药用橄榄油中不皂化物成分研究

目的:研究药用橄榄油不皂化物的化学组成。方法:通过水解除杂、硅胶柱层析、制备薄层色谱等方法对药用橄榄油不皂化物组分进行制备分离,采用核磁共振波谱、质谱等方法对分离所得化合物进行结构鉴定。结果:从药用橄榄油不皂化物中分离鉴定了6个化合物,分别为:角鲨烯(1)、D-α-生育酚(2)、β-谷甾醇(3)、24-亚甲基环阿屯醇(4)、菜油甾醇(5)、胆固醇(6)。结论:药用橄榄油不皂化物主要成分为甾体化合物和具有抗氧化作用的角鲨烯、生育酚等,化合物1~6均为首次通过分离从橄榄油中获得单体化合物,并通过波谱手段进行结构鉴定。

辣木种子提取物对小鼠实验性肝损伤的保护作用

目的考察辣木种子提取物对小鼠实验性肝损伤(急性酒精性肝损伤、四氯化碳致急性肝损伤)的保护作用。方法 RT-PCR、Western blotting分别检测小鼠肝组织ADH1和ALDH2 mRNA、蛋白表达。建立小鼠急性酒精性肝损伤模型,测定ALT、AST、ALP、LDH、GSH、MDA水平;建立小鼠四氯化碳致急性肝损伤模型,测定ALT、AST、GSH、MDA、T-SOD、GSH-Px、GR水平,RT-PCR检测C/EBPα、TNF-α、SREBP-1c、COX-2 mRNA表达,HE染色观察小鼠肝组织病理学变化。结果提取物(500 mg/kg)可提高ADH1 mRNA、蛋白表达,但对ALDH2无明显影响。对于急性酒精性肝损伤小鼠,各剂量提取物(125、250、500 mg/kg)降低ALT、AST、ALP、LDH、MDA水平,提高GSH水平;对于四氯化碳致急性肝损伤小鼠,各剂量提取物(32. 5、75、150 mg/kg)降低ALT、AST、MDA、GSHPx水平及COX-2、TNF-α、SREBP-1c mRNA表达,提高T-SOD、GSH、GR水平及C/EBPαmRNA表达,改善肝组织形态。结论辣木种子提取物对小鼠实验性肝损伤有明显保护作用,其机制可能与加快乙醇代谢、缓解炎症反应、抑制脂肪酸和胆固醇合成、改善脂质代谢紊乱有关。

艾纳香挥发油化学成分及药理研究进展

艾纳香挥发油为中药艾纳香的主要组成部分,具有镇痛抗炎、抗菌、抗氧化及抑制酪氨酸酶等药理作用,已被开发研制成多种制剂产品。艾纳香挥发油化学成分复杂,主要含有单砧、倍半砧与脂肪酸类化合物,其含量及组成受提取方法、产地、采收时间、烘干条件等多种因素影响。目前,对艾纳香挥发油的研究已取得一定进展,但仍存在提取方法单一,质量标准难以统一,药理研究分散等问题,探索高效节能的提取方法,基于Q-marker建立权威的质量标准及深入的药理研究对艾纳香挥发油的开发及应用具有重要意义。本文对艾纳香挥发油的提取工艺、化学成分、药理作用等方面进行综述,为艾纳香挥发油深度开发和高效综合利用提供参考。

指纹图谱结合一测多评法评价艾纳香药材质量

目的建立艾纳香药材指纹图谱,并采用一测多评法(QAMS)对其中7种黄酮类成分的含量进行测定,为艾纳香药材质量评价提供依据。方法根据指纹图谱和一测多评(QAMS)模式要求,采用依利特C18色谱柱(250 mm×4.6 mm,5μm);以乙腈-0.2%甲酸水溶液为流动相,梯度洗脱;柱温30℃;检测波长为271 nm;体积流量0.8 mL/min,建立艾纳香药材指纹图谱,并采用相似度分析、主成分分析及聚类分析法对指纹图谱进行评价。以艾纳香甲素为内参物,建立其余6种黄酮成分(金丝桃苷,槲皮素,3-甲氧基槲皮素,怪柳黄素,艾纳香素,鼠李素)的相对校正因子,比较分析一测多评法与外标法含量测定结果的差异性。结果12批药材的相似度均大于0.96,确定了17个共有峰,对7个共有峰进行了指认,聚类分析结果与药材的产地分布情况基本一致;7种黄酮类成分含量结果外标法和一测多评法之间无显著性差异。结论指纹图谱结合一测多评法可以有效用于艾纳香药材的质量评价。

凉粉草中2个新的倍半萜苯甲酰酯

凉粉草是岭南地区常用的药食两用植物,具有广泛的药理活性,但其化学成分研究尚不充分。该研究运用多种现代色谱分离技术,从凉粉草地上部位的95%乙醇提取物中分离得到了2个化合物,综合使用紫外光谱(UV)、红外光谱(IR)、高分辨质谱(HR-ESI-MS)、一维和二维核磁共振技术(1D NMR和2D NMR)、单晶X射线衍射技术(SC-XRD)等结构鉴定方法确定了它们的绝对构型,为2个新的倍半萜苯甲酰酯类化合物,并分别命名为凉粉草醇甲(mesonanol A)和凉粉草醇乙(mesonanol B)。药理活性评价结果显示,2个新化合物均未表现出明显的抗病毒和抗炎活性。

何首乌中1个新的黄酮二苯乙烯苷

广东德庆为何首乌药材的道地产区之一,该研究综合运用大孔树脂(HP-20)、硅胶、凝胶(Sephadex LH-20)、制备型HPLC等色谱技术,从广东德庆产何首乌的块根中分离得到了1个化合物,并通过理化常数、波谱技术、计算圆二色谱及化学方法鉴定了其结构,为1个新的黄酮二苯乙烯苷,命名为何首乌黄酮茋B(polygonflavanol B,1)。

普约狗牙花枝叶的生物碱类成分研究

目的研究夹竹桃科普约狗牙花Tabernaemontana sananho枝叶的化学成分。方法利用硅胶、ODS、Sephadex LH-20等柱色谱技术及薄层色谱、制备液相色谱等方法进行分离、纯化,根据化合物的理化性质及波谱学数据鉴定其化学结构。结果从普约狗牙花枝叶的总生物碱部位中分离得到12个生物碱类成分,分别鉴定为冠狗牙花碱氮氧化物(1)、3-羰基冠狗牙花碱(2)、3-羰基冠狗牙花羟基伪吲哚碱(3)、柳叶水甘草碱(4)、柳叶水甘草碱氮氧化物(5)、3-羰基柳叶水甘草碱(6)、5β-羟基-3-羰基柳叶水甘草碱(7)、lochnericine(8)、(+)-voaphylline(9)、deacetylakuammiline(10)、去氢骆驼蓬碱(11)和咖啡因(12)。结论化合物1为新的天然产物,化合物7和12为首次从该属植物中分离得到,化合物2~6、8~11为首次从该植物中分离得到。

蓬莱葛枝叶的生物碱类成分研究

目的研究蓬莱葛Gardneria multiflora枝叶的化学成分。方法采用硅胶、ODS、Sephadex LH-20和HPLC等色谱方法进行分离纯化,并根据化合物的理化性质及波谱学数据鉴定其化学结构。结果从蓬莱葛枝叶中分离得到13个生物碱类化合物,分别鉴定为antirhine 4α-oxide (1)、geissoschizol (2)、melosline E (3)、土波台文碱(4)、tubotaiwine N-oxide(5)、pyridinium (6)、melosline B (7)、N-甲基巴婆碱(8)、venoterpine (9)、肉桂酰胺(10)、lyaloside (11)、异长春花苷内酰胺(12)、柯诺辛碱(13)。结论化合物1~13均为首次从该植物中分离得到。

蒜香藤中2个新的吡喃并萘醌类化合物

蒜香藤原产南美洲的热带雨林地区,现在我国华南地区有引种,具多种药理活性,但目前对其化学成分的研究报道较少。该研究运用硅胶、十八烷基键合硅胶(ODS)、葡聚糖凝胶(Sephadex LH-20)、制备型高效液相色谱(PHPLC)等多种现代色谱技术,从蒜香藤枝叶95%乙醇提取物中分离得到2个化合物,并通过紫外光谱(UV)、红外光谱(IR)、高分辨质谱(HRESI-MS)和一维及二维核磁共振技术(NMR)等多种谱学方法,鉴定它们的结构分别为8,9-dimethoxy-α-lapachone(1)和7-hydroxy-8,9-dimethoxy-α-lapachone(2),为2个新的吡喃并萘醌类化合物,并分别命名为蒜香藤素甲(mansonin A,1)和蒜香藤素乙(mansonin B,2)。

Natural products as potent inhibitors of hypoxia-inducible factor-1α in cancer therapy

Hypoxia is a prominent feature of tumors. Hypoxia-inducible factor-1α(HIF-1α), a major subunit of HIF-1, is overexpressed in hypoxic tumor tissues and activates the transcription of many oncogenes. Accumulating evidence has demonstrated that HIF-1α promotes tumor angiogenesis, metastasis, metabolism, and immune evasion. Natural products are an important source of antitumor drugs and numerous studies have highlighted the crucial role of these agents in modulating HIF-1α. The present review describes the role of HIF-1α in tumor progression, summarizes natural products used as HIF-1α inhibitors, and discusses the potential of developing natural products as HIF-1α inhibitors for the treatment of cancer.

Total Saponins of Panax notoginseng Activate Akt/mTOR Pathway and Exhibit Neuroprotection in vitro and in vivo against Ischemic Damage

Objective:To reveal the neuroprotective effect and the underlying mechanisms of a mixture of the main components of Panax notoginseng saponins(TSPN)on cerebral ischemia-reperfusion injury and oxygenglucose deprivation/reoxygenation(OGD/R)of cultured cortical neurons.Methods:The neuroprotective effect of TSPN was evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide(MTT)assay,flow cytometry and live/dead cell assays.The morphology of dendrites was detected by immunofluorescence.Middle cerebral artery occlusion(MCAO)was developed in rats as a model of cerebral ischemia-reperfusion.The neuroprotective effect of TSPN was evaluated by neurological scoring,tail suspension test,2,3,5-triphenyltetrazolium chloride(TTC)and Nissl stainings.Western blot analysis,immunohistochemistry and immunofluorescence were used to measure the changes in the Akt/mammalian target of rapamycin(mTOR)signaling pathway.Results:MTT showed that TSPN(50,25 and 12.5μg/m L)protected cortical neurons after OGD/R treatment(P<0.01 or P<0.05).Flow cytometry and live/dead cell assays indicated that 25μg/m L TSPN decreased neuronal apoptosis(P<0.05),and immunofluorescence showed that 25μg/m L TSPN restored the dendritic morphology of damaged neurons(P<0.05).Moreover,12.5μg/m L TSPN downregulated the expression of Beclin-1,Cleaved-caspase 3 and LC3 B-Ⅱ/LC3 B-Ⅰ,and upregulated the levels of phosphorylated(p)-Akt and p-mTOR(P<0.01 or P<0.05).In the MCAO model,50μg/m L TSPN improved defective neurological behavior and reduced infarct volume(P<0.05).Moreover,the expression of Beclin-1 and LC3 B in cerebral ischemic penumbra was downregulated after 50μg/m L TSPN treatment,whereas the p-mTOR level was upregulated(P<0.05 or P<0.01).Conclusions:TSPN promoted neuronal survival and protected dendrite integrity after OGD/R and had a potential therapeutic effect by alleviating neurological deficits and reversing neuronal loss.TSPN promoted p-mTOR and inhibited Beclin-1 to alleviate ischemic damage,which may be the mechanism that underlies the neuroprotective activity of TSPN.

Two new diterpenoid lactones isolated from Andrographis paniculata

In the present study, two new diterpenoid lactones, 3-deoxy-andrographoside(1) and 14-deoxy-15-methoxy-andrographolide(2), were isolated from the aerial parts of Andrographis paniculata. Their structures were elucidated by combination of NMR, MS, and chemical methods. The configurations of 1 and 2 were established based on the analysis of ROESY data and single crystal X-ray diffraction experiment.

Four new corynanthe-type alkaloids from the roots of Alstonia scholaris

Four new corynanthe-type alkaloids,meloslines C–F(1–4),together with four known ones(5–8)were isolated from the roots of Alstonia scholaris.Their structures including absolute configurations were elucidated by extensive spectroscopic analysis and electronic circular dichroism(ECD)calculation.Compounds 1 and 2 exhibited potent vasorelaxant activity on endothelium-intact renal arteries precontracted with KCl.

Discovery of Eucalyptin C,derived from the fruits of Eucalyptus globulus Labill.,as a novel selective PI3Kγinhibitor for immunosuppressive treatment

The fruits of Eucalyptus globulus Labill.are known to have a plenty of medicinal properties,such as anti-tumor,anti-inflammatory,and immunosuppressive activity.Our previous study found that the phloroglucinol-sesquiterpene adducts in the fruits of E.globulus were immunosuppressive active constituents,especially Eucalyptin C(EuC).Phosphoinositide 3-kinases-γ(PI3Kγ)plays a pivotal role in T cell mediated excessive immune responses.In this study,EuC was first discovered to be a novel selective PI3Kγinhibitor with an IC50 value of 0.9μmol·L^(−1) and selectivity over 40-fold towards the other PI3K isoforms.Molecular docking,molecular dynamics simulation,and cellular thermal shift assay showed that EuC bound to PI3Kγ.Furthermore,EuC suppressed the downstream of PI3Kγto induce the apoptosis and inhibit the activation of primary spleen cells derived from allergic contact dermatitis mice.This work highlights the role of the fruits of E.globulus as a source of bioactive plant with immunosuppressive activity.

A new triterpenoid glycoside from Vitex negundo

AIM:To investigate the chemical constituents of Vitex negundo.METHOD:Compounds were isolated by different chromatographic methods and their structures were elucidated on the basis of NMR spectroscopy.RESULTS:Four compounds were isolated and identified as 2α,3α,24-trihydroxyurs-12,20(30)-dien-28-oic acid-28-O-β-D-glucopyranosyl ester(1),corosolic acid(2),vulgarsaponin A(3) and 2α,3α,24-trihydroxyurs-12-en-28-oic acid-28-O-β-Dglucopyranosyl ester(4),respectively.CONCLUSION:Compound 1 is a new triterpenoid glycoside.

Alkaloid constituents from the fruits of Flueggea virosa

Three new indole alkaloids, flueindolines A–C(1–3), along with nine known alkaloids(4–12), were isolated from the fruits of Flueggea virosa(Roxb. ex Willd.) Voigt. Compounds 1 and 2 are two new fused tricyclic indole alkaloids possessing an unusual pyrido[1, 2-a]indole framework, and 3 presents a rare spiro(pyrrolizidinyl-oxindole) backbone. Their structures with absolute configurations were elucidated by means of comprehensive spectroscopic analysis, chemical calculation, as well as X-ray crystallography. Chiral resolution and absolute configuration determination of the known compounds 4, 10, and 11 were reported for the first time. The hypothetical biogenetical pathways of 1–3 were herein also proposed.