相色谱方法,实现各组分的最佳分离,统计、记录其三维吸收图谱,并结合紫外全波长扫描,对前期制备的独一味总环烯醚萜苷中影响纯度的杂质特征进行分析,根据杂质特性优化大孔树脂结合聚酰胺柱制备过程,紫外实时监测,剔除杂质,产品溶液经冷冻干燥获得冻干粉,并以HPLC对比前后制备工艺产品成分差异。结果 工艺优化前产品中环烯醚萜苷含量为69.06%,优化后含量为90.60%,含量提升21.54%;本次制备总产率为16.70%（以水提取物的质量为参照）,总环烯醚萜苷转移率为74.72%（相对于水提取物中总环烯醚萜苷的质量）。结论 优化过程简单,操作步骤可控,易于实现,纯化效果显著。     

恩施巴戟环烯醚萜苷类成分提取工艺优选及抗氧化活性研究

目的 优化恩施巴戟中主要环烯醚萜苷类成分提取工艺,评价恩施巴戟体外抗氧化活性。方法 选择经典的加热回流提取法,以乙醇体积分数、溶剂倍量、提取时间为考察因素,以浸膏得率和水晶兰苷含量的综合评分为评判指标,设计正交试验筛选最佳提取工艺条件;测定总还原能力、DPPH清除率、羟自由基清除率,检测其体外抗氧化活性。结果 最佳提取工艺条件为6倍量的60%的乙醇加热回流2 h;恩施巴戟具有一定的抗氧化能力,乙酸乙酯部位活性最佳。结论 优化的提取工艺稳定可行,可用于提取恩施巴戟的环烯醚萜苷类成分,该研究初步证明了恩施巴戟具有一定的抗氧化活性。     

白毛夏枯草及其复方次生代谢产物含量与抑菌活性相关性研究

目的 比较白毛夏枯草饮片及其2种复方汤剂的次生代谢产物含量与抑菌活性的相关性,为合理配伍提供依据。方法 采用牛津杯琼脂扩散法测定抑菌圈大小,利用分光光度法测定次生代谢产物(总黄酮、总皂苷、环烯醚萜类和总生物碱)含量,并进行抑菌活性相关性和通径分析,确定目标化合物。结果 总黄酮、总皂苷和环烯醚萜类含量：复方1>复方2>单方,总生物碱含量：复方2>单方≈复方1。2种复方抑菌强度基本相同且显著高于单方,4种次生代谢产物对金黄色葡萄球菌的抑菌活性均起正相关作用,总环烯醚萜直接通径系数最大。结论 白毛夏枯草复方次生代谢产物含量和抑菌活性均高于单方,影响其抑菌活性的成分主要是环烯醚萜类与皂苷类。     

黄蝉属植物化学成分研究进展

以国内外文献为依据，对从黄蝉属植物中报道的化学成分进行了整理和综述，介绍黄蝉属化学成分研究概况，为其进一步开发利用提供参考。成分类别主要为环烯醚萜（iridoid）和木脂素（lignan）类，所发现的化合物分别为环烯醚萜24个，木脂素9个，其他类别成分较少。其中环烯醚萜类内酯成分黄蝉花定（Allamandin）、鸡蛋花素（plumericin）等的生物活性显示有抗肿瘤、抗真菌作用。     

Three new iridoids from leaves of Cornus officinalis

Three new iridoids, cornifins A–C (1–3), together with a known iridoid, were obtained from EtOAc layer of leaves of Cornus officinalis. The structures of new compounds were elucidated on the basis of extensive spectroscopic analyses. Compound 2 showed weak inhibitory activity against lung cancer cell line A-549 with IC₅₀ value of 29.1 μM.     

Coumarin derivatives: an updated patent review (2012 – 2014)

Introduction: Coumarins belong to the benzopyrones family. They are naturally plant-derived and synthetically taken polyphenolic substances, presenting a wide variety of biological activities and behaviours, supporting their use as therapeutic agents for multiple diseases. Their structural characteristics correlated to physicochemical properties seem to define the extent of the biological activity.

Areas covered: Recent patent publications (2012 – 2014), describing coumarins and their derivatives are analyzed. Synthesis, hybridization techniques and biological evaluation in vitro/in vivo, for example, antimitotic, antiviral, anticancer, cytotoxic, anti-acne and antioxidant coumarin macromolecule polymer agents are included. Furthermore, a wide range of pharmaceutical applications and pharmaceutical compositions are also summarized.

Expert opinion: Several natural and synthetic coumarins, hybrids and derivatives appear to have promising anticancer-antitumor activities. Their clinical evaluation will be critical to assess therapeutic utility. The compounds for which the mechanism of action is well defined can serve as lead compounds for the design of new more potent molecules.     

A new iridoid glycoside and NO production inhibitory activity of compounds isolated from Russelia equisetiformis

From the 1-BuOH-soluble fraction of a MeOH extract of the leaves of Russelia equisetiformis, one new iridoid glucoside was isolated along with 24 known compounds, comprising iridoids and iridoid glucosides, phenyl propane glucosides, phenyl ethanoids, lignan glucosides, and flavonoid glucosides. The structure of the new compound was elucidated to be 10-O-cinnamoyl sinuatol. Of the 25 compounds isolated, rehmaglutin B exhibited moderate inhibitory activity toward NO production, which was not associated with cytotoxicity.     

Iridoid and phenylpropanoid glycosides from Pedicularis artselaeri

Six new compounds, an iridoid glucoside, 6- O-methyl-epiaucubin, three iridoids, artselaenins A, B, C, a phenylethanoid glycoside, artselaeroside A, and a phenylpropanoid glycoside, artselaeroside B, as well as fourteen known compounds, nine iridoid glycosides and five phenylpropanoid glycosides were isolated from the whole plants (including roots, stems, leaves and flowers) of Pedicularis artselaeri. Their structures were identified mainly by spectral evidence.     

Rhodanine as a scaffold in drug discovery: a critical review of its biological activities and mechanisms of target modulation

Introduction: Rhodanine-based compounds have been associated with numerous biological activities. After many years of research in drug discovery, they have gained a reputation as being pan assay interference compounds (PAINS) and frequent hitters in screening campaigns. Rhodanine-based compounds are also aggregators that can non-specifically interact with target proteins as well as Michael acceptors and interfere photometrically in biological assays due to their color.

Areas covered: The authors review the recently reported biological activities of rhodanine-based compounds. Furthermore, the article provides details of their synthesis and occurrence in compound libraries through high-throughput screening (HTS) and virtual high-throughput screening (VHTS). Additionally, the authors provide the reader with possible mechanisms of non-specific target modulation, analysis of the crystal structures of enzyme–rhodanine complexes and a comparison of rhodanine and thiazolidine-2,4-dione moieties.

Expert opinion: The biological activity of compounds possessing a rhodanine moiety should be considered very critically despite the convincing data obtained in biological assays. In addition to the lack of selectivity, unusual structure–activity relationship profiles and safety and specificity problems mean that rhodanines are generally not optimizable.     

Two new non-glycosidic iridoids from the leaves of Campsis grandiflora

Two new non-glycosidic iridoids, which were named cachinol (1) and 1-O-methyl cachinol (2), were isolated from the methanol extract of the leaves of Campsis grandiflora together with a known iridoid cachineside I (3). The structures of compounds 1 and 2 were determined on the basis of spectroscopic methods including two dimensional NMR and high resolution mass spectrometry. All of the isolated compounds showed mild inhibitory activities on rat platelet aggregation. Compounds 1 and 3 (IC50 : 246 and 219 microM, respectively) showed about 2-fold higher inhibitory effects than acetylsalicylic acid (ASA, IC50: 412 microM) on collagen-induced aggregation. Compounds 1 and 2 (IC50: 43.2 and 38.4 microM, respectively) were about 2-fold more inhibitory than ASA (IC50: 75.2 microM), and about 4-fold more effective than their glycoside 3 (IC50: 189 microM) on AA-induced aggregation.     

Effects of iridoids on lipoxygenase and hyaluronidase activities and their activation by beta-glucosidase in the presence of amino acids

Enzyme inhibitory activities of 14 iridoids previously obtained from two Malaysian medicinal plants, Saprosma scortechinii and Rothmannia macrophylla, were evaluated in vitro using soybean lipoxygenase and bovine testis hyaluronidase. Most of the iridoids, including asperulosidic acid, paederosidic acid, and an epimeric mixture of gardenogenins A and B, did not show any effect on the enzyme activities, except for the bis-iridoids, which inhibited the lipoxygenase activity with their IC(50) values of approximately 1.3 times that of a known inhibitor, fisetin. Structural modification of asperulosidic acid and paederosidic acid through enzymatic hydrolysis by beta-glucosidase resulted in their inhibition towards the enzyme activities, and these activities were enhanced by the presence of some amino acids (lysine, leucine or glutamic acid) or ammonium acetate. Mixtures of gardenogenins A and B; isomers of non-glucosidic iridoids, incubated with amino acid or ammonium acetate did not show any inhibitory effect on the enzyme activities during the 6 h incubation period, except for lysine where spontaneous reaction between the iridoids and amino acid resulted in the inhibition of lipoxygenase activity. The results from these biomimetic reactions suggested that the iridoid aglycons and the intermediates formed by these reactive species could inhibit the enzyme activities, and thus substantiate previous reports that the formation of iridoidal aglycons is a prerequisite for the iridoid glycosides to demonstrate some of the biological activities. In addition, the results also indicated that it is worthwhile to further explore these intermediates as potential anti-inflammatory agents.     

Recent progress in therapeutic applications of chalcones

Introduction: Chalcones are a group of plant-derived polyphenolic compounds belonging to the flavonoids family that possess a wide variety of cytoprotective and modulatory functions, which may have therapeutic potential for multiple diseases. Their physicochemical properties seem to define the extent of their biological activity.

Areas covered: A comprehensive synopsis of recent patent literature (2005 – 2011) describing chalcones and their derivatives on selected activities (e.g., anti-inflammatory, antimitotic, cytotoxic, antioxidant, anti-infection) is provided in this paper. Synthesis, combinatorial techniques, biological evaluation in vitro/in vivo, and new biological assays are discussed. In addition to selected biological data, a wide range of pharmaceutical applications and pharmaceutical compositions are also summarized.

Expert opinion: Several natural and synthetic chalcones and their derivatives appear as promising anti-inflammatory and anticancer activities. Their clinical evaluation will be critical to assess their therapeutic utility. Those for which the mechanism of action is well defined can serve as lead compounds for the design of new, more promising molecules.