Analysis of Patent Application Status of Scutellaria Barbata Industrial Chain Based on Patent Data

Objective To analyze patent application status of Scutellaria Barbata industrial chain and provide some suggestions for its patent application and product development.Methods Patent data were collected through IncoPat patent analysis system.Meanwhile,the patent analysis method combined with text mining method was adopted to analyze the situation and development trend of patent application in China’s Scutellaria Barbata industrial chain by using pie chart,bubble chart,trend chart and other visual charts to display the results.Results and Conclusion The patent application of Scutellaria Barbata in China mainly experienced three stages:Slow development,rapid development,and recession period.The number of patents is large,but the authorization rate is low.Individuals and enterprises are the main applicants for patent applications.Product development is involved in the whole industrial chain,but it basically focuses on its efficacy in downstream drugs,health food and other aspects.Therefore,government should enhance the awareness of patent protection,encourage collaborative innovation in industry-university-research to promote the combination of basic research and market application.Besides,it should provide theoretical support to tackle the problem of short board products,which can promote the transformation of scientific and technological achievements and contribute to the upgrading of Scutellaria Barbata industrial chain.

Scutellaria barbata attenuates diabetic retinopathy by preventing retinal inflammation and the decreased expression of tight junction protein

AIM： To observe the attenuation of ethanol extract of Herba Scutellaria barbata （SE） against diabetic retinopathy （DR） and its engaged mechanism. METHODS： C57BL/6J mice were intraperitoneally injected with streptozotocin （STZ, 55 mg/kg） for 5 consecutive days to induce diabetes, The diabetic mice were orally given with SE （100, 200 mg/kg） for lmo at lmo after STZ injection. Blood-retinal barrier （BRB） breakdown was detected by using Evans blue permeation assay. Real-time polymerase chain reaction （RT-PCR）, Western blot and immunofiuorescence staining were used to detect mRNA and protein expression. Enzyme-linked immunosorbent assay （ELISA） was used to detect serum contents of tumor necrosis factor-e （TNF-a） and interleukin （IL）-II. RESULTS： SE （100, 200 mg/kg） reversed the breakdown of BRB in STZ-induced diabetic mice. The decreased expression of retinal claudin-1 and claudin-19, which are both tight junction （T J） proteins, was reversed by SE. SE decreased the increased serum contents and retinal mRNA expression of TNF-a and IL-113. SE also decreased the increased retinal expression of intercellular cell adhesion molecule-1 （ICAM-1）. SE reduced the increased phosphorylation of nuclear factor kappa B （NFKB） p65 and its subsequent nuclear translocation in retinas from STZ- induced diabetic mice. Results of Western blot and retinal immunofluorescence staining of ionized calcium-binding adapter molecule 1 （Ibal） demonstrated that SE abrogated the activation of microglia cells in STZ-induced diabetic mice. CONCLUSION： SE attenuates the development of DR by inhibiting retinal inflammation and restoring the decreased expression of TJ proteins including claudin-1 and claudin-19.

Attenuation of Scutellaria barbata flavonoids on cortical cytoplasm apoptotic factors disorders induced by complex Aβ_(25-35) in rats

OBJECTIVE To investigate the effect of SBF on cortical cytoplasm apoptotic factors disturbances induced by complex Aβ25-35in rats.METHODS The cerebral injuries model was established by rats received intracere-broventricular injection of RHTGF-β1,Aβ25-35and Al Cl3and then accepted SBF treatment.All the rats were sacrificed by decapitation for indicators detection at last the drug treatment.Western blotting method was for caspase-3 protein expression and RT-PCR method detected cytochrome c,apoptotic protease activating factor-1(Apaf-1),caspase-9 m RNA expression in cortical cytoplasm.RESULTS The protein expression of caspase-3in cortical cytoplasm of rats was assayed by Western blotting.The results indicated that compared with the sham group,the caspase-3 protein expression of cortical cytoplasm in Aβgroup was significantly increased(P<0.01).However,the increased expression can be obviously reversed by SBF at doses of 35,70 and 140mg·kg-1,as compared with model group(P<0.01).The Cyt-C,Apaf-1 and caspase-9 m RNA expressions in cortical cytoplasm of rats were determined by RT-PCR.The results indicated that compared with the sham group,the Cyt-C Apaf-1 and caspase-9 m RNA relative expressions of cortical cytoplasm in Aβgroup was significantly increased(P<0.01).However,these increased expressions can be differently reversed by SBF at doses of 35,70 and 140 mg·kg-1,as compared with model group(P<0.01).CONCLUSION SBF can definitely improve rats′cortical cytoplasm apoptotic factors disorders induced by complex Aβ25-35,which maybe benefit for treatment of degenerative disease.

Chemical profiling of Scutellaria barbata by ultra high performance liquid chromatography coupled with hybrid quadrupole-orbitrap mass spectrometry

An ultra high performance liquid chromatography coupled with hybrid quadrupole-orbitrap mass spectrometry （UHPLC-quadrupole-orbitrap MS） method was developed to systematically analyze chemical constituents of Scutellaria barbata D. Don. The 70% methanol extract was separated on an Agilent Eclipse Plus Cl8 column （1.8μm, 150 mm×2.1 mm）, and eluted with a gradient of methanol-acetonitrile-water containing 0.1% formic acid at a flow rate of 0.25 mL/min. Constituents were identified by HRMS in the negative ion mode using both full scan and two-stage threshold-triggered mass modes. A total of 56 compounds, including 20 free flavonoids, 20 flavonoid O-glycosides, 2 flavonoid C-glycosides, 4 phenylethanoid glycosides, and 10 phenolic compounds were identified by analyzing their high resolution mass spectral data. Among them, 8 flavonoids and 2 phenylethanoid glycosides were unambiguously identified by comparing with reference standards. This study demonstrates that hybrid quadrupole-orbitrap mass spectrometry is a powerful tool in structural identification of unknown compounds in comolicated herbal extracts.

Two New neo-Clerodane Diterpenoids from Scutellaria barbata

Two new neo-clerodane diterpenoids, 6,7-dibenzoyloxybarbatin C （1, named barbatin D） and 6-（2-acetoxy-3-methylbutanoloxy）-7-（2-carbonyl-3-methylbutanoyloxy） barbatin C （2, named barbatin E） were isolated from the whole plant of Scutellaria barbata D. Don. Their structures were elucidated by spectroscopic methods including extensive 1 D and 2D NMR analyses. In vitro, compounds 1-2 showed cytotoxic activities against three human cancer lines, namely, HONE-1 nasopharyngeal, KB oral epidermoid carcinoma, and HT29 colorectal carcinoma cells, and with IC50 values in the range of 3.5-6.7μM.

Scutellaria barbata D.Don Inhibits Colorectal Cancer Growth via Suppression of Wnt/β-Catenin Signaling Pathway

Objective： To investigate the effect of the ethanol extract of Scutellaria barbata D. Don（EESB） on colorectal cancer（CRC） growth and Wnt/β-catenin signaling pathway in vivo and in vitro. Methods： In vivoexperiment, CRC xenograft mouse model was constructed with injection of HT-29 cells. Following xenograft implantation, twenty mice were randomly divided into EESB-treated group（n=10） and control group（n=10） by a random number table, and were given with intra-gastric administration of 2 g/kg EESB or saline, 5 days a week for 16 days, respectively. At the end of experiment, tumors were removed and weighed by electronic scales. The proliferation biomarker Ki-67 of tumor was evaluated by immunohistochemistry（IHC） assay. In vitro study, HT-29 cells were treated with 0, 0.5, 1.5, 2.5 mg/m L EESB for 24 h. At the end of the treatment, the viability and survival of HT-29 cells were determined by methylthiazolyldiphenyl-tetrazolium bromide（MTT） assay and colony formation assay, respectively. The m RNA expression of c-Myc, Survivin and adenomatous polyposis coli（APC） was examined by reverse transcription-polymerase chain reaction（RT-PCR） both in tumor tissues of CRC xenograft mice and HT-29 cells. Protein expression of c-Myc, Survivin, APC, and β-catenin as well as β-catenin phosphorylation level were evaluated by IHC assay or Western blotting. Results： EESB significantly reduced tumor weight in CRC xenografts mice, compared with the control group（P〈0.05）. IHC assay showed that EESB significantly inhibited protein expression of Ki-67 in tumor tissues（P〈0.05）. MTT assay showed that EESB significantly reduced HT-29 cell viability in a dose-dependent manner（P〈0.05）. Colony formation assay showed that EESB dose-dependently decreased the survival of HT-29 cells（P〈0.05）. In addition, RT-PCR assay showed that EESB decreased the m RNA expression of c-Myc and Survivin and increased APC expression, both in tumor tissues of CRC xenograft mice and HT-29 cells（P〈0.05）. IHC assay or Western blotting showed that EESB decreased protein expression of β-catenin, c-Myc and Survivin, as well as increased APC expression and β-catenin phosphorylation in tumor tissues or HT-29 cells（P〈0.05）. Conclusions： EESB significantly reduced tumor growth in CRC xenografts mice, and inhibited the viability and survival of HT-29 cells. EESB could suppress the activation of the Wnt/β-catenin pathway, which might be one of the mechanisms whereby Scutellaria barbata D. Don exerts its anticancer activity.

不同配伍比例的半枝莲-白花蛇舌草药对对肝癌细胞增殖活性的影响

目的:研究不同配伍比例的半枝莲-白花蛇舌草药对(简称半白药对,SB-OD)对肝癌细胞株(MHCC97H细胞和Huh7细胞)增殖活性的抑制作用。方法:运用CCK-8法观察不同配伍比例的半白药对(半白1∶1,半白2∶1,半白1∶2)干预MHCC97H和Huh7细胞24 h,分别计算其IC_(50)值;并应用细胞平板克隆形成实验检测细胞克隆形成能力,分析不同配伍比例的半白药对对MHCC97H和Huh7细胞增殖活性的影响。结果:不同配伍比例的半白药对作用MHCC97H和Huh7细胞后的生存活力明显下降(P<0.01),并呈浓度依赖性,其中半白1∶1组作用于MHCC97H和Huh7细胞的IC_(50)值分别为6.69 mg/mL和7.95 mg/mL;半白2∶1组作用于MHCC97H和Huh7细胞的IC_(50)值分别为2.58 mg/mL和3.43 mg/mL;半白1∶2组作用于MHCC97H和Huh7细胞的IC_(50)值分别为15.04 mg/mL和16.60 mg/mL。不同配伍比例的半白药对干预MHCC97H和Huh7细胞后的克隆形成率明显降低(P<0.01)。结论:不同配伍比例的半白药对均能够抑制肝癌MHCC97H和Huh7细胞的增殖活性,2∶1配伍比例的抑制作用最佳,可作为半白药对抗肿瘤研究的实验基础。

半枝莲抗肿瘤的信号通路研究进展

半枝莲在中国药用历史悠久,经现代研究证实含有黄酮类、多糖类、二萜类等多种抗肿瘤有效成分。梳理近年来半枝莲及其活性成分靶向肿瘤的各个信号通路的相关文献发现,半枝莲及其活性成分通过调控磷脂酰肌醇3-激酶/蛋白激酶B(PI3K/Akt)、酪氨酸蛋白激酶/信号转导和转录激活因子(JAK/STAT)、Wnt/β-连环蛋白(Wnt/β-cate-nin)、丝裂原活化蛋白激酶(MAPK)、半胱氨酸蛋白酶(Caspase)途径、核因子-κB(NF-κB)、蛋白53(p53)和Hedgehog等多条信号通路,发挥抑制肿瘤细胞增殖、诱导肿瘤细胞凋亡、降低迁移和侵袭能力、抗肿瘤血管形成、调节机体的免疫功能等作用,达到抗肿瘤效应。广泛应用于结肠癌、肺癌、肝癌、乳腺癌等多种肿瘤疾病的治疗。研究以细胞信号通路为切入点,总结半枝莲抗肿瘤的作用机制,以期为深入挖掘半枝莲抗肿瘤机制及其临床应用提供参考。

整合网络药理学和体外实验探究夏枯草-半枝莲药对治疗乳腺癌的作用及机制

目的采用网络药理学和体外细胞实验探究夏枯草-半枝莲药对抗乳腺癌的作用机制。方法运用中药系统药理学数据库与分析平台筛选出夏枯草-半枝莲药对的有效成分和靶点;利用GeneCards、OMIM数据库找到乳腺癌靶点,进而构建药物-活性成分-关键靶点网络和蛋白-蛋白相互作用(PPI)网络;运用R语言进行GO功能和KEGG通路富集分析以及生存分析;将筛选出的活性成分和核心靶点进行分子对接验证;采用CCK-8法检测细胞活力;EdU、流式实验检测细胞增殖和凋亡情况;Western blot法检测p-AKT1、AKT1、β-catenin和c-MYC的蛋白表达水平。结果通过数据分析共筛选出有效成分36个,交集靶点105个,其核心成分是槲皮素、木犀草素、山奈酚、汉黄芩素、黄芩素;通过PPI和生存分析得出其关键靶点是AKT1、ESR1、CASP3、MYC;GO分析共包含4303条富集结果,KEGG分析共包含232条通路;分子对接显示核心成分与关键靶点均具有较强的结合能力。细胞实验证明,核心活性成分槲皮素可以抑制乳腺癌细胞的增殖并促进其凋亡(P<0.05),下调p-AKT1、β-catenin和c-MYC蛋白的表达水平(P<0.05)。结论夏枯草-半枝莲药对中活性成分槲皮素可能通过AKT1/β-catenin信号通路来发挥作用,为其治疗乳腺癌的作用机制研究提供了科学参考。

白花蛇舌草-半枝莲药对治疗胃癌的物质基础和作用机制研究进展

胃癌是消化系统的常见恶性肿瘤之一,好发于中老年人群。中医认为胃癌是由津亏热结、癌毒胶结于胃腹而形成的一种瘤瘕,在临床中常用清热解毒类药物进行治疗。白花蛇舌草-半枝莲药对具有清热解毒、活血化瘀、消痈散结、抗炎止痛的作用,可治疗胃癌。现代药理学研究证实,白花蛇舌草-半枝莲药对可通过诱导细胞凋亡、抑制细胞增殖、抑制血管生成、改善免疫微环境、下调端粒酶活性等途径起到抗胃癌的作用。本文对白花蛇舌草-半枝莲药对配伍后活性成分抗胃癌的机制进行综述,为白花蛇舌草-半枝莲药对的临床用药和抗胃癌新药研发提供理论依据和参考。

基于TCGA研究左右半结肠癌基因表达差异及苦参-大血藤-半枝莲作用机制

【目的】探讨左半结肠癌与右半结肠癌的基因表达差异及大肠癌核心药对苦参-大血藤-半枝莲作用于左右半结肠癌的机制差异。【方法】下载134例左半结肠癌及194例右半结肠癌患者癌症基因组图谱(TCGA)的转录组数据,应用R软件实现2组差异基因分析及京都基因与基因组百科全书(KEGG)通路富集分析;通过BATMAN-TCM数据库获取苦参-大血藤-半枝莲药对的活性成分及靶点,基于左右半结肠癌差异基因,分别进行药对-左/右半结肠癌KEGG富集分析、蛋白质互作(PPI)网络构建,比较药对治疗左、右半结肠癌富集的生物信号通路差异及关键靶点差异。【结果】左半结肠癌与右半结肠癌相对于正常癌旁组织共同的差异表达基因共6051个,左半结肠癌特异性的差异表达基因共1958个,右半结肠癌特异性的差异表达基因共1739个;左半结肠癌特异性KEGG富集通路14条,右半结肠癌特异性KEGG富集通路23条。苦参-大血藤-半枝莲药对活性化合物共85个,对应的靶点合计469个,药对-左半结肠癌靶点富集于10条KEGG信号通路,关键靶点为DRD2、CACNA1C、HTR3A、COMT、TH,药对-右半结肠癌靶点富集于1条KEGG信号通路,核心靶点为HTR3A、DRD2、TH、AGT、GRIN2B。【结论】左半结肠癌与右半结肠癌存在基因表达差异:左半结肠癌与免疫功能异常、AMPK信号通路异常等机制有关,右半结肠癌与中性粒细胞外陷阱形成、酒精中毒、Hippo信号通路异常等机制有关。除调控细胞周期及必需氨基酸代谢等机制外,苦参-大血藤-半枝莲药对对调节左半结肠癌肠道内分泌功能、抑制右半结肠癌炎症反应具有特异性作用,亦可能对结肠癌患者具有情绪调控作用。

广西产半枝莲中黄酮类化学成分研究

目的:对广西产半枝莲的黄酮类成分进行研究。方法:综合利用正反相柱层析、MCI柱层析、HPLC等色谱分离技术对半枝莲全草进行提取分离,并通过波谱数据进行结构鉴定。结果:从半枝莲中共分离和鉴定了5个化合物,分别为白杨素(1)、芹菜素(2)、木犀草素(3)、千层纸素(4)、柚皮素(5)。结论:分离得到的化合物类型均为黄酮类化合物,可为广西半枝莲的黄酮成分分析提供一定的参考。

基于网络药理学和分子对接的半枝莲黄酮类成分治疗肝细胞癌的机制研究

目的网络药理学方法探究半枝莲黄酮类成分治疗肝细胞癌的作用机制及分子对接技术验证。方法通过TCMSP、SwissTargetPrediction、OMIM、BioGPS等数据库筛选黄酮类成分、肝特异性靶点;构建肝特异性靶点蛋白互作网络、筛选核心模块和基因;进行肝特异性靶点生物通路富集分析;将黄酮类成分和核心蛋白靶点在SwissDock平台进行分子对接。结果黄酮类成分36个,肝特异性靶点135个,核心基因4个;关键生物通路均与肝细胞癌的增殖抑制相关。黄酮成分与核心靶点有较强的结合活性。结论半枝莲黄酮类成分抗肿瘤作用可能是通过多成分-多靶点阻滞肝癌细胞的有丝分裂G1/S细胞周期,抑制肝细胞癌增殖。

半枝莲抗肝癌活性部位的化学成分研究

前期研究发现,半枝莲(Scutellaria barbata)全草醇提物的乙酸乙酯萃取部位经大孔吸附树脂处理,其70%乙醇洗脱部位具有较好的抗肝癌活性。为明确其活性成分,该研究采用硅胶柱色谱、Sephadex LH-20柱色谱、制备TLC、半制备液相色谱等对活性部位进行分离和纯化,运用多种波谱分析方法鉴定了单体化合物结构,并利用CCK-8法评价了所有单体化合物对人肝癌HepG2细胞体外增殖抑制活性,同时利用分子对接技术考察了活性最好的化合物与肝癌靶标的结合情况。结果表明:(1)从该活性部位共分离得到14个化合物,包括12个新克罗烷型二萜类化合物和2个黄酮类化合物,分别鉴定为scutefolide C(1)、6-乙酰氧基-7-烟酸酰氧基半枝莲碱G(2)、scutestrigillosin D(3)、scutehenanine D(4)、半枝莲碱A(5)、半枝莲碱B(6)、7-烟酸酰氧基半枝莲碱H(7)、半枝莲碱N(8)、半枝莲碱Y(9)、barbatin A(10)、barbatin B(11)、barbatin D(12)、5,7,6′-三羟基-2′-甲氧基黄酮醇(13)和5,8-二羟基-6,7-二甲氧基黄酮(14)。其中,化合物1-3、13、14为首次从该植物中分离得到。(2)活性测试结果显示,化合物4、7、10-12表现出较弱的HepG2细胞增殖抑制活性,化合物6的细胞增殖抑制活性和阳性对照(顺铂)活性接近,而化合物5表现出比顺铂更强的细胞增殖抑制活性。(3)分子对接结果显示,化合物5和化合物6与肝癌靶蛋白VEGF-2均具有良好的结合力。该研究结果不仅丰富了半枝莲的化学物质类群,也为进一步深入研究活性化合物抗肝癌的作用机制提供了参考。

半枝莲含药血清对膀胱癌T24细胞凋亡和黏附力的影响探究

目的:探究半枝莲含药血清对膀胱癌T24细胞凋亡和黏附力的影响。方法:SPF级雄性Wistar大鼠20只,随机分为无药血清组、半枝莲低剂量组、半枝莲中剂量组、半枝莲高剂量组,每组5只,分别以蒸馏水及半枝莲1.5g/(kg·d)、3g/(kg·d)、6g/(kg·d)腹腔注射灌胃,连续3d。末次灌胃后抽取心主动脉血,经灭活处理及微孔过滤或获得半枝莲含药血清。体外培养膀胱癌T24细胞株,分为无药血清组、半枝莲(低、中、高剂量)组,分别对应各组动物血清,以无药血清及含10%的药物血清培养。使用CCK-8法检测细胞增殖情况;流式细胞仪检测各组细胞凋亡率及周期分布;MTT酶标仪法检测各药物浓度下细胞的黏附率;以蛋白印记免疫法检测凋亡相关蛋白[B-细胞淋巴瘤因子2(Bcl-2)抗体、BCL2关联X蛋白(Bax)抗体、胱天蛋白酶3(CASP3)]的表达。结果:与无药血清组比较,半枝莲低剂量组24h及48h的增殖抑制率及凋亡率、细胞G0/G1期、黏附率增加(P<0.05);与半枝莲低剂量组比较,半枝莲中剂量组24h及48h的增殖抑制率及凋亡率、细胞G0/G1期、黏附率增加(P<0.05);与半枝莲中剂量组比较,半枝莲高剂量组24h及48h的增殖抑制率及凋亡率、细胞G0/G1期、黏附率增加(P<0.05)。与无药血清组比较,半枝莲低剂量组Bcl-2相对表达量下降,Bax、CASP3相对表达量增加(P<0.05);与半枝莲低剂量组比较,半枝莲中剂量组Bcl-2相对表达量下降,Bax、CASP3相对表达量增加(P<0.05);与半枝莲中剂量组比较,半枝莲高剂量组Bcl-2相对表达量下降,Bax、CASP3相对表达量增加(P<0.05)。结论:半枝莲含药血清体外培养膀胱癌T24细胞,可有效抑制细胞增殖、降低黏附力,并能诱导细胞凋亡,具有作为抗膀胱癌药物研发的价值。

中药半枝莲质量评价的研究进展

目的了解中药半枝莲质量评价的研究进展。方法通过查阅相关文献并归纳总结,对半枝莲质量评价方面的研究进行综述。结果半枝莲质量评价的研究内容主要包括性状和显微鉴定、指纹图谱研究以及含量测定研究,其中对于有效部位和药材中单体成分的含量测定研究报道相对较多。结论半枝莲的质量评价研究取得了一定进展,但尚存在一些问题,需要进一步深入探讨。

半枝莲含药血清通过抑制mTOR信号通路影响非小细胞肺癌NCI-H1650细胞上皮间质转化

目的探讨半枝莲含药血清通过抑制雷帕霉素靶蛋白(mammalian target of rapamycin,mTOR)信号通路影响非小细胞肺癌(non-small cell lung cancer,NSCLC)NCI-H1650细胞上皮间质转化。方法选取健康青紫蓝大白兔制备半枝莲含药血清,根据不同剂量分为对照组、低剂量组(A组)、中剂量组(B组)、高剂量组(C组)。选取人非小细胞肺癌细胞NCI-H1650与含药血清培养,采用逆转录RT-PCR、免疫印迹、MTT、划痕实验等方法,观察4组不同剂量半枝莲含药血清抑制mTOR信号通路对NCI-H1650细胞上皮间质转化、增殖、迁移的影响。结果4组mTOR表达量差异具有统计学意义,其中C组mTOR表达量低于对照组和A组(P<0.05);4组Vimentin、N-cadherin、E-cadherin蛋白表达相对灰度值差异具有统计学意义,且C组Vimentin、N-cadherin灰度值低于对照组、A组、B组,E-cadherin灰度值高于对照组(P<0.05);4组24、48、72 h吸光度差异具有统计学意义,且C组24、48、72 h吸光度低于对照组、A组、B组(P<0.05);4组NCI-H1650细胞迁移率差异具有统计学意义,且A组、B组、C组迁移率低于对照组,C组低于A组、B组(P<0.05)。结论高剂量半枝莲含药血清可通过抑制mTOR信号通路影响NCI-H1650细胞上皮间质转化、增殖及迁移,从而抑制NSCLC发生和发展。

近十年半枝莲抗肿瘤作用机制研究概况

半枝莲在调控肿瘤细胞的生长、侵袭转移、免疫功能和抗化疗药物耐药等方面发挥重要的作用,具有多成分、多效应、多途径、多靶点和毒副作用小的优势。半枝莲在临床中是一种极具开发潜力的药用资源,具有广阔的应用前景。本文现从抑制肿瘤细胞增殖,阻滞细胞生长周期,诱导细胞凋亡,促进细胞自噬,抑制血管生成,抑制细胞迁移和侵袭,调节免疫、抗化疗药物耐药等药理作用机制着手,对近十年的国内外关于半枝莲抗肿瘤作用机制方面的研究进行综述,发现半枝莲可通过调控Wnt/胞内β-连锁蛋白(β-catenin)、microRNA、磷脂酰肌醇-3激酶(phosphatidylinositol-3-kinases,PI3K)/蛋白激酶B(protein kinase B,Akt)和刺猬因子(sonic hedgehog,SHH)相关信号通路抑制肿瘤细胞生长。此外,半枝莲还能通过抑制肿瘤细胞运动相关蛋白和细胞因子,调节肿瘤细胞分解酶的活性及分解酶/分解酶抑制剂的平衡,发挥抑制细胞迁移和侵袭的作用,并能通过调节免疫相关细胞因子水平和抑制P-糖蛋白(P-glycoprotein,P-gp)的外排逆转化疗药物耐药。在今后的研究中有必要从转录组学、基因组学和蛋白组学等分子水平进一步探讨和验证其抗肿瘤作用机制,为临床应用和进一步新型靶向药物研究提供有力的证据支持。

半枝莲化学成分及其体外抑制乳腺癌细胞增殖活性

目的研究半枝莲Scutellaria barbata D.Don化学成分及其体外乳腺癌细胞增殖活性。方法半枝莲95%乙醇提取物采用聚酰胺、Sephadex LH-20、HPLC进行分离纯化,根据理化性质及波谱数据鉴定所得化合物的结构。采用MTT法对半枝莲各乙醇洗脱部位进行抗乳腺癌活性筛选,并评价各化合物对人乳腺癌细胞MDA-MB-231和人乳腺导管癌细胞株HCC38体外增殖的影响。结果从中分离得到9个化合物,分别鉴定为毛蕊花糖苷(1)、异毛蕊花糖苷(2)、白杨素(3)、野黄芩苷(4)、6-羟基木犀草素(5)、野黄芩素(6)、木犀草素(7)、异野黄芩素(8)、芹菜素(9)。大孔树脂50%乙醇洗脱部分抗乳腺癌活性最好。化合物7对MDA-MB-231细胞和HCC38细胞株体外增殖的抑制作用最好,其次为化合物5,而化合物4、6、9则表现出较弱的抑制作用。同时,化合物3、8对MDA-MB-231细胞体外增殖有较弱的抑制作用。结论化合物1~3为首次从该植物中分离。化合物5、7可以作为乳腺癌药物研究的潜在分子。

半枝莲二萜类化学成分及药理作用研究进展

半枝莲是一种传统抗癌中药,从中分离得到的二萜类化合物对人鼻咽癌、人口腔表皮样癌、人直肠癌等表现出较强的细胞毒活性,同时也具有较好的抗病毒、抗氧化等活性。本文对半枝莲中二萜类化合物,尤其是“同物异名”、“同名异物”进行了梳理,从化学成分、药理活性方面进行了综述,希望能对半枝莲中二萜类化合物的更一步深入研究提供理论基础。