Long noncoding RNAs HAND2-AS1 ultrasound microbubbles suppress hepatocellular carcinoma progression by regulating the miR-873-5p/tissue inhibitor of matrix metalloproteinase-2 axis

BACKGROUND Increasing data indicated that long noncoding RNAs(lncRNAs)were directly or indirectly involved in the occurrence and development of tumors,including hepatocellular carcinoma(HCC).Recent studies had found that the expression of lncRNA HAND2-AS1 was downregulated in HCC tissues,but its role in HCC progression is unclear.Ultrasound targeted microbubble destruction mediated gene transfection is a new method to overexpress genes.AIM To study the role of ultrasound microbubbles(UTMBs)mediated HAND2-AS1 in the progression of HCC,in order to provide a new reference for the treatment of HCC.METHODS In vitro,we transfected HAND2-AS1 siRNA into HepG2 cells by UTMBs,and detected cell proliferation,apoptosis,invasion and epithelial-mesenchymal transition(EMT)by cell counting kit-8 assay,flow cytometry,Transwell invasion assay and Western blotting,respectively.In addition,we transfected miR-837-5p mimic into UTMBs treated cells and observed the changes of cell behavior.Next,the UTMBs treated HepG2 cells were transfected together with miR-837-5p mimic and tissue inhibitor of matrix metalloproteinase-2(TIMP2)overexpression vector,and we detected cell proliferation,apoptosis,invasion and EMT.In vivo,we established a mouse model of subcutaneous transplantation of HepG2 cells and observed the effect of HAND2-AS1 silencing on tumor formation ability.RESULTS We found that UTMBs carrying HAND2-AS1 restricted cell proliferation,invasion,and EMT,encouraged apoptosis,and HAND2-AS1 silencing eliminated the effect of UTMBs.Additionally,miR-873-5p targets the gene HAND2-AS1,which also targets the 3’UTR of TIMP2.And miR-873-5p mimic counteracted the impact of HAND2-AS1.Further,miR-873-5p mimic solely or in combination with pcDNA-TIMP2 had been transformed into HepG2 cells exposed to UTMBs.We discovered that TIMP2 reversed the effect of miR-873-5p mimic caused by the blocked signalling cascade for matrix metalloproteinase(MMP)2/MMP9.In vivo results showed that HAND2-AS1 silencing significantly inhibited tumor formation in mice.CONCLUSION LncRNA HAND2-AS1 promotes TIMP2 expression by targeting miR-873-5p to inhibit HepG2 cell growth and delay HCC progression.

α-Glucosidase Inhibitory Activities of Lutein and Zeaxanthin Purified from Green Alga Chlorella ellipsoidea

α-Glucosidase inhibitors are used therapeutically to treat type-2 diabetes mellitus. Through a bioassay-guided fractionation technique, three carotenoids,(all-E)-lutein,(all-E)-zeaxanthin and(9-Z)-zeaxanthin, were purified from the green alga Chlorella ellipsoidea, in which(all-E)-lutein and(9-Z)-zeaxanthin had potent α-glucosidase inhibitory activity. IC_(50) values of(all-E)-lutein and(9-Z)-zeaxanthin were 70 and 53.5 μmol L^(-1) against Saccharomyces cerevisiae α-glucosidase, respectively, with non-competitive inhibition. In addition, IC_(50) values of(9-Z)-zeaxanthin against Bacillus stearothermophilus and rat-intestinal α-glucosidase were 805.1 and 671.2 μmol L^(-1), respectively. The K_i values of(all-E)-lutein and(9-Z)-zeaxanthin against S. cerevisiae α-glucosidase were 78.1 and 16.5 μmol L^(-1), respectively. Therefore, C. ellipsoidea carotenoids might be utilized as a novel candidate to prevent type-2 diabetes mellitus related disorders in food and medical industry.

Antioxidant and α-glucosidase inhibitor activities of natural compounds isolated from Quercus gilva Blume leaves

Objective: To isolate and investigate antioxidant and α-glucosidase inhibitor compounds in the leaves of Quercus gilva Blume(Q. gilva).Methods: Dry leaves of Q. gilva were extracted with methanol and the methanolic extract was further separated by silica gel column chromatography using several solvents with increasing polarity. The antioxidant activities of the isolated compounds were evaluated using various in vitro assays: 1,1-diphenyl-2-picrylhydrazyl radical scavenging activity, hydrogen peroxide radical scavenging activity, β-carotene bleaching assay, and reducing power assay. The α-glucosidase inhibitory assay was conducted against α-glucosidase from Saccharomyces cerevisiae.Results: Three compounds were isolated and their structures were identii ed as catechin(1), epicatechin(2), and tiliroside(3) using an instrumental analysis. Compound 2 had higher antioxidant activity with inhibitory concentrations(IC50) of(22.55 ± 2.23) μmol/L than that of quercetin, which was used as the standard, with an IC50 of(28.08 ± 2.39) μmol/L, followed by compound 1 with IC50 of(40.86 ± 3.45) μmol/L. On the other hand, compound 3 had the lowest antioxidant activity with an IC50 of(160.24 ± 8.15) μmol/L. However, compound 3 had the highest α-glucosidase inhibitory activity with an IC50 of(28.36 ± 0.11) μmol/L, followed by compounds 1 and 2 with(168.60 ± 5.15) and(920.60 ± 10.10) μmol/L, respectively.Conclusions: The results obtained for the antioxidant activities and α-glucosidase inhibitory activities in a methanolic extract from the leaves of Q. gilva coni rmed the potential of this plant as a source of natural antioxidants and antidiabetic medicine.

1-Deoxynojirimycin Content and Alfa-Glucosidase Inhibitory Activity and Heat Stability of 1-Deoxynojirimycin in Silkworm Powder

Silkworm powder containing 1-deoxynojirimycin (DNJ) has α-glucosidase inhibitory activity and is promising as a complementary and alternative medicine (CAM) agent in Japan. Silkworm powder produced in Korea was extracted with 75% ethanol. The extract was derivatized with 9-fluorenylmethyl chloroformate (FMOC-Cl), and DNJ-FMOC content was measured by HPLC. Then, alfa-glucosidase inhibition by silkworm and mulberry powder in pig liver crude enzyme was assayed using 4-nitrophenyl-alfa-D-glucopyranoside as a substrate. Silkworm powder DNJ content (0.39 to 0.58%) was higher than that in mulberry powder (0.08 to 0.12%). The alfa-glucosidase inhibitory activity of silkworm powder was more potent than that of mulberry leaves and green tea. Silkworm powder DNJ was stable upon heating to 121?C for up to 15 min.

Identification of α-glucosidase inhibitors from Clinacanthus nutans leaf extract using liquid chromatography-mass spectrometry-based metabolomics and protein-ligand interaction with molecular docking

The present study used in vitro and in silico techniques, as well as the metabolomics approach to characterise α-glucosidase inhibitors from different fractions of Clinacanthus nutans. C. nutans is a medicinal plant belonging to the Acanthaceae family, and is traditionally used to treat diabetes in Malaysia. nHexane, n-hexane: ethyl acetate(1:1, v/v), ethyl acetate, ethyl acetate: methanol(1:1, v/v), and methanol fractions were obtained via partitioning of the 80% methanolic crude extract. The in vitro α-glucosidase inhibitory activity was analyzed using all the fractions collected, followed by profiling of the metabolites using liquid chromatography combined with mass spectrometry. The partial least square(PLS) statistical model was developed using the SIMCA P^+14.0 software and the following four inhibitors were obtained:(1) 4,6,8-Megastigmatrien-3-one;(2) N-Isobutyl-2-nonen-6,8-diynamide;(3) 1′,2′-bis(acetyloxy)-3′,4′-didehydro-2′-hydro-β, ψ-carotene; and(4) 22-acetate-3-hydroxy-21-(6-methyl-2,4-octadienoate)-olean-12-en-28-oic acid. The in silico study performed via molecular docking with the crystal structure of yeast isomaltase(PDB code: 3 A4 A) involved a hydrogen bond and some hydrophobic interactions between the inhibitors and protein. The residues that interacted include ASN259, HID295, LYS156, ARG335,and GLY209 with a hydrogen bond, while TRP15, TYR158, VAL232, HIE280, ALA292, PRO312, LEU313,VAL313, PHE314, ARG315, TYR316, VAL319, and TRP343 with other forms of bonding.

Isolation and screening of glucosidase inhibitors from Chinese medicines

Objective: To search for glucosidase inhibitors from Chinese medicines. Methods: Six kinds of widely-used Chinese medicines with the activity of decreasing blood glucose were prepared by the process of boiling, condensing, precipitating, exchanging with resins and rinsing. In vitro glucosidase inhibitory activities were examined by photometric bioassay derived from rats, yeast and almond of all the Chinese medicine extracts. Diabetic ICR mice models were established by intraperitoneal injection of STZ (200 mg/kg). To investigate the in vivo effect of lowering blood glucose, the mouse blood glucose level was assayed at 30 min after being given 2.5 g/kg starch and acarbose or varied concentrations of different constituents of some Chinese medicines by stomach tube. Results: The constituents of Sangye, Sangzhi, Sangbaipi, Dihuang and Yuzhu showed potent inhibitory activities against glucosidase. Furthermore, the first kind of constituents was proved to be beneficial in reducing blood glucose by in vivo glucose tolerance experiments. Conclusion: The constituents of Chinese medicines with reducing blood glucose effect have been discovered, thus providing a clue to novel drugs.

辣椒叶α-葡萄糖苷酶抑制剂的提取及稳定性研究

辣椒叶中含有在小肠中延缓糖分分解吸收的α-葡萄糖苷酶抑制剂,以辣椒叶粉为原料,乙醇为提取溶剂,在单因素(液料比、乙醇体积分数、提取温度和提取时间)试验的基础上设计响应面试验,优化提取α-葡萄糖苷酶抑制剂的工艺,并探索α-葡萄糖苷酶抑制剂在提取后真空浓缩过程中的温度、食品加工过程中的温度、强酸条件下的稳定性。结果表明,辣椒叶中α-葡萄糖苷酶抑制剂的最佳提取条件为:液料比10∶1、乙醇体积分数35%、提取温度26℃、提取时间5 h;提取液在真空浓缩过程中温度控制在50℃以下相对稳定,而在加工特性研究中发现,α-葡萄糖苷酶抑制剂对高温比较敏感,而在pH 2.0~6.0范围内稳定性良好。研究结果可为辣椒叶资源的高值化开发利用提供理论依据。

药桑、两色金鸡菊、刺山柑提取物对α-葡萄糖苷酶的抑制作用研究

以三种新疆特色食药两用资源药桑、两色金鸡菊、刺山柑为研究对象,以临床糖尿病常用的药物阿卡波糖为阳性对照,用经典α-葡萄糖苷酶活性测定方法,对其水提物及醇提物进行酶抑制活性筛选,并对其中抑制作用最强的提取物进行了酶促反应动力学分析。药桑、两色金鸡菊、刺山柑提取物对α-葡萄糖苷酶均有明显的抑制作用,药桑醇提物IC_(50)为2.636μg·mL^(-1)、药桑水提物IC50为7.948μg·mL^(-1)、两色金鸡菊醇提物IC_(50)为0.000645μg·mL^(-1)、两色金鸡菊水提物IC_(50)为6.962μg·mL^(-1)、刺山柑醇提物IC_(50)为78.11μg·mL^(-1)、刺山柑水提物IC50为88.5μg·mL^(-1)、阿卡波糖IC_(50)为24.68μg·mL^(-1);由酶动力学实验结果得到,两色金鸡菊醇提物对α-葡萄糖苷酶的抑制作用表现为可逆竞争性抑制。两色金鸡菊及药桑的水及醇提物具有较好的α-葡萄糖苷酶抑制活性,可作为潜在的抑制α葡萄糖苷酶、降低餐后血糖的食药两用资源,具有较高的研究价值。

贵州废弃烟叶中具有α-糖苷酶抑制活性的多酚类化合物的分离纯化与结构鉴定

为了探究贵州废弃烟叶在降低血糖方面的物质基础,以贵州废弃烟叶为原料,通过提取、浓缩、硅胶柱层析、凝胶柱层析等技术方法从其乙醇提取物的石油醚中分离纯化获得9个多酚类单体化学成分,通过ESI-MS、^(1)H-NMR、^(13)C-NMR、DEPT等现代波谱学检测解析技术对所有得到的化合物进行了结构鉴定,被鉴定的9个多酚类单体化合物分别为Chlorogenicacid(1)、Rutin(2)、5,7,4'-trihydroxy-3,3'-dimethoxyflavone(3)、5,7-dihydroxyl-6,8,4'-trimethoxylflavone(4)、Kaempferol-3-methyl ether(5)、Scosoletin(6)、Dihydroferulic acid methyl ester(7)、2-(4-hydroxyphenyl)ethanol(8)、1,2,4,5-tetrahydroxybenzene(9)。继续采用PNPG法测定多酚类单体化合物的α-糖苷酶抑制活性,结果显示化合物9具有显著的抑制α-糖苷酶的活性,且优于阳性药阿卡波糖,这表明化合物9具有成为α-糖苷酶抑制剂的潜力,也为进一步探讨贵州废弃烟叶多用途和研制天然α-糖苷酶抑制剂产品奠定了科学依据。

多金属氧酸盐类α-葡萄糖苷酶抑制剂的研究进展

α-葡萄糖苷酶在淀粉转化为葡萄糖的过程中发挥着重要作用,而抑制α-葡萄糖苷酶活性是控制餐后血糖升高的有效途径。对α-葡萄糖苷酶抑制剂的抑制机理和研究进展进行综述,并重点概述了多金属氧酸盐(polyoxometalates,POMs)作为α-葡萄糖苷酶抑制剂的研究成果。

瑞格列奈联合α-葡萄糖苷酶抑制剂治疗老年T2DM患者的效果观察

目的观察分析瑞格列奈联合α-葡萄糖苷酶抑制剂治疗老年2型糖尿病(T2DM)患者的效果。方法98例老年T2DM患者,以数字号形式随机分为对照组和观察组,每组49例。对照组患者行瑞格列奈治疗,观察组行瑞格列奈联合α-葡萄糖苷酶抑制剂治疗。比较两组患者临床疗效以及治疗前后的糖化血红蛋白、空腹血糖、餐后2 h血糖、空腹胰岛素(FINS)、胰岛素抵抗指数(HOMA-IR)、胰高血糖素样肽-1(GLP-1)水平。结果观察组治疗总有效率93.88%高于对照组的75.51%,差异具有统计学意义(χ^(2)=6.376,P=0.012<0.05)。治疗后,观察组患者糖化血红蛋白(6.15±0.43)%、空腹血糖(5.86±0.70)mmol/L、餐后2 h血糖(7.11±0.32)mmol/L均低于对照组的(7.27±0.66)%、(7.14±0.94)mmol/L、(8.88±0.41)mmol/L,差异均具有统计学意义(P<0.05)。治疗后,观察组患者FINS(14.17±0.59)mU/L、GLP-1(5.07±0.26)pmol/L高于对照组的(9.97±0.93)mU/L、(3.14±0.24)pmol/L,HOMA-IR(3.31±0.53)低于对照组的(4.44±0.66),差异均具有统计学意义(P<0.05)。结论老年T2DM患者行瑞格列奈联合α-葡萄糖苷酶抑制剂治疗,疗效显著,可以有效控制患者血糖水平,胰岛素分泌情况改善,值得推广。

左炔诺孕酮联合miRNA-21-5p抑制剂对子宫内膜癌细胞增殖、转移的作用及机制

目的利用左炔诺孕酮(LNG)和miRNA-21-5p抑制剂(inhibitor)联合靶向多发性肿瘤抑制基因磷酸酶基因(PTEN)评估对子宫内膜癌细胞增殖、转移的作用。方法将实验用人子宫内膜癌细胞分为Control组、LNG处理组、LNG处理+miR-21 NC组和LNG处理+miR-21 inhibitor组;免疫组化检测LNG治疗前后子宫内膜癌患者内膜组织中PTEN表达;CCK8和流式细胞仪筛选LNG最佳作用浓度和时间;实时荧光定量(qRT)-聚合酶链反应(PCR)法检测miR-21-5p inhibitor处理后miR-21-5p mRNA表达水平;LNG联合miR-21-5p inhibitor处理后CCK8检测增殖,流式检测凋亡,Transwell检测侵袭,划线检测迁移,Western印迹检测细胞中PTEN、磷脂酰肌醇3-激酶(PI3K)、p-PI3K、丝氨酸/苏氨酸激酶(AKT)和p-AKT蛋白表达水平。结果与治疗前比,LNG治疗后子宫内膜组织中PTEN表达水平显著升高(P=0.000)。筛选出LNG最佳浓度为100μmol/L,时间为24 h。miR-21-5p inhibitor处理后miR-21-5p表达显著降低(P<0.05)。与Control组相比,LNG组处理后细胞凋亡及PTEN表达显著升高,细胞迁移、侵袭能力及细胞活力显著下降(P<0.05),miR-21-5p、p-AKT/AKT、p-PI3K/PI3K表达也明显下降(P<0.05);与LNG组相比,LNG+miR-21-5p inhibitor组细胞活力、细胞凋亡、迁移、侵袭能力、miR-21-5p表达、p-AKT/AKT、p-PI3K/PI3K明显下降,PTEN表达则明显升高(P<0.05)。结论LNG联合miR-21-5p inhibitor具有协同抑制子宫内膜癌细胞增殖、转移的作用,此过程与靶向上调PTEN并抑制PI3K/AKT通路活化相关。

太行菊黄酮对α-葡萄糖苷酶活性的抑制作用

为研究太行菊醇提物不同极性萃取相中黄酮对α-葡萄糖苷酶活性的影响及其抑制作用的动力学特征,采用萃取法制得太行菊黄酮的乙酸乙酯相、正丁醇相、残余水相和石油醚相,使用体外(PNPG)法建立抑制α-葡萄糖苷酶活性的筛选模型,通过酶促反应动力学绘制Lineweaver-Burk曲线,分析太行菊黄酮对α-葡萄糖苷酶作用的抑制类型。太行菊不同极性萃取物对α-葡萄糖苷酶呈现不同程度的抑制作用,而且抑制活性与黄酮的质量浓度之间呈现明显的剂量效应关系。其中乙酸乙酯相和正丁醇相中黄酮质量分数及α-葡萄糖苷酶抑制活性均显著高于其他萃取相,且高于阿卡波糖,而残余水相和石油醚相中黄酮对α-葡萄糖苷酶的抑制活性低于阿卡波糖。酶抑制活性乙酸乙酯(IC_(50)=1.01 mg/mL)<正丁醇(IC_(50)=1.25 mg/mL)<阿卡波糖(IC_(50)=1.47 mg/mL)<残余水相(IC_(50)=1.77 mg/mL)<石油醚(IC_(50)=2.12 mg/mL)。酶抑制动力学研究发现,乙酸乙酯相和正丁醇相中太行菊黄酮对α-葡萄糖苷酶是混合型抑制类型中竞争与非竞争关系;残余水相和石油醚相中太行菊黄酮对α-葡萄糖苷酶是竞争与反竞争的混合抑制类型。太行菊醇提物不同极性萃取相黄酮均具有一定的α-葡萄糖苷酶的抑制活性,在开发成辅助降血糖的保健食品或药品方面具有良好的潜力,有望将太行菊醇提物乙酸乙酯相和正丁醇相黄酮开发为新型α-葡萄糖苷酶抑制剂。

The new K_V3.4 inhibitor BDS-I[1–8] as a potential pharmacological opportunity in Alzheimer’s disease therapy

Alzheimer's disease(AD)is the most common neurodegenerative disorder and the first cause of dementia in the elderly,with no treatment able to prevent or to block disease progression.AD is characterized by memory impairment and cognitive dysfunction,followed in the late phases of the disease by severe neurodegeneration and neuronal death.The amyloid-β(Aβ)peptide,generated upon the processing of the amyloid precursor protein,is considered the main initiator of AD pathology.Indeed,Aβpeptides,which aggregate and accumulate to form extracellular plaques and intraneuronal deposits.

金露梅中一种α-葡萄糖苷酶抑制剂的提取富集及活性研究

本研究采用AB-8大孔吸附树脂、半制备高效液相色谱对金露梅枝叶中槲皮素-7-O-β-D-葡糖苷酸提取分离,并通过13 C NMR鉴定其化学结构,最后采用以4-硝基酚-α-D-吡喃葡萄糖苷(pNPG)为底物的酶抑制剂筛选模型检测其对α-葡萄糖苷酶的抑制活性和类型。结果显示:槲皮素-7-O-β-D-葡糖苷酸分布在20%乙醇大孔吸附树脂(AB-8)洗脱液中,采用半制备高效液相色谱和高效液相色谱分离纯化得槲皮素-7-O-β-D-葡糖苷酸2481.8 mg,纯度为97.95%。活性检测结果表明,槲皮素-7-O-β-D-葡糖苷酸对α-葡萄糖苷酶的最大抑制率为94.67%,IC 50为0.259 mmol/L,抑制率显著高于阳性对照药物阿卡波糖,且抑制剂类型为竞争性抑制。

冠突散囊菌发酵鲜桑叶对其黄酮抑制α-葡萄糖苷酶活性的影响

为提高桑叶中黄酮类物质含量并改善其α-葡萄糖苷酶抑制活性,采用冠突散囊菌(Eurotium cristatum CY-1)进行鲜桑叶固态发酵的研究。研究结果表明,E.cristatum CY-1可以新鲜桑叶为发酵基质进行良好的生长。以30 g鲜桑叶(含水量76.92%)为发酵基质进行固态发酵时,第8天菌体生物量达到378.2 mg。随着发酵的进行,桑叶黄酮提取物(mulberry leaf flavonoids,MLF)的含量在第8天时升至最高值,为3.289 mg/g干桑叶,相对于未发酵桑叶提高了78.7%。MLF对α-葡萄糖苷酶的半数抑制浓度(IC_(50))随着发酵时间的延长而显著降低,其中经E.cristatum CY-1发酵10 d的桑叶MLF和未发酵桑叶的MLF的IC_(50)值分别为4.925μg/mL和25.995μg/mL。综上,冠突散囊菌的发酵不仅可以有效提高桑叶黄酮的含量,还可以提高其对α-葡萄糖苷酶的抑制效率。

A novel thioredoxin reductase inhibitor inhibits cell growth and induces apoptosis in HL-60 and K562 cells

Human thioredoxin reductase (TrxR) system is associated with cancer cell growth and anti-apoptosis process. Effects of 1,2-bis(1,2-benzisoselenazolone-3(2H)-ketone)ethane (BBSKE),a novel TrxR inhibitor,were investigated on human leu-kemia cell lines HL-60 and K562. BBSKE treatment induced cell growth inhibition and apoptosis in both cell lines. Apoptosis induced by BBSKE is through Bcl-2/Bax and caspase-3 pathways. Ehrlich's ascites carcinoma-bearing mice were used to inves-tigate the anti-tumor effect of BBSKE in vivo. Tumor-bearing mice treated with BBSKE showed an increase of life span with a comparable effect to cyclophosphamide (CTX). These results suggest a potential usage of BBSKE as a therapeutic agent against non-solid tumors.

Synthesis and Crystal Structure of a Novel Ethyl 5-(4-(2-Phenylacetamido)phenyl)-1H-pyrazole-3-carboxylate as an Acrosin Inhibitor

The title compound （ethyl5-（4-（2-phenylacetamido）phenyl）-lH-pyrazole-3-carboxylate, C20H19N3O3） was synthesized by the reaction of Claisen condensation, cyclization, reduction and acylation. The structure was characterized by X-ray diffraction, MS, NMR and IR. It belongs to the monoclinic system, space group C2/c with a = 22.723（9）, b = 9.324（4）, c = 18.890（8） A, β = 114.259（6）°, V = 3649（3） A^3, Dc = 1.272 Mg·m^3, Z = 8, Mr = 349.38, p = 0.087 mm^-1, F（000） = 1472, the final R = 0.0615 and wR = 0.1643. The biological test shows that the title compound has a moderate acrosin inhibition activity.

A new angiotensin-converting enzyme inhibitor from Peperomia pellucida(L.) Kunth

Objective:To isolate,identify,and evaluate a new angiotensin-converting enzyme inhibitor from Peperomia pellucida(L.)Kunth herbs.Methods:A dried sample of Peperomia pellucida herb was successively macerated with n-hexane and ethyl acetate.The ethyl acetate extract solution was evaporated to obtain the crude extract.Vacuum liquid column chromatography and thin layer chromatography were performed to obtain two pure compounds.Then,both compounds were elucidated and identified using the spectroscopic method.Angiotensin-converting enzyme inhibitory activity studies of both compounds were determined using angiotensin-converting enzyme kit WST-1 with spectrophotometer microplate reader 96-well at 450 nm wavelength.Results:Two bioactive compounds were successfully isolated from Peperomia pellucida herb,including a new compound of 2,3,5-trimethoxy-9-(12,14,15-trimethoxybenzyl)-1 H-indene and pellucidin A.Both compounds demonstrated angiotensin-converting enzyme inhibitory activity,with IC50 values of 72 μM(27.95 μg/mL)and 1 1μM(4.4 μg/mL),respectively.Conclusions:In the present study,two active angiotensin-converting enzyme inhibitors were successfully isolated and purified from Peperomia pellucida which is used as an antihypertensive in traditional medicine,and support its use as an angiotensin-converting enzyme-inhibiting drug.

Synthesis of 1-aryl-3-(3,4-dihydro-2H-chromen-5-yl) ureas as TNF-αinhibitors

A new series of compounds, 1-aryl-3-（3,4-dihydro-2H-chromen-5-yl） ureas, have been synthesized and their structures were confirmed by FAB-MS and IH NMR. The preliminary pharmacological screening showed that these compounds inhibited TNF-α production in lipopolysaccharide （LPS）-stimulated THP-1 cells.