南蛇藤属植物及其活性成分抗炎作用与机制研究进展

南蛇藤属(Celastrus L.)植物具有抗肿瘤、抗炎、抗衰老及杀虫抑菌等生物活性,在我国民间以及中医药领域有着悠久的应用历史。南蛇藤属植物的抗炎作用备受关注,相关机制研究取得较大进展,但缺乏系统整理。笔者通过对南蛇藤属提取物及其所含活性成分的药理作用进行总结,发现其对类风湿性关节炎、非酒精性脂肪性肝炎、结肠炎、胃溃疡及神经炎症等炎性疾病模型均具有较好的改善作用,且主要通过降低炎性反应、调节氧化应激及抑制炎性细胞增殖等发挥作用。因此该文主要对南蛇藤属植物及其单体活性成分抗炎的药理作用与机制研究进展按疾病种类进行综述,以期为其抗炎活性的深入研究及相关功能新产品的开发提供参考。     

南蛇藤属植物的化学成分与药理作用

南蛇藤属植物分布广泛，含有丰富的萜类、生物碱、黄酮类化合物。近来的研究证明其具有抗肿瘤、抗炎、镇痛、抗菌等广泛的药理活性，因此对其药效学物质基础进行深入的研究具有重要的现实意义。     

过山枫有效成分南蛇藤素和扁蒴藤素对斑马鱼节间血管生成的抑制作用研究

目的 观察过山枫有效成分南蛇藤素和扁蒴藤素对Fli1-GFP转基因荧光斑马鱼节间血管生成的影响。方法 采用Fli1-GFP转基因荧光斑马鱼胚胎,胚胎发育至6 h后,分别加入不同浓度的南蛇藤素及扁蒴藤素与斑马鱼胚胎共同孵育,待胚胎发育至30 h时,荧光显微镜下观察并计数斑马鱼胚胎节间血管的数量、血管芽数,测量血管长度并计算新生血管长度抑制率。结果 与阴性对照组比较,南蛇藤素与扁蒴藤素干预后,两组斑马鱼胚胎新生血管数量明显减少(P < 0.01),血管芽增多(P < 0.01),新生血管长度抑制率升高(P < 0.01)。结论 南蛇藤素及扁蒴藤素对斑马鱼节间血管生成有显著的抑制作用,这种作用与给药浓度呈正相关,南蛇藤素与扁蒴藤素比较,具有相近的新生血管抑制作用。     

穗花南蛇藤化学成分

目的:对贵州产穗花南蛇藤化学成分进行研究。方法:穗花南蛇藤乙醇提取物用乙酸乙酯萃取,乙酸乙酯部分用薄层色谱,硅胶反复柱色谱分离纯化,并用波谱学方法进行结构鉴定。结果:从中分离并鉴定了5个化合物,分别为β-谷甾醇(1)、β-香树酯醇(2)、β-香树酯醇乙酸酯(3)、30-hydroxylup-20(29)-en-3-one(4)、3-oxolup-20-(29)-en-30-al(5)。结论:所有化合物均首次从该植物中分离得到。     

南蛇藤化学成分及药理研究的进展

为探讨南蛇藤的药用价值,综述南蛇藤的植物来源、化学成分和药理作用.结果表明,南蛇藤有抗炎抗风湿、抗肿瘤、抗生育、抗氧化及抗多药耐药作用,有广阔的应用前景,值得深入研究.     

南蛇藤提取物化学成分及药理作用研究进展

目的:对南蛇藤植物的化学成分和药理作用研究进展作一综述.方法:按照化学结构类型和药理作用对南蛇藤植物的化学成分及活性物质和药理作用进行分类综述.结果:南蛇藤植物含有多种化学成分,主要有倍半萜、三萜及黄酮类化合物等,其药理作用主要有抗炎抗风湿、抗肿瘤、抗生育、抗氧化及抗多药耐药作用等.结论:南蛇藤植物应用前景广阔,值得深入研究.     

南蛇藤茎的化学成分(英文)

目的:研究南蛇藤Celastrus orbiculatus Thunb.茎的化学成分。方法:采用硅胶、Sephadex LH-20和ODS柱色谱方法进行化合物的分离和纯化。根据理化性质和光谱数据鉴定化合物结构。结果:从南蛇藤茎的乙酸乙酯部位分离得到11个化合物,经鉴定分别为:3β-hydroxy-2-oxoolean-12-ene-22,29-lactone(1),2,6-二甲氧基苯醌(2),3-氧代齐墩果酸(3),24-去甲基齐墩果烷-12-烯-28-酸-3-酮(4),白头翁酸(5),香草酸(6),23-羟基齐墩果烷-12-烯-28-酸-3-酮(7),丁香酸(8),齐墩果酸(9),β-谷甾醇(10),β-胡萝卜苷(11)。结论:化合物1为新三萜化合物,化合物2-5和7为首次从该属植物中分离得到,化合物8和9为首次从该植物中分离得到。     

南蛇藤茎的化学成分研究

目的研究南蛇藤Celastrus orbiculatus茎的化学成分。方法采用石油醚、醋酸乙酯、正丁醇分别对南蛇藤茎的乙醇提取物进行萃取;对萃取物运用硅胶、凝胶等分离手段进行反复分离纯化,经理化常数测定,结合UV、IR、1H-NMR、13C-NMR、MS方法鉴定结构。结果分离得到10个化合物,分别鉴定为山海棠二萜内酯A(Ⅰ)、(5β,8α,9β,10α,16β)-16-hydroxykaurane-18-oic acid(Ⅱ)、水杨酸(Ⅲ)、2,4,6-三甲氧基苯酚-1-O-β-D-葡萄糖苷(Ⅳ)、异槲皮苷(Ⅴ)、槲皮素-7-O-β-D-葡萄糖苷(Ⅵ)、( )-儿茶素(Ⅶ)、香草酸(Ⅷ)、β-胡萝卜苷(Ⅸ)、β-谷甾醇(Ⅹ)。结论以上化合物均为首次从该植物的藤茎中分离得到,化合物Ⅰ~Ⅲ为本属植物中首次分离得到,化合物Ⅳ~Ⅷ为本植物中首次分离得到。     

扁蒴藤素的抗氧化与抗肿瘤作用

目的 :研究扁蒴藤素的体外抗氧化与抗肿瘤活性。方法 :用TBA比色法测Fe2 抗坏血酸 (Fe2 AA)诱导的大鼠心、肝、肾组织匀浆MDA生成 ;用MTT法测定对HL 60细胞的抗肿瘤活性。结果 :扁蒴藤素剂量依赖性抑制Fe2 AA诱导的大鼠心、肝、肾组织匀浆MDA的生成 ,剂量、时间依赖性地抑制IL 60细胞生长。结论 :扁蒴藤素有明显抗氧化及抗肿瘤作用。     

南蛇藤的研究进展

南蛇藤含有丰富的萜类、生物碱、黄酮类化合物。现代研究证实其具有抗炎镇痛、抗肿瘤、抗菌、抗病毒、抗生育等广泛的药理活性,对其药效学物质基础进行深入的研究和开发,具有重大意义。     

绿独籽藤根皮的化学成分研究

目的:对绿独籽藤(Celastrus virens)根皮的化学成分进行研究。方法:用色谱法分离,并用波谱法对化合物的结构进行鉴定。结果:从绿独籽藤根皮中分离并鉴定了7个化合物,分别为齐墩果烯(oleanene 1)、木栓酮(3-oxo-friedelane 2)、3,12-二氧代木栓烷(3,12-dioxofriedelane 3)、3-氧代-30-羟基木栓烷(3-oxo-30-hydroxyfriedelane 4)、3-氧代-12α-羟基木栓烷(3-oxo-12α-hydroxyfriedelane 5)、扁蒴藤素(pristimerin 6)、雷公藤红素(celastrol 7)。结论:首次对绿独籽藤根皮的化学成分进行了报道。     

独子藤化学成分研究

目的 研究独子藤Celastrus monospermus Roxb.根的化学成分.方法 用乙酸乙酯提取,依次用石油醚、三氯甲烷和乙酸乙酯萃取,硅胶正相柱色谱及结晶法进行化学成分的分离纯化,通过理化性质和波谱分析鉴定结构.结果 从独子藤根中分离得到10个化合物,鉴定了其中8个化合物,分别为木栓酮(1)、28-羟基木栓酮...     

Antiinflammatory constituents of Celastrus orbiculatus inhibit the NF-kappaB activation and NO production.

Two new sesquiterpene esters, 1beta,8beta-diacetoxyl-6alpha,9alpha-difuroyloxydihydro-beta-agarofuran (1) and 1beta-acetoxyl-2beta,6alpha,9alpha-trifuroyloxydihydro-beta-agarofuran (2), together with four known sesquiterpene esters (3-6), celastrol (7), and celaphanol A (8) were isolated from the roots of Celastrus orbiculatus in a search for inhibitors of NF-kappaB activation and nitric oxide production. Compound 7 was the most active, while compounds 1, 2, 4, and 8 showed moderate inhibition in both NF-kappaB activation and nitric oxide production.     

Antinociceptive and hypnotic properties of Celastrus orbiculatus

Ethnopharmacological relevance

Celastrus orbiculatus, a woody vine of the Celastraceae family, has been widely used as a traditional medicine for the treatment of many diseases, including rheumatoid arthritis and odontalgia. In this study, we assessed the sedative and antinociceptive activities of the methanolic extract of Celastrus orbiculatus (MCO).

Materials and methods

The antinociceptive effect of MCO was evaluated using several experimental pain models, including thermal nociception methods, such as the tail immersion and the hotplate tests, as well as chemical nociception induced by intraperitoneal acetic acid and subplantar formalin administration in mice. To verify the possible connection of the opioid receptor to the antinociceptive activity of MCO, we performed a combination test with naloxone, a nonselective opioid receptor antagonist. The sedative effect of MCO was studied using the pentobarbital-induced sleeping model.

Results

MCO demonstrated strong and dose-dependent antinociceptive activity compared to tramadol and indomethacin in various experimental pain models. The combination test using naloxone revealed that the antinociceptive activity of MCO is associated with activation of the opioid receptor. MCO also caused decreased sleep latency and increased sleeping time in the pentobarbital-induced sleeping model; however, MCO alone did not induce sleep.

Conclusions

In the present study, MCO showed potent antinociceptive and sedative activities. Based on these results, MCO may be considered a valuable anti-nociceptive and hypnotic agent for the treatment of various diseases.     

Cytotoxic dihydroagarofuranoid sesquiterpenes from the seeds of Celastrus orbiculatus

A chemical study on the seeds of Celastrus orbiculatus has led to the isolation of nine new (1- 9) and 13 known dihydro-beta-agarofuran derivatives. The identification and structural elucidation of the new compounds were based on spectroscopic data analysis, and the absolute configurations of compounds 1- 6, 8-10, and 16, as well as derivatives 2a and 6a, were determined by CD studies or by chemical methods. All compounds isolated were evaluated for cytotoxic activity against HL-60 human leukemia cells.     

山核桃树皮化学成分研究

目的 研究山核桃树皮化学成分.方法 利用硅胶柱色谱及重结晶等方法进行分离纯化,通过理化性质及波谱分析鉴定结构.结果 得到15个化合物,鉴定为:4,8-二羟基萘酚-1-O-β-D-(6'-乙酰氧基)吡喃葡萄糖苷(Ⅰ)、双氢山柰酚(Ⅱ)、胡桃醌(Ⅲ)、胡萝卜苷(Ⅳ)、山柰酚(Ⅴ)、4,8-二羟基萘酚-1-O-β-D-[6-O-(3",5"-二甲氧基-4"-羟基苯甲酰基)]吡哺葡萄糖苷(Ⅵ)、山柰酚-3-O-α-L-鼠李糖苷(Ⅶ)3,3'-二甲氧基鞣花酸(Ⅷ)、柚皮素(Ⅸ)、槲皮索(Ⅹ)、4,8-二羟基四氢萘醌(Ⅺ)、槲皮素-3-O-α-L-鼠李糖苷(Ⅻ)、柚皮素-7-O-β-D-葡萄糖苷(XⅢ)、4,8-二羟基萘酚-1-O-β-D-吡喃葡萄糖苷(XⅣ)、4,5,8-三羟基-α-四氢萘醌-5-O-β-D-[6'-O-(3",5"-二甲氧基-4"-羟基苯甲酰基)]吡喃葡萄糖苷(XⅤ).结论 化合物I为新化合物,命名为山核桃酚;化合物Ⅰ、Ⅶ～Ⅸ、Ⅷ、XⅢ系首次从该属植物中得.     

太白楤木根皮化学成分的研究

目的：对新种太白木（ＡｒａｌｉａｔａｉｂａｉｅｎｓｉｓＺ．Ｚ．ＷａｎｇｅｔＨ．Ｃ．Ｚｈｅｎｇ）的化学成分进行研究。方法：利用溶剂提取和硅胶柱层析进行分离，根据化合物理化性质和光谱数据鉴定其结构。结果：得到３个化合物，分别确定为齐墩果酸（ｏｌｅａｎｏｌｉｃａｃｉｄ，Ⅰ），去葡萄糖竹节参皂苷Ⅳa（２８－ｄｅｓｇｌｕｃｏｓｙｌ－ｃｈｉｋｕｓｅｔｓｕｓａｐｏｎｉｎⅣａ，Ⅱ）和竹节参皂苷Ⅰｂ（ｃｈｉｋｕｓｅｔｓｕｔｓａｐｏｎｉｎⅠｂ，Ⅲ）。结论：３个化合物均为首次从该植物中分得。     

Cytotoxic sesquiterpenoids from the ethanol extract of fruits of Celastrus orbiculatus

AIM OF THE STUDY: To investigate the cytotoxic compounds against human melanoma A375-S2 and human cervical carcinoma Hela cell lines from the fruits of Celastrus orbiculatus. MATERIALS AND METHODS: The ethanol extract of the fruits of C. orbiculatus was found to exhibit significant cytotoxic activity. After partition, the column chromatography and Semi-preparative HPLC were used for activity guided fractionation from the active petroleum ether-soluble part. NMR and ESI-MS spectra for structure analysis were recorded on spectrometers, respectively. The cytotoxic activities of the isolated compounds were determined using the MTT assay. RESULTS: Four sesquiterpenoids (1-4) were isolated by activity guided fractionation from the ethanol extract of the fruits of C. orbiculatus. Compounds 1-3 exhibited promising cytotoxicities against the Hela cells and A375-S2 cells. The cytotoxic activities of compounds 1-3 seemed to be dose-dependent, which exhibited more potent inhibition for the proliferation of two cell lines when increased the concentrations of every compounds. Among these compounds, compound 2 showed most cytotoxicities against either Hela cells or the A375-S2 cells. CONCLUSIONS: The cytotoxic activity of the ethanol extract of fruits of C. orbiculatus against human melanoma A375-S2 and human cervical carcinoma Hela cells due to its content of sesquiterpenoids, supports its potential therapeutic value for the treatment of tumor.