发酵时间对水豆豉理化特性和对MCF-7人乳腺癌细胞体外抗癌作用的影响

水豆豉是一种短时间发酵的黄豆制品,采用理化试验和癌细胞体外试验,通过p H、酸度、总菌数、氨基酸态氮含量、铵态氮含量、γ-谷氨酰转肽酶(γ-GTP)活性、感官评价、MTT试验和RT-PCR,评价不同发酵时间水豆豉的理化特性和体外抑制作用。随着发酵时间的增加,p H值和总菌数增加,发酵48 h水豆豉的蛋白质含量、酸度、γ-GTP和活性大豆异黄酮(大豆黄素和金雀异黄素)含量都比其他发酵时间水豆豉高,在感官评价上48 h发酵的水豆豉也优于其他发酵时间的水豆豉。48 h发酵的水豆豉也具有对MCF-7人乳腺癌细胞最强的生长抑制作用,且48 h发酵水豆豉处理后的MCF-7细胞的Bax,caspase 3,9基因的表达强于其他发酵时间的水豆豉,Bcl-2基因则弱于其他发酵时间的水豆豉。结果显示48 h发酵的水豆豉具有最好的理化品质和体外抗癌效果。研究结果为改善水豆豉生产工艺提供理论支持。     

Bis(dipyridophenazine)(2‐(2′‐pyridyl)pyrimidine‐4‐carboxylic acid)ruthenium(II) Hexafluorophosphate: A Lesson in Stubbornness

Ruthenium complexes are currently considered to be among the most promising alternatives to platinum anticancer drugs. In this work, thirteen structural analogues and organelle/receptor‐targeting peptide bioconjugates of a cytotoxic bis(dppz)‐Ru^II complex [Ru(dppz)₂(CppH)](PF₆)₂ ( 1 ) were prepared, characterized, and assessed for their cytotoxicity and cellular localization (CppH=2‐(2′‐pyridyl)pyrimidine‐4‐carboxylic acid; dppz=dipyrido[3,2‐a:2′,3′‐c]phenazine). It was observed that structural modifications (lipophilicity, charge, and size‐based) result in the cytotoxic potency of 1 being compromised. Confocal microscopy studies revealed that unlike 1 , the screened complexes/bioconjugates do not have a preferential accumulation in mitochondria. The results of this important structure–activity relationship strongly support our initial hypothesis that accumulation in mitochondria is crucial for 1 to exert its cytotoxic action.     

黑色素-纳米硒的制备及其性质

以黑芝麻黑色素为模板剂和还原剂制备黑色素-纳米硒,对黑色素-纳米硒的制备工艺进行优化,并表征其结构和形貌,之后进一步探讨其缓释特性、体外抗氧化能力,评价其对红细胞和内皮细胞EAhy926氧化损伤的保护作用,通过肺癌细胞A549模型和海虾致死实验探讨其抑癌活性和生物相容性。结果表明黑色素-纳米硒合成的最适条件为：0.3 mg/mL黑色素溶液与0.555 mg/mL二氧化硒溶液体积比为9∶5,反应pH 7,40℃避光磁力搅拌(400 r/min)反应5 h。X射线光电子能谱结果表明Se⁴⁺可被全部还原。红外结果表明黑色素结构中羧基及共轭结构可能参与了反应。同步光散射仪表征黑色素-纳米硒粒径约为200 nm,性质稳定,能较好地分布于水分散体系中。黑色素-纳米硒在人工模拟胃液环境中可稳定存在2 h,具有一定的pH值稳定性,在人工模拟肠液环境中可缓慢释放,能实现在肠液中的长效缓释。体外抗氧化结果表明黑色素-纳米硒对2,2’-联氮双(3-乙基苯并噻唑啉-6-磺酸)阳离子自由基清除率和总还原力显著优于二氧化硒。黑色素-纳米硒能显著抑制H₂O₂     

Apoptotic Effects of Anthocyanins from Vitis coignetiae Pulliat Are Enhanced by Augmented Enhancer of the Rudimentary Homolog (ERH) in Human Gastric Carcinoma MKN28 Cells

Evidence suggests that augmented expression of a certain gene can influence the efficacy of targeted and conventional chemotherapies. Here, we tested whether the high expression of enhancer of the rudimentary homolog (ERH), which serves as a prognostic factor in some cancers, can influence the efficacy of anthocyanins isolated from fruits of Vitis coignetiae Pulliat, Meoru in Korea (AIMs) on human gastric cancer cells. The anticancer efficacy of AIMs was augmented in ERH-transfected MKN28 cells (E-MKN28 cells). Molecularly, ERH augmented AIM-induced caspase-dependent apoptosis by activating caspase-3 and -9. The ERH-augmented apoptotic effect was related to mitochondrial depolarization and inhibition of antiapoptotic proteins, XIAP, and Bcl-2. In addition, reactive oxygen species (ROS) generation was augmented in AIMs-treated E-MKN28 cells compared to AIMs-treated naïve MKN28 cells. In conclusion, ERH augmented AIM-induced caspase-dependent mitochondrial-related apoptosis in MKN28 cells. A decrease in expression of Bcl-2 and subsequent excessive ROS generation would be the mechanism for ERH-augmented mitochondrial-related apoptosis in AIMs-treated MKN28 cells. A decrease in expression of XIAP would be another mechanism for ERH-augmented caspase-dependent apoptosis in AIMs-treated MKN28 cells.     

金属配合物抗癌活性的研究进展

自从发现顺铂具有抗癌活性以来,金属配合物作为新一类抗癌药物引起了人们的广泛关注。综述了近年来铂类配合物、钌类配合物和席夫碱配合物在抗癌药物中的研究进展,重点阐述了铂类配合物抗癌活性的研究现状及作用原理,并对金属配合物抗癌活性的研究进展进行总结,为金属配合物抗癌药物研究提供参考和依据。     

姜黄素的生物学活性研究进展

姜黄素是一种从姜科植物姜黄等的根茎中提取得到的黄色色素,具有广泛的生物学活性。本文对姜黄素生物学活性等方面的研究进展做一综述,为姜黄素的进一步深入研究和开发利用提供参考。     

异海松酸基酰腙化合物的合成及抗癌活性研究

以异海松酸(IPA)为原料,通过羧基酰氯化、肼解和缩合3步反应,合成了5种异海松酸基酰腙化合物(Ⅲa~Ⅲe)。目标化合物的结构通过IR、~1HNMR、~(13)CNMR和MS分析得到确证,并通过MTT法测试目标产物对小鼠HepG2癌细胞的抑制活性。结果表明,5种化合物对小鼠HepG2癌细胞均表现出抑制活性,其中,化合物Ⅲa和Ⅲc在浓度为100μmol/L时对小鼠HepG2癌细胞表现出显著的抑制活性,抑制率分别为75.42%和70.50%。     

Modulation of Biodistribution,Pharmacokinetics, and Photosensitivity with the Delivery Vehicle of a Bacteriochlorin Photosensitizer for Photodynamic Therapy

Intravenous (i.v.) formulations with various amounts of organic solvents [PEG₄₀₀, propylene glycol (PG), cremophor EL (CrEL)] were used to deliver a fluorinated sulfonamide bacteriochlorin to mice, rats, and minipigs. Biodistribution studies in mice showed that a low‐content CrEL formulation combines high bioavailability with high tumor‐to‐muscle and tumor‐to‐skin ratios. This formulation was also the most successful in the photodynamic therapy of mice with subcutaneously implanted CT26 murine colon adenocarcinoma tumors. Pharmacokinetic studies in mice and minipigs revealed that with the same low CrEL formulation, the half‐life of the photosensitizer in the central compartment was longer in minipigs. Differences in biodistribution with the various formulations, and in pharmacokinetics between the two animal species with the same formulation, are attributed to the interaction of the formulations with low‐density lipoproteins (LDLs). Skin photosensitivity studies in rats showed that 30 min exposure of the skin to a solar simulator 7 days after i.v. administration of the fluorinated sulfonamide bacteriochlorin at 1 mg kg^?1 did not elicit significant skin reactions.