Linsitinib_HNMR_23891_MedChemExpress
染料木黄酮诱导前列腺癌DU-145细胞凋亡的研究
染料木黄酮诱导前列腺癌DU-145细胞凋亡的研究萧聪勤;胡建波;周一南【摘要】目的探讨染料木黄酮诱导前列腺癌细胞系DU-145细胞凋亡的作用.方法在Caspase抑制剂Z-VAD存在或不存在的情况下,以染料木黄酮作用于前列腺癌DU-145细胞,采用MTT法检测细胞存活率、Annexin V-FITC/PI双染法流式细胞术检测细胞凋亡、PI染色法流式细胞术检测细胞周期、JC-1染色法流式细胞术测定细胞线粒体膜电位(△ψm),比色检测试剂盒测定caspase-8活性.结果染料木黄酮能明显降低前列腺癌DU-145细胞的存活率、诱导癌细胞凋亡、降低△ψm 及提高caspase-8活性(全部P＜0.05).Z-VAD能够逆转Gen抗前列腺癌的效应.结论染料木黄酮使细胞阻滞于G0和G1,分别通过凋亡信号通路的外源性和内源性途径,诱导前列腺癌细胞凋亡.【期刊名称】《岭南现代临床外科》【年(卷),期】2016(016)002【总页数】4页(P215-218)【关键词】染料木黄酮;前列腺癌;凋亡【作者】萧聪勤;胡建波;周一南【作者单位】510180广州广州市第一人民医院泌尿外科;510180广州广州市第一人民医院泌尿外科;510180广州广州市第一人民医院泌尿外科【正文语种】中文【中图分类】R737.25作者单位：510180广州广州市第一人民医院泌尿外科在欧美国家，前列腺肿瘤是男性最常见的恶性肿瘤，发病率已经超越肺癌排名第一位，是导致美国男性死亡第二多的恶性肿瘤［1，2］。
探讨一种安全、有效的抗前列腺癌的药物治疗方法是临床关注的焦点。
染料木黄酮（genistein，Gen）是从大豆中提取的异黄酮类化合物，是异黄酮类中活性最强的功能成分，具有抗白血病、抗病毒、抗肿瘤、抗辐射损伤和抗骨质疏松等多种生物活性，尤其在抗肿瘤活性方面更为显著［5］。
本项目通过染料木黄酮诱导前列腺癌细胞凋亡的作用，探讨其机制，对临床上治疗前列腺癌具有重要意义。
marked manuscript
Quality evaluation of Flos Lonicerae through a simultaneous determination of seven saponins by HPLC with ELSDXing-Yun Chai1, Song-Lin Li2, Ping Li1*1Key Laboratory of Modern Chinese Medicines and Department of Pharmacognosy, China Pharmaceutical University, Nanjing, 210009, People’s Republic of China2Institute of Nanjing Military Command for Drug Control, Nanjing, 210002, People’s Republic of China*Corresponding author: Ping LiKey Laboratory of Modern Chinese Medicines and Department of Pharmacognosy, China Pharmaceutical University, Nanjing 210009, People’s Republic of China.E-mail address: lipingli@Tel.: +86-25-8324-2299; 8539-1244; 135********Fax: +86-25-8532-2747AbstractA new HPLC coupled with evaporative light scattering detection (ELSD) method has been developed for the simultaneous quantitative determination of seven major saponins, namely macranthoidinB (1), macranthoidin A (2), dipsacoside B (3), hederagenin-28-O-β-D-glucopyranosyl(6→1)-O-β-D- glucopyranosyl ester (4), macranthoside B (5), macranthoside A (6), and hederagenin-3-O-α-L-arabinopyranosyl(2→1)-O-α-L-rhamnopyranoside (7)in Flos Lonicerae, a commonly used traditional Chinese medicine (TCM) herb.Simultaneous separation of these seven saponins was achieved on a C18 analytical column with a mixed mobile phase consisting of acetonitrile(A)-water(B)(29:71 v/v) acidified with 0.5% acetic acid. The elution was operated from keeping 29%A for 10min, then gradually to 54%B from 10 to 25 min on linear gradient, and then keep isocratic elution with 54%B from 25 to 30min.The drift tube temperature of ELSD was set at 106℃, and with the nitrogen flow-rate of 2.6 l/min. All calibration curves showed good linear regression (r2 0.9922) within test ranges. This method showed good reproducibility for the quantification of these seven saponins in Flos Lonicerae with intra- and inter-day variations of less than 3.0% and 6.0% respectively. The validated method was successfully applied to quantify seven saponins in five sources of Flos Lonicerae, which provides a new basis of overall assessment on quality of Flos Lonicerae.Keywords: HPLC-ELSD; Flos Lonicerae; Saponins; Quantification1. IntroductionFlos Lonicerae (Jinyinhua in Chinese), the dried buds of several species of the genus Lonicera (Caprifoliaceae), is a commonly used traditional Chinese medicine (TCM) herb. It has been used for centuries in TCM practice for the treatment of sores, carbuncles, furuncles, swelling and affections caused by exopathogenic wind-heat or epidemic febrile diseases at the early stage [1]. Though four species of Lonicera are documented as the sources of Flos Lonicerae in China Pharmacopeia (2000 edition), i.e. L. japonica, L. hypoglauca,L. daystyla and L. confusa, other species such as L. similes and L. macranthoides have also been used on the same purpose in some local areas in China [2]. So it is an important issue to comprehensively evaluate the different sources of Flos Lonicerae, so as to ensure the clinical efficacy of this Chinese herbal drug.Chemical and pharmacological investigations on Flos Lonicerae resulted in discovering several kinds of bioactive components, i.e. chlorogenic acid and its analogues, flavonoids, iridoid glucosides and triterpenoid saponins [3]. Previously, chlorogenic acid has been used as the chemical marker for the quality evaluation of Flos Lonicerae,owing to its antipyretic and antibiotic property as well as its high content in the herb. But this compound is not a characteristic component of Flos Lonicerae, as it has also been used as the chemical marker for other Chinese herbal drugs such as Flos Chrysanthemi and so on[4-5]. Moreover, chlorogenic acid alone could not be responsible for the overall pharmacological activities of Flos Lonicerae[6].On the other hand, many studies revealed that triterpenoidal saponins of Flos Lonicerae possess protection effects on hepatic injury caused by Acetaminophen, Cd, and CCl4, and conspicuous depressant effects on swelling of ear croton oil [7-11]. Therefore, saponins should also be considered as one of the markers for quality control of Flos Lonicerae. Consequently, determinations of all types of components such as chlorogenic acid, flavonoids, iridoid glucosides and triterpenoidal saponins in Flos Lonicerae could be a better strategy for the comprehensive quality evaluation of Flos Lonicerae.Recently an HPLC-ELSD method has been established in our laboratory for qualitative and quantitative determination of iridoid glucosides in Flos Lonicerae [12]. But no method was reported for the determination of triterpenoidal saponins in Flos Lonicera. As a series studies on the comprehensive evaluation of Flos Lonicera, we report here, for the first time, the development of an HPLC-ELSD method for simultaneous determination of seven triterpenoidal saponins in the Chinese herbal drug Flos Lonicerae, i.e.macranthoidin B (1), macranthoidin A (2), dipsacoside B (3), hederagenin-28-O-β-D-glucopyranosyl(6→1)-O-β-D- glucopyranosyl ester (4), macranthoside B (5), macranthoside A (6), and hederagenin-3-O-α-L-arabinopyranosyl(2→1)-O-α-L-rhamnopyranoside (7) (Fig. 1).2. Experimental2.1. Samples, chemicals and reagentsFive samples of Lonicera species,L. japonica from Mi county, HeNan province (LJ1999-07), L. hypoglauca from Jiujang county, JiangXi province (LH2001-06), L. similes from Fei county, ShanDong province (LS2001-07), L. confuse from Xupu county, HuNan province (LC2001-07), and L. macranthoides from Longhu county, HuNan province (LM2000-06) respectively, were collected in China. All samples were authenticated by Dr. Ping Li, professor of department of Pharmacognosy, China Pharmaceutical University, Nanjing, China. The voucher specimens were deposited in the department of Pharmacognosy, China Pharmaceutical University, Nanjing, China. Seven saponin reference compounds: macranthoidin B (1), macranthoidin A (2), dipsacoside B (3), hederagenin-28-O-β-D-glucopyranosyl(6→1)-O-β-D- glucopyranosyl ester (4), macranthoside B (5), macranthoside A (6), and hederagenin-3-O-α-L-arabinopyranosyl(2→1)-O-α-L-rhamnopyranoside (7) were isolated previously from the dried buds of L. confusa by repeated silica gel, sephadex LH-20 and Rp-18 silica gel column chromatography, their structures were elucidated by comparison of their spectral data (UV, IR, MS, 1H- NMR and 13C-NMR) with references [13-15]. The purity of these saponins were determined to be more than 98% by normalization of the peak areas detected by HPLC with ELSD, and showed very stable in methanol solution.HPLC-grade acetonitrile from Merck (Darmstadt, Germany), the deionized water from Robust (Guangzhou, China), were purchased. The other solvents, purchased from Nanjing Chemical Factory (Nanjing, China) were of analytical grade.2.2. Apparatus and chromatographic conditionsAglient1100 series HPLC apparatus was used. Chromatography was carried out on an Aglient Zorbax SB-C18 column（250 4.6mm, 5.0µm）at a column temperature of 25℃.A Rheodyne 7125i sampling valve (Cotati, USA) equipped with a sample loop of 20µl was used for sample injection. The analog signal from Alltech ELSD 2000 (Alltech, Deerfield, IL, USA)was transmitted to a HP Chemstation for processing through an Agilent 35900E (Agilent Technologies, USA).The optimum resolution was obtained by using a linear gradient elution. The mobile phase was composed of acetonitrile(A) and water(B) which acidified with 0.5% acetic acid. The elution was operated from keeping 29%A for 10min, then gradually to 54%B from 10 to 25 min in linear gradient, and back to the isocratic elution of 54%B from 25 to 30 min.The drift tube temperature for ELSD was set at 106℃and the nitrogen flow-rate was of 2.6 l/min. The chromatographic peaks were identified by comparing their retention time with that of each reference compound tried under the same chromatographic conditions with a series of mobile phases. In addition, spiking samples with the reference compounds further confirmed the identities of the peaks.2.3. Calibration curvesMethanol stock solutions containing seven analytes were prepared and diluted to appropriate concentration for the construction of calibration curves. Six concentrationof the seven analytes’ solution were injected in triplicate, and then the calibration curves were constructed by plotting the peak areas versus the concentration of each analyte. The results were demonstrated in Table1.2.4. Limits of detection and quantificationMethanol stock solution containing seven reference compounds were diluted to a series of appropriate concentrations with methanol, and an aliquot of the diluted solutions were injected into HPLC for analysis.The limits of detection (LOD) and quantification (LOQ) under the present chromatographic conditions were determined at a signal-to-noise ratio (S/N) of 3 and 10, respectively. LOD and LOQ for each compound were shown in Table1.2.5. Precision and accuracyIntra- and inter-day variations were chosen to determine the precision of the developed assay. Approximate 2.0g of the pulverized samples of L. macranthoides were weighted, extracted and analyzed as described in 2.6 Sample preparation section. For intra-day variability test, the samples were analyzed in triplicate for three times within one day, while for inter-day variability test, the samples were examined in triplicate for consecutive three days. Variations were expressed by the relative standard deviations. The results were given in Table 2.Recovery test was used to evaluate the accuracy of this method. Accurate amounts of seven saponins were added to approximate 1.0g of L. macranthoides,and then extracted and analyzed as described in 2.6 Sample preparation section. The average recoveries were counted by the formula: recovery (%) = (amount found –original amount)/ amount spiked ×100%, and RSD (%) = (SD/mean) ×100%. The results were given in Table 3.2.6. Sample preparationSamples of Flos Lonicerae were dried at 50℃until constant weight. Approximate 2.0g of the pulverized samples, accurately weighed, was extracted with 60% ethanol in a flask for 4h. The ethanol was evaporated to dryness with a rotary evaporator. Residue was dissolved in water, followed by defatting with 60ml of petroleum ether for 2 times, and then the water solution was evaporated, residue was dissolved with methanol into a 25ml flask. One ml of the methanol solution was drawn and transferred to a 5ml flask, diluted to the mark with methanol. The resultant solution was at last filtrated through a 0.45µm syringe filter (Type Millex-HA, Millipore, USA) and 20µl of the filtrate was injected to HPLC system. The contents of the analytes were determined from the corresponding calibration curves.3. Results and discussionsThe temperature of drift tube and the gas flow-rate are two most important adjustable parameters for ELSD, they play a prominent role to an analyte response. In ourprevious work [12], the temperature of drift tube was optimized at 90°C for the determination of iridoids. As the polarity of saponins are higher than that of iridoids, more water was used in the mobile phase for the separation of saponins, therefore the temperature for saponins determination was optimized systematically from 95°C to 110°C, the flow-rate from 2.2 to 3.0 l/min. Dipsacoside B was selected as the testing saponin for optimizing ELSD conditions, as it was contained in all samples. Eventually, the drift tube temperature of 106℃and a gas flow of 2.6 l/min were optimized to detect the analytes. And these two exact experimental parameters should be strictly controlled in the analytical procedure [16].All calibration curves showed good linear regression (r2 0.9922) within test ranges. Validation studies of this method proved that this assay has good reproducibility. As shown in Table 2, the overall intra- and inter-day variations are less than 6% for all seven analytes. As demonstrated in Table 3, the developed analytical method has good accuracy with the overall recovery of high than 96% for the analytes concerned. The limit of detection (S/N=3) and the limit of quantification (S/N=10) are less than 0.26μg and 0.88μg respectively (Table1), indicating that this HPLC-ELSD method is precise, accurate and se nsitive enough for the quantitative evaluation of major non- chromaphoric saponins in Flos Lonicerae.It has been reported that there are two major types of saponins in Flos Lonicerae, i.e. saponins with hederagenin as aglycone and saponins with oleanolic acid as the aglycone [17]. But hederagenin type saponins of the herb were reported to have distinct activities of liver protection and anti-inflammatory [7-11]. So we adoptedseven hederagenin type saponins as representative markers to establish a quality control method.The newly established HPLC-ELSD method was applied to analyze seven analytes in five plant sources of Flos Lonicerae, i.e. L. japonica,L. hypoglauca,L. confusa,L. similes and L. macranthoides(Table 4). It was found that there were remarkable differences of seven saponins contents between different plant sources of Flos Lonicerae. All seven saponins analyzed could be detected in L. confusa and L. hypoglauca, while only dipsacoside B was detected in L. japonica. Among all seven saponins interested, only dipsacoside B was found in all five plant species of Flos Lonicerae analyzed, and this compound was determined as the major saponin with content of 53.7 mg/g in L. hypoglauca. On the other hand, macranthoidin B was found to be the major saponin with the content higher than 41.0mg/g in L. macranthoides,L. confusa, and L. similis, while the contents of other analytes were much lower.In our previous study [12], overall HPLC profiles of iridoid glucosides was used to qualitatively and quantitatively distinguish different origins of Flos Lonicerae. As shown in Fig.2, the chromatogram profiles of L. confusa, L. japonica and L. similes seem to be similar, resulting in the difficulty of clarifying the origins of Flos Lonicerae solely by HPLC profiles of saponins, in addition to the clear difference of the HPLC profiles of saponins from L. macranthoides and L. hypoglauca.Therefore, in addition to the conventional morphological and histological identification methods, the contents and the HPLC profiles of saponins and iridoids could also be used as accessory chemical evidence toclarify the botanical origin and comprehensive quality evaluation of Flos Lonicerae.4. ConclusionsThis is the first report on validation of an analytical method for qualification and quantification of saponins in Flos Lonicerae. This newly established HPLC-ELSD method can be used to simultaneously quantify seven saponins, i.e. macranthoidin B, macranthoidin A, dipsacoside B, hederagenin-28-O-β-D-glucopyranosyl(6→1)-O-β-D- glucopyranosyl ester, macranthoside B, macranthoside A, and hederagenin-3-O-α-L-arabinopyranosyl(2→1)-O-α-L-rhamnopyranoside in Flos Lonicerae. Together with the HPLC profiles of iridoids, the HPLC-ELSD profiles of saponins could also be used as an accessory chemical evidence to clarify the botanical origin and comprehensive quality evaluation of Flos Lonicerae.AcknowledgementsThis project is financially supported by Fund for Distinguished Chinese Young Scholars of the National Science Foundation of China (30325046) and the National High Tech Program（2003AA2Z2010）.[1]Ministry of Public Health of the People’s Republic of China, Pharmacopoeia ofthe People’s Republic of China, V ol.1, 2000, p. 177.[2]W. Shi, R.B. Shi, Y.R. Lu, Chin. Pharm. J., 34(1999) 724.[3]J.B. Xing, P. Li, D.L. Wen, Chin. Med. Mater., 26(2001) 457.[4]Y.Q. Zhang, L.C. Xu, L.P. Wang, J. Chin. Med. Mater., 21(1996) 204.[5] D. Zhang, Z.W. Li, Y. Jiang, J. Pharm. Anal., 16(1996) 83.[6]T.Z. Wang, Y.M. Li, Huaxiyaoxue Zazhi, 15(2000) 292.[7]J.ZH. Shi, G.T. Liu. Acta Pharm. Sin., 30(1995) 311.[8]Y. P. Liu, J. Liu, X.SH. Jia, et al. Acta Pharmacol. Sin., 13 (1992) 209.[9]Y. P. Liu, J. Liu, X.SH. Jia, et al. Acta Pharmacol. Sin., 13 (1992) 213.[10]J.ZH. Shi, L. Wan, X.F. Chen.ZhongYao YaoLi Yu LinChuang, 6 (1990) 33.[11]J. Liu, L. Xia, X.F. Chen. Acta Pharmacol. Sin., 9 (1988) 395[12]H.J. Li, P. Li, W.C. Ye, J. Chromatogr. A 1008(2003) 167-72.[13]Q. Mao, D. Cao, X.SH. Jia. Acta Pharm. Sin., 28(1993) 273.[14]H. Kizu, S. Hirabayashi, M. Suzuki, et al. Chem. Pharm. Bull., 33(1985) 3473.[15]S. Saito, S. Sumita, N. Tamura, et al. Chem Pharm Bull., 38(1990) 411.[16]Alltech ELSD 2000 Operating Manual, Alltech, 2001, p. 16. In Chinese.[17]J.B. Xing, P. Li, Chin. Med. Mater., 22(1999) 366.Fig. 1 Chemical structures of seven saponins from Lonicera confusa macranthoidin B (1), macranthoidin A (2), dipsacoside B (3), hederagenin-28-O-β-D-glucopyranosyl(6→1)-O-β-D- glucopyranosyl ester (4), macranthoside B (5), macranthoside A (6), and hederagenin-3-O-α-L-arabinopyranosyl(2→1)-O-α-L-rhamnopyranoside (7)Fig. 2Representative HPLC chromatograms of mixed standards and methanol extracts of Flos Lonicerae.Column: Agilent Zorbax SB-C18 column（250 4.6mm, 5.0µm）, temperature of 25℃; Detector: ELSD, drift tube temperature 106℃, nitrogen flow-rate 2.6 l/min.A: Mixed standards, B: L. confusa, C: L. japonica, D: L. macranthoides, E: L. hypoglauca, F: L. similes.Table 1 Calibration curves for seven saponinsAnalytes Calibration curve ar2Test range(μg)LOD(μg)LOQ(μg)1 y=6711.9x－377.6 0.9940 0.56–22.01 0.26 0.882 y=7812.6x－411.9 0.9922 0.54–21.63 0.26 0.843 y=6798.5x－299.0 0.9958 0.46–18.42 0.22 0.724 y=12805x－487.9 0.9961 0.38–15.66 0.10 0.345 y=4143.8x－88.62 0.9989 0.42–16.82 0.18 0.246 y=3946.8x－94.4 0.9977 0.40–16.02 0.16 0.207 y=4287.8x－95.2 0.9982 0.42–16.46 0.12 0.22a y: Peak area; x: concentration (mg/ml)Table 2 Reproducibility of the assayAnalyteIntra-day variability Inter-day variability Content (mg/g) Mean RSD (%) Content (mg/g) Mean RSD (%)1 46.1646.2846.2246.22 0.1346.2245.3647.4226.33 2.232 5.385.385.165.31 2.405.285.345.045.22 3.043 4.374.304.184.28 2.244.284.464.024.255.204 nd1)-- -- nd -- --5 1.761.801.821.79 1.701.801.681.841.77 4.706 1.281.241.221.252.451.241.341.201.26 5.727 tr2)-- -- tr -- -- 1): not detected; 2): trace. RSD (%) = (SD/Mean) ×100%Table 3 Recovery of the seven analytesAnalyteOriginal(mg) Spiked(mg)Found(mg)Recovery(%)Mean(%)RSD(%)1 23.0823.1423.1119.7122.8628.1042.7346.1351.0199.7100.699.399.8 0.722.692.672.582.082.913.164.735.515.7698.197.6100.698.8 1.632.172.152.091.732.182.623.884.404.6598.8103.297.799.9 2.94nd1)1.011.050.980.981.101.0297.0104.8104.1102.0 4.250.880.900.910.700.871.081.561.752.0197.197.7101.898.9 2.660.640.620.610.450.610.751.081.211.3397.796.796.096.8 0.97tr2)1.021.101.081.031.111.07100.9102.799.1100.9 1.81): not detected; 2): trace.a Recovery (%) = (Amount found –Original amount)/ Amount spiked ×100%, RSD (%) = (SD/Mean) ×100%Table 4 Contents of seven saponins in Lonicera spp.Content (mg/g)1 2 3 4 5 6 7 L. confusa45.65±0.32 5.13±0.08 4.45±0.11tr1) 2.04±0.04tr 1.81±0.03 L. japonica nd2)nd 3.44±0.09nd nd nd nd L. macranthoides46.22±0.06 5.31±0.13 4.28±0.10 tr 1.79±0.03 1.25±0.03 tr L. hypoglauca11.17±0.07 nq3)53.78±1.18nd 1.72±0.02 2.23±0.06 2.52±0.04 L. similes41.22±0.25 4.57±0.07 3.79±0.09nd 1.75±0.02tr nd 1): trace; 2): not detected.. 3) not quantified owing to the suspicious purity of the peak.。
黄芩素通过调节HIF-1α
黄芩素通过调节HIF -1α/VEGF 信号通路抑制类风湿关节炎大鼠的炎症反应和病理性血管生成*杜红丽1，张晨宇1，赵清2△［1河南中医药大学第五临床医学院（郑州人民医院）风湿免疫科，河南郑州450053；2河南大学淮河医院风湿免疫科，河南开封475099］［摘要］目的：探讨黄芩素（BA ）调节缺氧诱导因子1α（HIF -1α）/血管内皮生长因子（VEGF ）信号通路对类风湿关节炎（RA ）大鼠炎症反应和病理性血管生成的影响。
方法：按照随机数字表法将SD 大鼠分为对照（control ）组、模型（model ）组、低剂量（10mg/kg ）BA （BA -L ）组、高剂量（30mg/kg ）BA （BA -H ）组、雷公藤多苷片（TWP ；6.25mg/kg ）组和BA -H+HIF -1α激动剂二甲基草酰甘氨酸（DMOG ；40mg/kg ）组，每组12只。
除control 组外，其它组大鼠均采用II 型胶原蛋白-完全弗氏佐剂法诱导RA 大鼠模型。
第2次免疫24h 后开始给药处理，每天给药一次，持续4周。
检测大鼠在给药第0、7、14和28天时的足趾肿胀度，计算关节炎指数；计算大鼠胸腺和脾脏指数；HE 染色检测大鼠踝关节滑膜组织病理损伤；ELISA 法检测大鼠踝关节滑膜组织中肿瘤坏死因子α（TNF -α）和白细胞介素6（IL -6）水平；免疫组化检测大鼠踝关节滑膜组织中VEGF 和VEGF 受体2（又称激酶插入域受体，KDR ）表达；Western blot 检测各组大鼠踝关节滑膜组织中HIF -1α和VEGF 蛋白表达。
结果：与control 组比较，model 组大鼠踝关节滑膜组织病理损伤严重，足趾肿胀度、关节炎指数、胸腺和脾脏指数，以及滑膜组织TNF -α、IL -6、VEGF 、KDR 、HIF -1α和VEGF 水平均显著升高（P <0.05）；与model 组比较，BA -L 组、BA -H 组和TWP 组对应指标变化趋势与上述相反（P <0.05）；BA -H 组与TWP 组比较，上述指标变化差异无统计学意义（P >0.05）；DMOG 减弱了BA -H 对RA 大鼠炎症反应和病理性血管生成的抑制作用。
211232350_莪术醇通过调节lncRNA_NR2F1-AS1
莪术醇通过调节lncRNA NR2F1-AS1/miR-145-5p表达抑制前列腺癌细胞增殖及转移汪洋杨君①（咸宁市中心医院，湖北科技学院附属第一医院泌尿外科，咸宁 437100）中图分类号R737.25 文献标志码 A 文章编号1000-484X（2023）04-0745-05［摘要］目的：探讨莪术醇对前列腺癌细胞增殖及转移的影响及其可能作用机制。
方法：不同浓度的莪术醇处理人前列腺癌细胞LNCap，采用脂质体转染法将si-NC、si-lncRNA NR2F1-AS1分别转染至LNCap细胞，将pcDNA、pcDNA-lncRNANR2F1-AS1分别转染至LNCap细胞后加入100 μg/ml莪术醇处理；CCK-8法、平板克隆形成实验、Transwell实验分别检测细胞增殖、克隆形成、迁移及侵袭；qRT-PCR检测lncRNA NR2F1-AS1、miR-145-5p表达量；双荧光素酶报告实验验证lncRNA NR2F1-AS1与miR-145-5p的靶向关系。
结果：莪术醇可降低细胞存活率，并可降低lncRNA NR2F1-AS1表达量，克隆形成数、迁移及侵袭细胞数减少（P<0.05），而miR-145-5p表达量升高（P<0.05）；lncRNA NR2F1-AS1可靶向调控miR-145-5p的表达（P< 0.05）；转染si-lncRNA NR2F1-AS1后细胞存活率降低（P<0.05），miR-145-5p表达量升高（P<0.05），克隆形成数、迁移及侵袭细胞数减少（P<0.05）；转染pcDNA-lncRNA NR2F1-AS1可降低莪术醇对LNCap细胞增殖及转移的作用。
结论：莪术醇可通过调节lncRNA NR2F1-AS1/miR-145-5p表达，抑制前列腺癌细胞增殖、克隆形成、迁移及侵袭。
［关键词］莪术醇；前列腺癌；lncRNA NR2F1-AS1；miR-145-5p；细胞增殖；迁移；侵袭Curcumol inhibits proliferation and metastasis of prostate cancer cells by regulating expression of lncRNA NR2F1-AS1/miR-145-5pWANG Yang， YANG Jun. Department of Urology， Xianning Central Hospital， the First Affiliated Hospital of Hubei University of Science and Technology， Xianning 437100， China［Abstract］Objective：To explore the effect of curcumol on the proliferation and metastasis of prostate cancer cells and its pos‐sible mechanism. Methods：Different concentrations of curcumol were used to treat human prostate cancer cells LNCap. si-NC， si-lnc-RNA NR2F1-AS1， pcDNA and pcDNA-lncRNA NR2F1-AS1 were transfected into LNCap cells by liposome transfection method re‐spectively. CCK-8 method， plate colony formation experiment， Transwell experiment were used to detect cell proliferation， colony for‐mation， migration and invasion. qRT-PCR was used to detect the expression of lncRNA NR2F1-AS1 and miR-145-5p. The dual lucifer‐ase report experiment was used to verify the targeting relationship between lncRNA NR2F1-AS1 and miR-145-5p. Results：Curcurmol decreased the cell survival rate and the expression of lncRNA NR2F1-AS1， and the number of colony formation， migration and inva‐sion cells were decreased （P<0.05）， while the expression of miR-145-5p was increased （P<0.05）. lncRNA NR2F1-AS1 could target the expression of miR-145-5p （P<0.05）， while the cell survival rate was decreased （P<0.05）， and the numbers of clone formation，migration and invasion cells were decreased （P<0.05）. pcDNA-lncRNA NR2F1-AS1 transfected could reduce the effect of curcumol on the proliferation and metastasis of LNCap cells. Conclusion：Curcumol can inhibit the proliferation， clone formation， migration and invasion of prostate cancer cells by regulating the expression of lncRNA NR2F1-AS1/miR-145-5p.［Key words］Curcumol；Prostate cancer；lncRNA NR2F1-AS1；miR-145-5p；Cell proliferation；Migration；Invasion前列腺癌是常见的一种恶性肿瘤，中药或从天然植物中提取的活性成分具有抗前列腺癌的作用，其主要通过多靶点、多途径等发挥抗肿瘤作用［1-4］。
Linsitinib_SDS_MedChemExpress
Inhibitors, Agonists, Screening LibrariesSafety Data Sheet Revision Date:Jul.-05-2017Print Date:Jul.-05-20171. PRODUCT AND COMPANY IDENTIFICATION1.1 Product identifierProduct name :LinsitinibCatalog No. :HY-10191CAS No. :867160-71-21.2 Relevant identified uses of the substance or mixture and uses advised againstIdentified uses :Laboratory chemicals, manufacture of substances.1.3 Details of the supplier of the safety data sheetCompany:MedChemExpress USATel:609-228-6898Fax:609-228-5909E-mail:sales@1.4 Emergency telephone numberEmergency Phone #:609-228-68982. HAZARDS IDENTIFICATION2.1 Classification of the substance or mixtureNot a hazardous substance or mixture.2.2 GHS Label elements, including precautionary statementsNot a hazardous substance or mixture.2.3 Other hazardsNone.3. COMPOSITION/INFORMATION ON INGREDIENTS3.1 SubstancesSynonyms:OSI 906; OSI–906; OSI906Formula:C26H23N5OMolecular Weight:421.49CAS No. :867160-71-24. 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胰岛素样生长因子系统在NSCLC中作用的研究进展
胰岛素样生长因子系统在NSCLC中作用的研究进展王毓洲;宁小红;周建凤【摘要】世界范围内，肺癌已居恶性肿瘤死亡率之首位。
近年来，针对肿瘤重要分子途径治疗非小细胞肺癌（nonsmall cell lung cancer,NSCLC）的靶向药物研究取得很大进展，其中，抗表皮细胞生长因子受体（Epidermal growth factor receptor,EGFR）和干扰血管内皮细胞生长因子（Vascular endothelial growth factor,VEGF）制剂已进入临床，并取得较好治疗效果。
但是，影响肺癌发病机制的分子机制尚未完全明了。
研究表明细胞膜表面受体和细胞核受体途径的信号交互作用具有控制肺癌细胞增长的重要作用，并决定了肿瘤细胞对靶向治疗的反应性。
【期刊名称】《中国肺癌杂志》【年(卷),期】2009(012)007【总页数】5页(P816-820)【作者】王毓洲;宁小红;周建凤【作者单位】100730北京,中国医学科学院,清华大学医学部,北京协和医学院北京协和医院肿瘤内科;100730北京,中国医学科学院,清华大学医学部,北京协和医学院北京协和医院肿瘤内科;100730北京,中国医学科学院,清华大学医学部,北京协和医学院北京协和医院肿瘤内科【正文语种】中文【中图分类】R734.2世界范围内，肺癌已居恶性肿瘤死亡率之首位。
近年来，针对肿瘤重要分子途径治疗非小细胞肺癌（nonsmall cell lung cancer, NSCLC）的靶向药物研究取得很大进展，其中，抗表皮细胞生长因子受体（Epidermal growth factor receptor, EGFR）和干扰血管内皮细胞生长因子（Vascular endothelial growth factor, VEGF）制剂已进入临床，并取得较好治疗效果。
但是，影响肺癌发病机制的分子机制尚未完全明了。
研究表明细胞膜表面受体和细胞核受体途径的信号交互作用具有控制肺癌细胞增长的重要作用，并决定了肿瘤细胞对靶向治疗的反应性。
氰基硼氢化钠还原胺化京尼平合成拟生物碱与活性
氰基硼氢化钠还原胺化京尼平合成拟生物碱与活性秦杰琛 1），曾小娟 1），张韶湘 1），张晓梅 2），刘鑫洋 1），邹 澄 1），赵 庆 2）（1）昆明医科大学药学院暨云南省天然药物药理重点实验室，云南 昆明 650500；2）云南中医药大学中药学院，云南 昆明 650500）[ 摘要 ] 目的 以京尼平苷为原料通过还原胺化反应合成拟生物碱的方法。
方法 京尼平与胺类化合物在氰基硼氢化钠存在下进行还原反应：京尼平与芳基乙胺的甲醇溶液混合后，加入过量氰基硼氢化钠，放置室温下反应3d，产物经石油醚-异丙醇-二乙胺，石油醚-乙酸乙酯等洗脱分离。
结果 合成共得到9个拟生物碱并对部分拟生物碱进行活性筛选，找到治疗Ⅱ型糖尿病的PTP1B 抑制剂。
结论 部分受试化合物对PTP1B 有抑制作用。
一系列活性衍生物的获得为化合物结构及其生物活性间的构效关系研究打下了基础，有利于寻找具有更高活性的PTP1B 抑制剂。
[ 关键词 ] 京尼平； 拟生物碱； 还原胺化； 抗PTP1B 活性[ 中图分类号 ] R284.1 [ 文献标志码 ] A [ 文章编号 ] 2095 − 610X （2021）02 − 0018 − 05Reductive Amination of Genipin with NaBH 3CN toSynthesize Alkaloid-likes and BioactivityQIN Jie-chen 1），ZENG Xiao-juan 1），ZHANG Shao-xiang 1），ZHANG Xiao-mei 2），LIU Xin-yang 1），ZOU Cheng 1），ZHAO Qing 2）（1） School of Pharmaceutical Science & Yunnan Key Laboratory of Pharmacology for Natural Products ，Kunming Medical University ，Kunming Yunnan 650500; 2） Faculty of Pharmacy ，Yunnan University of Chinese Medicine ，Kunming Yunnan 650500，China ）［Abstract ］ Objective To explore a method for the synthesis of alkaloid-likes from Genipin by reductive amination is reported. Methods The reduction of Genipin and amines in the presence of sodium cyanoborohydride：after the methanol solution of Genipin and arylethylamine was mixed，excessive sodium cyanoborohydride was added and the reaction was kept at room temperature for 3 days. The product was eluted and separated on silica gel by petroleum ether-isopropyl alcohol-diethylamine and petroleum ether-ethyl acetate. Results Nine alkaloid-likes were synthesized. Some alkaloid-likes were screened for inhibition activity of PTP1B enzyme for Ⅱ diabetes treatment. Conclusions All of the tested compounds have a certain inhibitory effect on PTP1B. The acquisition of a series of active derivatives has laid a foundation for the study of the structure-activity relationship between the compounds and their bioactivities，so as to facilitate the search for more active PTP1B inhibitors.［Key words ］ Genipin；Alkaloid-likes；Reductive amination；Inhibition activity against PTP1B目前，通过发现先导化合物是现代新药研发的重要出发点，研究者对具有特定生物活性的先导化合物，利用生物、化学方法进行结构修饰，从而减少化合物毒副作用，提高化合物的活性，增强其生物利用度，最终找到一些作用效果明显，副作用少的新药应用于临床治疗。
德谷门冬双胰岛素注射液治疗2_型糖尿病临床效果及安全性探讨
DOI：10.16658/ki.1672-4062.2023.17.098德谷门冬双胰岛素注射液治疗2型糖尿病临床效果及安全性探讨林生，谢平，陈予福州市长乐区人民医院内分泌科，福建福州350200[摘要]目的研究德谷门冬双胰岛素注射液治疗2型糖尿病的临床效果及安全性。
方法选取于2022年7月—2023年4月福州市长乐区人民医院收治的2型糖尿病患者98例为研究对象，采用随机抓阄法分为两组，每组49例。
两组均联用常规降糖药物治疗，对照组采用甘精胰岛素注射液治疗，观察组采用德谷门冬双胰岛素注射液治疗。
对比两组临床治疗效果、临床症状好转时间和胰岛素用量情况、糖代谢指标、胰岛素功能指标、不良反应发生情况、心血管不良事件发生情况。
结果观察组总有效率高于对照组，差异有统计学意义（P<0.05）。
观察组尿酮体转阴时间、血糖达标时间、胰岛素用量均优于对照组，差异有统计学意义（P< 0.05）。
观察组空腹血糖、餐后2 h血糖、糖化血红蛋白均低于对照组，差异有统计学意义（P<0.05）。
观察组胰岛β细胞功能指数高于对照组，胰岛素抵抗指数、空腹胰岛素低于对照组，差异有统计学意义（P<0.05）。
两组恶心呕吐、倦怠乏力、低血糖总发生率比较，差异无统计学意义（P>0.05）。
两组心绞痛、心力衰竭总发生率比较，差异无统计学意义（P>0.05）。
结论德谷门冬双胰岛素注射液治疗2型糖尿病临床效果显著优于甘精胰岛素注射液，但是治疗安全性无显著变化。
[关键词] 2型糖尿病；德谷门冬双胰岛素注射液；不良反应；心血管不良事件[中图分类号] R59 [文献标识码] A [文章编号] 1672-4062（2023）09（a）-0098-04Discussion on the Clinical Effect and Safety of Insulin Degludec and Insu⁃lin Aspart Injection in the Treatment of Type 2 Diabetes MellitusLIN Sheng, XIE Ping, CHEN YuDepartment of Endocrinology, Changle District People's Hospital, Fuzhou, Fujian Province, 350200 China[Abstract] Objective To study the clinical effect and safety of insulin degludec and insulin aspart injection in the treatment of type 2 diabetes mellitus. Methods A total of 98 patients with type 2 diabetes admitted to Fuzhou Changle District People's Hospital from July 2022 to April 2023 were selected as the study objects and divided into two groups with 49 cases in each group by random lottery method. Both groups were treated with conventional hypoglycemic drugs, the control group was treated with insulin glargine injection, and the observation group was treated with Degu asparton double insulin injection. The clinical therapeutic effect, time of improvement of clinical symptoms, insulin dosage, glucose metabolism index, insulin function index, occurrence of adverse reactions and cardiovascular adverse events were compared between the two groups. Results The total effective rate of the observation group was higher than that of the control group, and the difference was statistically significant (P<0.05). The time of urine ketone body turning negative, blood glucose reaching standard and insulin dosage in observation group were better than those in control group, and the differences were statistically significant (P<0.05). Fasting plasma glucose, 2-hour postprandial blood glucose and glycated hemoglobin in the observation group were lower than those in the control group, and the differences were statistically significant (P<0.05). The function index of islet β cells in observation group was higher than that in control group, the insulin resistance index and fasting insulin was lower than that in control group, the dif⁃ference was statistically significant (P<0.05). There was no statistically significant difference in the total incidence of [作者简介]林生（1981-），男，本科，副主任医师，研究方向为糖尿病及其并发症的相关临床研究。
细胞蛇的研究进展
2007年,英国牛津大学的刘骥陇等在研究果蝇U 小体和P 小体(U 小体和P 小体是真核生物细胞质中的无膜细胞器)的功能关系时,用4种针对Cup (P 小体中的一种蛋白质)的抗体,对雌性果蝇的卵巢组织进行免疫组织化学染色,染色结果除了预期标记上的P 小体外,还标记出了长条形的丝状结构[1]。
这种结构的形状和数量与纤毛很相似,导致当时以为在果蝇中找到了有纤毛的新细胞类型。
但后来的一系列实验表明,该结构与纤毛没有关系,于是将其命名为“细胞蛇”。
最初是抗Cup 抗体不纯产生假象,意外发现的细胞蛇,而采用亲和层析纯化后的抗Cup 抗体无法再DOI:10.16605/ki.1007-7847.2020.10.0258细胞蛇的研究进展收稿日期:2020-10-22;修回日期:2020-11-19;网络首发日期:2021-07-27基金项目:宁夏自然科学基金项目(2020AAC03179);国家自然科学基金资助项目(31560329)作者简介:李欣玲(1999—),女,广西贵港人,学生;*通信作者:俞晓丽(1984—),女,宁夏银川人,博士,副教授,主要从事干细胞与生殖生物学研究,E-mail:********************。
李欣玲,张樱馨,李进兰,潘文鑫,王彦凤,杨丽蓉,王通,俞晓丽*(宁夏医科大学生育力保持教育部重点实验室临床医学院基础医学院,中国宁夏银川750000)摘要:细胞蛇是近年来细胞生物学研究的热门方向之一,由于其在细胞的增殖、代谢和发育上具有一定的生物学功能,因此,对一些疾病如癌症等的临床诊断或治疗具有一定的指导意义。
细胞蛇是由三磷酸胞苷合成酶(cytidine triphosphate synthetase,CTPS)聚合而成的无膜细胞器,其形成过程及功能在不同类型的细胞中不尽相同。
例如:细胞蛇能促进癌细胞增殖,并使患者病情恶化;过表达的细胞蛇可抑制神经干细胞增殖,影响大脑皮层发育;在卵泡细胞中,细胞蛇相当于CTPS 的存储库,在卵子发生过程起到促进细胞增殖和代谢的作用。
角鲨烯环氧酶对宫颈鳞癌细胞增殖、凋亡及迁移侵袭的影响
ａｓｓｅｓｓｔｈｅｅｆｆｅｃｔｏｆＡＩＣＡＲｏｎｔｈｅｓｔａｂｉｌｉｔｙｏｆｃＭｙｃｍＲ ＮＡａｎｄｐｒｏｔｅｉｎ．ＷｅｓｔｅｒｎｂｌｏｔｗａｓｕｓｅｄｔｏｅｘａｍｉｎｅｔｈｅｒｅｇｕｌａｔｏｒｙｅｆｆｅｃｔｏｆＡＩＣＡＲｏｎｃ Ｍｙｃｉｎｖａｒｉｏｕｓｃａｎｃｅｒｃｅｌｌｌｉｎｅｓ．ＴｈｅＭＴＴａｓｓａｙｗａｓｕｓｅｄｔｏｄｅｔｅｒｍｉｎｅｔｈｅｅｆｆｅｃｔｏｆＡＩＣＡＲｏｎｃｅｌｌｖｉａｂｉｌｉｔｙｉｎｔｈｅｓｅｃｅｌｌｌｉｎｅｓ．Ｒｅｓｕｌｔｓ ＡＩＣＡＲｓｉｇｎｉｆｉｃａｎｔｌｙｕｐ ｒｅｇｕｌａｔｅｄｃ ＭｙｃａｔｂｏｔｈｍＲＮＡａｎｄｐｒｏｔｅｉｎｌｅｖｅｌｓ．Ｔｈｅｐｒｏｔｅｉｎｌｅｖｅｌｏｆｃ Ｍｙｃｒｅａｃｈｅｄａｐｌａｔｅａｕ１２ｈａｆｔｅｒｔｈｅＡＩＣＡＲｔｒｅａｔ ｍｅｎｔ．Ｔｈｅｕｐ ｒｅｇｕｌａｔｏｒｙｅｆｆｅｃｔｏｆｃ ＭｙｃｉｎｄｕｃｅｄｂｙＡＩＣＡＲｗａｓｎｏｔｄｅｐｅｎｄｅｎｔｏｎｅｉｔｈｅｒｔｈｅＡＭＰＫｓｉｇｎａ ｌｉｎｇｐａｔｈｗａｙｏｒｔｈｅｄｏｗｎｓｔｒｅａｍｍｅｔａｂｏｌｉｔｅｓｏｆＡＩＣＡＲ．ＡＩＣＡＲｃｏｕｌｄｓｉｇｎｉｆｉｃａｎｔｌｙｅｎｈａｎｃｅｔｈｅｍＲＮＡｓｔａｂｉｌｉｔｙｏｆｃ Ｍｙｃｂｕｔｄｉｄｎｏｔａｆｆｅｃｔｔｈｅｐｒｏｔｅｉｎｓｔａｂｉｌｉｔｙ．Ｔｈｅｕｐ ｒｅｇｕｌａｔｉｏｎｏｆｃ ＭｙｃｉｎｄｕｃｅｄｂｙＡＩＣＡＲｗａｓｃｅｌｌ ｔｙｐｅｓｐｅｃｉｆｉｃ．ＡＩＣＡＲｕｐ ｒｅｇｕｌａｔｅｄｃ ＭｙｃｉｎＳＷ１９９０，７８６ Ｏ，ａｎｄＡ５４９，ｗｈｉｌｅｄｏｗｎ ｒｅｇｕｌａｔｅｄｃ ＭｙｃｉｎＨｅｐＧ２，ＭＣＦ７，ａｎｄＵ２ＯＳ．ＩｎＨｅｐＧ２ｃｅｌｌｓ，ＡＩＣＡＲｔｒｅａｔｍｅｎｔｄｅｃｒｅａｓｅｄｃｅｌｌｖｉａｂｉｌｉｔｙ．Ｈｏｗｅｖｅｒ，ｉｎＳＷ１９９０ａｎｄＡ５４９ｃｅｌｌｓ，ＡＩＣＡＲｔｒｅａｔｍｅｎｔｄｉｄｎｏｔｌｅａｄｔｏａｎｙｓｉｇｎｉｆｉｃａｎｔｄｉｆｆｅｒｅｎｃｅｉｎｃｅｌｌｖｉａｂｉｌｉｔｙ．ＡＩＣ ＡＲｄｅｃｒｅａｓｅｄｔｈｅｃｅｌｌｖｉａｂｉｌｉｔｙｏｎｌｙｗｈｅｎｃ ＭｙｃｗａｓｋｎｏｃｋｅｄｄｏｗｎｉｎＳＷ１９９０ａｎｄＡ５４９ｃｅｌｌｓ．Ｃｏｎｃｌｕ ｓｉｏｎｓ ＡＩＣＡＲｄｉｒｅｃｔｌｙｕｐ ｒｅｇｕｌａｔｅｓｃ ＭｙｃｅｘｐｒｅｓｓｉｏｎｉｎａｎＡＭＰＫ ｉｎｄｅｐｅｎｄｅｎｔｍａｎｎｅｒ．Ｔｈｅｕｐ ｒｅｇｕｌａｔｉｏｎｅｆｆｅｃｔｉｓｃｅｌｌ ｔｙｐｅｄｅｐｅｎｄｅｎｔ．Ｔｈｅｒｅｇｕｌａｔｉｏｎｏｆｃ ＭｙｃｅｘｐｒｅｓｓｉｏｎｂｙＡＩＣＡＲｉｓｌｉｎｋｅｄｔｏｔｈｅｉｎｈｉｂｉｔｏｒｙｅｆｆｅｃｔｏｆＡＩＣＡＲｏｎｔｕｍｏｒｃｅｌｌｐｒｏｌｉｆｅｒａｔｉｏｎ．Ｋｅｙｗｏｒｄｓ：ＡＩＣＡＲ；ｃ Ｍｙｃ；ＡＭＰＫ；ｃｅｌｌｐｒｏｌｉｆｅｒａ ｔｉｏｎ；ｃａｎｃｅｒｈｅｔｅｒｏｇｅｎｅｉｔｙ；ａｎｔｉ ｃａｎｃｅｒｃｏｍｐｏｕｎｄ网络出版时间：２０２３－１２－０１１６：３５：４６ 网络出版地址：ｈｔｔｐｓ：／／ｌｉｎｋ．ｃｎｋｉ．ｎｅｔ／ｕｒｌｉｄ／３４．１０８６．Ｒ．２０２３１１３０．１３２１．０３２角鲨烯环氧酶对宫颈鳞癌细胞增殖、凋亡及迁移侵袭的影响夏娜娜，陈思颖，杨京蕊，康 敏，余敏敏（南京中医药大学附属南京医院／南京市第二医院，江苏南京 ２１０００３）ｄｏｉ：１０．１２３６０／ＣＰＢ２０２２１１０２６文献标志码：Ａ文章编号：１００１－１９７８（２０２３）１２－２２９５－１０中国图书分类号：Ｒ３２９ ２５；Ｒ３２９ ２８；Ｒ３４５ ４；Ｒ３９４ ２；Ｒ７３７ ３３摘要：目的 探究角鲨烯环氧酶（ｓｑｕａｌｅｎｅｅｐｏｘｉｄａｓｅ，ＳＱＬＥ）在宫颈鳞癌中的作用及其分子机制。
双去甲氧基姜黄素对小鼠乳腺癌的抗肿瘤作用及机制
双去甲氧基姜黄素对小鼠乳腺癌的抗肿瘤作用及机制李学瑛;徐阳;王秘【期刊名称】《国际医药卫生导报》【年(卷),期】2022(28)16【摘要】目的本研究旨在研究双去甲氧基姜黄素(bisdesmethoxycurcumin,BDMC)对小鼠乳腺癌的影响及机制。
方法采用小鼠乳腺癌4T1细胞,分为Control组及不同剂量(3、9、27μM)BDMC组,通过CCK8法检测BDMC对小鼠乳腺癌4T1细胞增殖的影响,TUNEL染色检测BDMC对4T1细胞凋亡的影响,Western blot检测BDMC对4T1细胞Bax、Bcl-2及cleaved caspase-3表达的影响;采用4T1乳腺癌荷瘤小鼠模型,分为Control组及不同剂量(10、30 mg/kg)BDMC组,检测BDMC对小鼠肿瘤体积及体质量的影响,Western blot检测BDMC对乳腺癌小鼠肿瘤组织Bax、Bcl-2及cleaved caspase-3表达的影响。
采用单因素方差分析。
结果与Control组相比,9、27μM BDMC均能明显抑制4T1细胞增殖(均P<0.01),促进其凋亡(均P<0.01),同时上调细胞Bax/Bcl-2比值及cleaved caspase-3表达(均P<0.01);10、30 mg/kg BDMC均能明显抑制乳腺癌小鼠肿瘤体积的增长(均P<0.05),同时明显上调肿瘤组织Bax/Bcl-2比值及cleaved caspase-3表达(均P<0.05),但对体质量无明显影响。
结论BDMC对乳腺癌小鼠模型具有明显的抗肿瘤作用,其机制与激活线粒体凋亡通路有关。
【总页数】5页(P2311-2315)【作者】李学瑛;徐阳;王秘【作者单位】滨州职业学院健康学院;上海市医药学校生物技术制药系【正文语种】中文【中图分类】R73【相关文献】1.双去甲氧基姜黄素抑制肝癌细胞增殖并诱导凋亡的机制2.双脱甲氧基姜黄素抗血管生成作用分子学机制研究3.双去甲氧基姜黄素对四氯化碳致小鼠急性肝损伤的保护作用及机制4.双脱甲氧基姜黄素对db/db小鼠胰岛素抵抗和糖稳态作用及机制研究5.双去甲氧基姜黄素对四氯化碳致小鼠急性肝损伤的保护作用及机制因版权原因，仅展示原文概要，查看原文内容请购买。