大黄-黄芪组分自微乳的制备及在体肠吸收特性研究

目的 研究大黄-黄芪多组分自微乳的处方与制备工艺,评价制剂质量,并考察其大鼠肠吸收特性。方法 通过溶解度实验、油相与乳化剂和助乳化剂配伍实验及伪三元相图的绘制,筛选出最优处方组成;并从自微乳的外观、形态、粒径、稳定性等方面对自微乳进行评价。通过大鼠在体单向肠灌流实验考察自微乳的肠吸收特性。结果 自微乳处方中油相为辛酸癸酸单双甘油酯、乳化剂为聚氧乙烯蓖麻油35、助乳化剂为乙二醇。在微乳形成区选择各辅料用量,采用适宜方法加入大黄总蒽醌及黄芪总皂苷制得的组分自微乳,外观均一透明,加水分散后形成黄色乳光的微乳液,透射电镜显微镜（transmission electron microscopy,TEM）下观察到微乳分散均匀,无黏连,呈大小均一圆球形乳滴;平均粒径为（33.01±0.12）nm、多分散指数（polydispersion index,PDI）为0.10±0.02、电位为（-10.10±1.00）m V;自微乳中大黄总蒽醌和黄芪总皂苷质量分数分别为6.29、8.80 mg/g。自微乳中大黄总蒽醌在十二指肠、空肠段的吸收速率常数（Ka）及表观吸收系数（Papp）较回肠段均有显著提高;黄芪...     

降糖方对糖耐量异常大鼠糖脂代谢及骨骼肌组织IκB-α和NF-κBp65的影响

目的:探讨降糖方对糖耐量异常大鼠糖脂代谢及骨骼肌组织κB抑制蛋白α(IκB-α)、核转录因子肽p65(NF-κBp65)的影响。方法:SD大鼠随机分为正常组、模型组、盐酸二甲双胍组、降糖方低、高剂量组,采用高脂饮食喂养4周,链脲佐菌素(STZ)腹膜内注射建立糖耐量异常大鼠模型,治疗8周后,观察骨骼肌组织病理变化,测定空腹血糖(FPG)、血清胰岛素(FINS)、胰岛素抵抗指数(HOMA-IR)、甘油三酯(TG)、总胆固醇(TC)、低密度脂蛋白(LDL-C)、骨骼肌组织IκB-α mRNA、NF-κBp65 mRNA水平、骨骼肌组织白细胞介素-4(IL-4)、白细胞介素-12(IL-12)、肿瘤坏死因子-α(TNF-α)蛋白水平。结果:正常组大鼠骨骼肌组织结构正常,模型组骨骼肌排列紊乱、肌纤维断裂、可见明显炎症细胞浸润;盐酸二甲双胍及降糖方干预后,骨骼肌炎症细胞浸润减少,肌纤维排列趋于整齐。模型组大鼠FPG、FINS、HOMA-IR水平、血清TG、TC、LDL-C水平、骨骼肌IκB-α mRNA、NF-κBp65 mRNA和蛋白水平、骨骼肌组织IL-4、IL-12、TNF-α蛋白水平高于对...     

Circulating magnesium status is associated with type 2 diabetes remission after Roux-en-Y gastric bypass surgery: a long-term cohort study

BackgroundLow serum magnesium levels predict cardiovascular and all-cause mortality in patients with typ 2 diabetes.SettingOutpatient clinic of obesity and central hospital.ObjectivesTo assess long-term alterations in circulating magnesium status after Roux-en-Y gastric bypass (RYGB) surgery and associations with remission of type 2 diabetes (T2D).MethodsRetrospective analysis of 5-year outcomes of plasma magnesium (p-Mg) and glucometabolic statuses in patients who underwent primary RYGB and who completed the annual follow-up program. Data were investigated from 84 patients without diabetes and 62 with T2D before RYGB, who showed either prolonged remission (n = 30), temporary remission (n = 16), or no remission (n = 16) after surgery.ResultsBody mass indexes before RYGB were similar in patients with and without T2D, irrespective of remission. The patients not achieving remission showed longer diabetes durations; higher circulating glucose levels; more intensive antidiabetic drug treatment, including insulin; and significantly lower p-Mg concentrations (.73 [±.08] mmol/L compared with .80–.82 [±.07] mmol/L, respectively; P < .01) than the groups showing remission or without diabetes before surgery. After RYGB, the p-Mg increased similarly, by 10–12% in the groups with T2D before surgery, irrespective of remission; however, the nonremission group did not reach the p-Mg levels registered in the other groups after follow-up. The nonremission group reached .82 (.09) mmol/L, compared with .87 (.06) and .88 (.08) mmol/L (P < .05), respectively, in patients with remission or without a history of diabetes.ConclusionThe p-Mg concentrations increased after RYGB, with similar increments irrespective of T2D remission; however, the nonremission group started from an inferior level and did not reach the p-Mg concentrations seen in the groups achieving remission or without a history of diabetes before surgery.     

Binding of lipopeptide to CD14 induces physical proximity of CD14, TLR2 and TLR1

Lipoproteins or lipopeptides (LP) are bacterial cell wall components detected by the innate immune system. For LP, it has been shown that TLR2 is the essential receptor in cellular activation. However, molecular mechanisms of LP recognition are not yet clear. We used a FLAG-labeled derivative of the synthetic lipopeptide N-palmitoyl-S-[2,3-bis(palmitoyloxy)-(2R,S)-propyl]-(R)-cysteinyl-seryl-(lysyl)(3)-lysine (Pam(3)CSK(4)) to study the roles of CD14, TLR2 and TLR1 in binding and signaling of LP and their molecular interactions in human cells. The activity of Pam(3)CSK(4)-FLAG was TLR2 dependent, whereas the binding was enabled by CD14, as evaluated by flow cytometry and confocal microscopy. Using FRET and FRAP imaging techniques to study molecular associations, we could show that after Pam(3)CSK(4)-FLAG binding, CD14 and Pam(3)CSK(4)-FLAG associate with TLR2 and TLR1, and TLR2 is targeted to a low-mobility complex. Thus, LP binding to CD14 is the first step in the LP recognition, inducing physical proximity of CD14 and LP with TLR2/TLR1 and formation of the TLR2 signaling complex.     

乙酰基二肽-1鲸蜡酯的皮肤抗衰老作用及其机制

乙酰基二肽-1鲸蜡酯（acetyl dipeptide-1 cetyl ester,AD-1）是乙酸和十六烷基醇与精氨酸和酪氨酸组成的人工合成肽,具有一定的抗炎和提高皮肤屏障功能的作用,已被用于敏感肌化妆品中。该成分虽然也被用于抗衰老化妆品中,但缺乏公开的系统科学研究。本研究通过评价AD-1的体外抗氧化和抗糖基化作用、建立UVA反复照射真皮原代成纤维细胞的光老化模型,探讨其在光老化细胞中的抗衰老活性。采用MTT法测定AD-1对细胞活力的影响;RT-qPCR法检测AD-1和UVA对衰老相关p21、p53、MMPs、IL6、Col1、Col3以及自噬相关p62、ATG5、ATG7 mRNA表达的影响;Western blot法检测AD-1和UVA对衰老及自噬相关p16、p21、p53、Col1、LC3B、p62蛋白水平的影响;β-半乳糖苷酶染色和MDC染色评价细胞衰老损伤,并通过荧光探针DCFH-DA检测细胞内活性氧水平。实验结果显示,AD-1干预可以减少UVA诱导的细胞损伤和mRNA表达异常,改善p16、p21、p53、Col1、LC3B、p62蛋白水平异常。结果表明,AD-1具有一定的...     

Cross-reactivity between pollen extracts from six artemisia species

Pollen extracts of six different ARTEMISIA species, A. VULGARIS, A. SCOPARIA, A. PRINCEPS, A. TRIDENTATA, A. ANNUA, and A. CAMPESTRIS were compared using SDS-PAGE, IEF, immunoblotting, and immunoelectrophoretic methods. The band patterns obtained after SDS-PAGE and IEF showed a large degree of similarity between the extracts. Immunoblotting of these gels using a pool of sera from patients allergic to A. VULGARIS gave essentially the same IgE-binding band pattern with all the extracts, demonstrating an extensive degree of cross-reactivity between A. VULGARIS and the other ARTEMISIA species. FRIE using a polyspecific antiserum against A. VULGARIS showed that all the extracts contained several antigens that were immunologically identical to antigens in A. VULGARIS extract. Antigens showing immunological identity to the important A. VULGARIS allergens Ag 12 and ART V II were present in all the extracts. The cross-reactivity between A. VULGARIS and A. PRINCEPS was further verified by screening of ten Korean and nine Norwegian individual patient sera against extracts of both species in SDS-PAGE or IEF immunoblotting. Both groups of patients had essentially the same pattern of reactivity towards both pollen extracts.     

Autologous peripheral blood stem cell transplantation in the patients with hematologic malignancies and solid tumors

Objective To evaluate the long-term therapeutic effects of autologous peripheral blood st em cell transplantation (auto-PBSCT) on the treatment of hematological and soli d tumors. Methods Fifty-one patients were recruited in this auto-PBSCT study, in which several p otentially important parameters were studied including the optimal time for stem cell co llection, the dose of stem cell reinfusion, the time of hematopoietic reconsti tution, the disease free survival (DFS) and overall survival (OS), complication s related to transplantation, and maintenance chemotherapy after auto-PBSCT. Results After APBSCT, 3-year and 5-year survival rates of NHL were 83.3%; those of AM L were 74.7%; those of MM were 37.9% and 19%; those of ALL were 40% and 0% res pectively. Hematopoietic reconstitution was greatly promoted by granulocyte col ony stimulating factor (G-CSF). The mean time for patients’ neutrophil to reco ver up to &gt;0.5×10(9) /L after APBSCT was 11.14 days in the group of the patien ts receiving G-CSF in contrast to 17.6 days in the group receiving no G-CSF. The most common complications of transplantation were fever, liver dysfunction and hypokalaemia, which were curable. No death was due to transplantation related complications.Conclusion Comparing with conventional chemotherapy, our study suggests that auto-PBSCT i s a very important therapeutic option that can significantly improve the prognos is in the patients with hematological and solid tumors, especially in the patien ts with AML and NHL.     

Effects of benactyzine on action potentials and contractile force of guinea pig papillary muscles

ＩＮＴＲＯＤＵＣＴＩＯＮＢｅｎａｃｔｙｚｉｎｅｉｓａｓｙｎｔｈｅｔｉｃｂｌｏｃｋｅｒｏｆＭ ｒｅｃｅｐｔｏｒｐｏｓ ｓｅｓｓｉｎｇｓｍｏｏｔｈｍｕｓｃｌｅｒｅｌａｘａｎｔｐｒｏｐｅｒｔｉｅｓａｎｄｑｕｉｎｉｄｉｎｅ ｌｉｋｅａｃｔｉｏｎｏｎｈｅａｒｔ[1] .Ｂｅｎａｃｔｙｚｉｎｅｉｓｅｆｆｅｃｔｉｖｅｉｎｒｅｓｔｏｒ ｉｎｇｃｉｒｃｕｌａｔｏｒｙｆｕｎｃｔｉｏｎｄｉｓｔｕｒｂｅｄｂｙｏｒｇａｎｏｐｈｏｓｐｈａｔｅｐｏｉ ｓｏｎｉｎｇ[2 ,3] .Ｐｒｅｖｉｏｕｓｓｔｕｄｉｅｓｓｕｇｇｅｓｔｅｄｔｈａｔｂｅｎａ…     

姜黄素与羟基脲对K562细胞的体外联合作用

目的 了解姜黄素与羟基脲合用对人白血病Ｋ５６２细胞的体外作用。方法 采用ＭＴＴ法测定药物的体外杀伤作用,应用ＡＯ／ＥＢ荧光染料染色观察药物诱导细胞凋亡,金氏公式进行联合用药分析。结果 姜黄素５,１０ｕｇ／ｍｌ,羟基脲２５,５０ｕｇ／ｍｌ同时给药,对Ｋ５６２细胞可产生单纯相加的协同杀伤效果。姜黄素与羟基脲同时给药诱导Ｋ５６２细胞凋亡率高于羟基脲单独用药,低于姜黄素单独用药。结论 姜黄素与羟基脲同时联     

THAP11通过抑制p53的泛素化影响食管癌细胞的增殖和凋亡

目的：探讨死亡相关蛋白(thanatos-associated protein,THAP)11对食管癌细胞增殖和凋亡的影响及其潜在 的机制。方法：采用蛋白质印迹法检测人食管上皮细胞Het-1A和人食管癌细胞(Eca109,TE-1和Ec 9706)中THAP11的 表达。将食管癌TE-1细胞分为空白对照(NC)组、阴性对照(LV-LC)组、TRA P11(LV-TRA P11)组,按分组处理细胞后, 采用MTT 法检测细胞活力,流式细胞术检测细胞凋亡,caspases试剂盒检测caspase-3和caspase-9的活性。采用体外泛素 化实验检测TE-1细胞的p53泛素化水平。结果：与Het-1A细胞相比,食管癌细胞中THAP11的表达显著下降(P<0.05)。 LV-THAP11转染食管癌细胞后,细胞活力降低(P<0.05),凋亡率升高(P<0.05),caspase-3和caspase-9活性升高(P<0.05)。 THAP11能够提高食管癌细胞中p53蛋白的表达(P<0.05)。与LV-LC组相比,转染THAP11后食管癌细胞中p53的表达上调 (P<0.05),MDM2调节的p53的泛素化也被抑制。结论：THAP11通过抑制p53的泛素化抑制食管癌细胞的增殖,促进食管 癌细胞的凋亡。