Leucoxenols A and B,two new phenolics from Bornean medicinal plant Syzygium leucoxylon

The medicinal plant, Syzygium leucoxylon or commonly known as Obah found in North Borneo was considered as traditional medicine by local committee. Two new phenolics, leucoxenols A (1) and B (2) were isolated and identified as major secondary metabolites from the leaves of S. leucoxylon. Their chemical structures were elucidated based on spectroscopic data such as NMR and HRESIMS. Furthermore, these compounds were active against selected strains of fungi.     

反应氧族促进血管生成的作用及其脑内意义

反应氧族（reactive oxygen specise,ROS）是细胞有氧代谢产生的物质,在脑缺血发生与进展的过程中扮演着重要角色。以往研究多以消除ROS 作为神经保护的重要途径。近年研究表明ROS 不只介导缺血后脑组织的损伤,更是重要的信号通路分子﹑参与调控缺血后的组织修复。一定含量的ROS 可激活细胞增殖、细胞迁移,激活血管生成的相关通路,促进血管生成。因此,全面了解ROS 在脑缺血后动态过程中的作用,合理调控脑缺血后组织中ROS 的含量,可促进受损区域的血管生成,对及时恢复血供、保护神经功能具有重要意义。     

马勃的化学成分及其药理作用的研究进展

马勃（Lasiosphaera seu Calvatia）是大型食药用真菌,为灰包科真菌脱皮马勃、大马勃或紫色马勃的干燥子实体,其营养成分十分丰富,在2015 年《中国药典》中记载功能与主治清肺利咽,止血,用于风热郁肺咽痛,音哑,咳嗽,外治鼻衄,创伤出血。该文通过对马勃的种类、化学成分及其药用的功效进行综述,为此类真菌研究开发做进一步参考。     

Successful development and clinical translation of a novel anterior lamellar artificial cornea

Blindness due to corneal diseases is a common pathology affecting up to 23 million individuals worldwide. The tissue‐engineered anterior human cornea, which is currently being tested in a Phase I/II clinical trial to treat severe corneal trophic ulcers with preliminary good feasibility and safety results. This bioartificial cornea is based on a nanostructured fibrin–agarose biomaterial containing human allogeneic stromal keratocytes and cornea epithelial cells, mimicking the human native anterior cornea in terms of optical, mechanical, and biological behavior. This product is manufactured as a clinical‐grade tissue engineering product, fulfilling European requirements and regulations. The clinical translation process included several phases: an initial in vitro and in vivo preclinical research plan, including preclinical advice from the Spanish Medicines Agency followed by additional preclinical development, the adaptation of the biofabrication protocols to a good manufacturing practice manufacturing process, including all quality controls required, and the design of an advanced therapy clinical trial. The experimental development and successful translation of advanced therapy medicinal products for clinical application has to overcome many obstacles, especially when undertaken by academia or SMEs. We expect that our experience and research strategy may help future researchers to efficiently transfer their preclinical results into the clinical settings.     

水飞蓟宾对内毒素血症心肌损伤的保护作用及机制

摘要：目的探究水飞蓟宾（SIL）对小鼠内毒素血症心肌损伤的保护作用和分子机制。方法24只C57BL/6小鼠分为对照（Control）组、SIL组、LPS组、LPS+SIL组,每组6只。通过腹腔注射脂多糖（LPS,10 mg/kg）制备内毒素血症心肌损伤小鼠模型。LPS注射前3 d,SIL组和LPS+SIL组每日通过灌胃方式给予SIL（100 mg/kg）,共给药3次;Control组和LPS组每日通过灌胃方式给予等量（0.2 mL）生理盐水,共灌胃3次。LPS注射6 h后超声检测各组小鼠心脏收缩功能;ELISA检测血清IL-1β和TNF-α表达水平;DHE染色观察各组小鼠心肌组织内活性氧（ROS）产量;TUNEL染色检测心肌凋亡率;Western blot检测凋亡相关蛋白Bax、Bcl-2、Caspase 3和NOX2表达。结果与Control组相比,LPS组小鼠左心室射血分数、左心室短轴缩短率和Bcl-2表达量明显降低,而ROS产量、NOX2、Bax、Caspase 3、IL-1β与TNF-α表达量以及心肌凋亡率明显增加（P＜0.05）。与LPS组相比,LPS+SIL组经水飞蓟宾预处理后可明显改善LPS引起的上述改变（P＜0.05）。与Control组相比,单纯给予SIL干预对上述指标的变化无明显影响（P＞0.05）。结论水飞蓟宾可有效缓解内毒素血症心肌损伤,其作用可能与抑制氧化应激、炎症反应和抗凋亡有关。     

Quinalizarin induces cycle arrest and apoptosis via reactive oxygen species-mediated signaling pathways in human melanoma A375 cells

Quinalizarin, a bioactive and highly selective compound, is known to promote apoptosis in colon and lung cancer cells. However, studies evaluating quinalizarin-induced apoptosis in melanoma cells have not been conducted. In the present study, we investigated the underlying mechanisms of antimelanoma activity of quinalizarin in human melanoma A375 cells. The MTT assay and Trypan blue staining were used to evaluate the cell viability. The flow cytometry was used to detect cell cycle, apoptosis and reactive oxygen species (ROS). Western blot was used to detect the expression of cell cycle and apoptosis-related proteins, MAPK, and STAT3. The results revealed a significant dose and time dependent effect of quinalizarin on inhibiting proliferation in three kinds of human melanoma cells, and had no significant toxic effects on normal cells. Moreover, quinalizarin triggered G2/M phase cell arrest by modulating the protein expression levels of CDK 1/2, cyclin A, cyclin B, p21 and p27, and induced apoptosis by down-regulating the antiapoptotic protein Bcl-2 and upregulating the proapoptotic protein BAD, leading to the activation of caspase-3 and PARP in the caspase cascade in A375 cells. Quinalizarin treatment led to apoptosis of A375 cells via activation of MAPK and inhibition of STAT3 signaling pathways. In addition, quinalizarin increased the level of ROS, but ROS scavenger NAC inhibited quinalizarin-induced apoptosis by regulating MAPK and STAT3 signaling pathways. In summary, quinalizarin induces cell cycle arrest and apoptosis via ROS-mediated MAPK and STAT3 signaling pathways in human melanoma A375 cells, and quinalizarin may be used as a novel and effective antimelanoma therapeutic.     

人参皂苷对过氧化氢诱导的HepG2细胞损伤的保护作用

目的：探讨人参皂苷对过氧化氢（H₂O₂）诱导的HepG2细胞氧化应激损伤的保护作用,并阐明其作用机制。方法：体外培养HepG2细胞,采用不同浓度（0.1、0.2、0.3、0.4、0.5、0.6、0.7、0.8和1.0 mmol·L^-1）H₂O₂诱导HepG2细胞损伤。将HepG2细胞分为空白组、对照组、损伤组、人参皂苷对照组和人参皂苷保护组。10、20和40μmol·L^-1人参皂苷RH1、F1、RD、RO和RE分别孵育细胞3 h,H₂O₂损伤2 h,采用细胞增殖与毒性检测试剂盒（CCK-8）检测细胞存活率,CAA法检测细胞抗氧化活性,2',7'-二氯荧光黄双乙酸盐（DCFH-DA）荧光探针法检测细胞中活性氧（ROS）水平,WST-1法检测细胞中超氧化物歧化酶（SOD）活性。结果：H₂O₂半数抑制浓度（IC₅₀）为0.4 mmol·L^-1。与损伤组比较,10、20和40μmol·L^-1人参皂苷RH1、F1、RD、RO和RE预处理后,H₂O₂诱导氧化损伤的HepG2细胞存活率均有不同程度的升高,其中人参皂苷F1保护组细胞存活率升高最明显（P<0.05）。与对照组比较,10、20和40μmol·L^-1人参皂苷RH1、F1、RD、RO和RE保护组HepG2细胞存活率差异无统计学意义（P>0.05）。人参皂苷F1的半数效应浓度（EC₅₀）为（15.82±0.82）μmol·L^-1,CAA当量为（1 275.20±33.90）μmol TE/100 μmol·L^-1人参皂苷F1。与对照组比较,损伤组细胞中ROS水平明显升高（P<0.05）,SOD活性明显降低（P<0.05）;与损伤组比较,人参皂苷F1保护组细胞中ROS水平明显降低（P<0.05）,SOD活性明显升高（P<0.05）。结论：人参皂苷F1通过提高细胞抗氧化能力,降低细胞中ROS水平,提高细胞SOD活性对H₂O₂诱导的HepG2细胞氧化应激损伤起到保护作用。