科素亚与卡托普利治疗高血压的对比研究

目的 :对比、观察科素亚在治疗高血压中的临床疗效及不良反应。方法 :将 3 0例轻、中度高血压病人随机分为科素亚 L组及卡托普利 C组。在治疗前、后观察血压变化及不良反应并记录之。结果 :1科素亚组在治疗后 SBP下降 1 .3 3～ 2 k Pa(P<0 .0 5 ) ,DBP下降 0 .67k Pa(P>0 .0 5 )。 2科素亚组起效时间在用药后 1 0～ 1 4d,卡托普利组在治疗后 5～ 7d起效。3科素亚组未见不良反应 ,卡托普利组有 3例出现不良反应。结论 :科素亚对于轻、中度高血压有肯定的降压效果 (尤其 SBP) ;降压作用较为平和、缓慢 ,适合老年人使用 ;不良反应少 ,是一安全有效的药物。     

维生素E和二甲亚砜对油酸型ARDS防治作用的研究

目的 研究氧化性肺损伤在成人呼吸窘迫综合征（ＡＲＤＳ）发病中的作用及维生素Ｅ和二甲亚砜的抗氧化保护作用。方法 将２８只大鼠随机分成４组：油酸组,ＶＥ组,ＤＭＳＯ组,正常对照组。油酸于尾静脉注入,维生素Ｅ和二甲亚砜由腹腔注射。注油酸后２ｈ观察肺系数,肺组织ＭＤＡ含量,ＰａＯ２及肺组织病理改变。结果 ＶＥ组和ＤＭＳＯ组较油酸组肺系数,ＭＤＡ含量降低,ＰａＯ２同,肺组织病理改变明显减轻。     

Effect of biphenyl dimethyl dicarboxylate on the cellular and nonspecific immunosuppressions by ketoconazole in mice

The effect of biphenyl dimethyl dicarboxylate (PMC) on the cellular and nonspecific immunosuppressions by ketoconazole (KCZ) was investigated in ICR mice. PMC at a dose of 6 mg/kg was administered orally to mice daily for 14 consecutive days. KCZ was suspended in RPMI 1640 medium and orally administered at 160 mg/kg/day 2 hrs after the administration of PMC. Immune responses of the delayed-type hypersensitivity (DTH) reaction to sheep red blood cells (SRBC), phagocytic activity and natural killer (NK) cell activity were evaluated. DTH reaction to SRBC was enhanced to normal level by the combination of PMC and KCZ, compared with treatment of KCZ alone. In the combination of PMC and KCZ, as compared with the treatment of KCZ alone, there were also significant increases in activities of natural killer (NK) cells and phagocytes along with circulating leukocytes. These findings indicate that PMC shows a significant restoration from the immunotoxic status induced by KCZ.     

二甲基亚砜对培养人视网膜色素上皮细胞增殖的影响

目的　探讨细胞分化诱导剂及端粒酶抑制剂二甲基亚砜 (dimethylsulfoxide ,DMSO)对人视网膜色素上皮细胞增殖的抑制作用。方法　本研究分实验组和对照组 ,对照组弃原培养液 ,加无血清培养液继续培养 ,实验组用不同浓度的DMSO 5、10、2 0、4 0mL·L-1分别作用于人RPE细胞 2 4、4 8、72、96h ,用MTT法检测DMSO对hRPE细胞生长的影响 ,流式细胞仪检测DMSO对hRPE细胞周期的影响。结果　 10mL·L-1DMSO处理的hRPE细胞从作用 4 8h开始 ,OD值 ( 0 .5 37± 0 .0 10 )小于对照组 ( 0 .6 4 7± 0 .0 2 2 ) ,有显著性差异 (P <0 .0 0 1) ,细胞生长受到抑制 ,且随浓度增加及作用时间延长 ,抑制越显著。流式细胞仪检测 2 0mL·L-1DMSO作用 72h细胞周期发生明显变化 ,G1期细胞由4 1 31%增加至 5 9.6 5 % ,S期由 32 .0 9%减至 2 1.2 1% ,G2 期由 2 6 .6 5 %减至 19 14 % ,细胞生长被阻滞在G1期 ,生长受到抑制。结论　DMSO能阻滞hRPE细胞于G1期 ,抑制hRPE细胞增殖且呈剂量依赖性。     

司帕沙星、联苯乙酸对大鼠海马神经元GABA-A和离子型谷氨酸受体的作用(英文)

目的 :观察司帕沙星单用和与联苯乙酸合用时 ,对γ 氨基丁酸 (GABA) ,NMDA ,AMPA和海人藻酸诱导电流的作用。方法 :应用全细胞式膜片钳技术在急性打散的新生大鼠海马锥体神经元上记录GABA ,NMDA ,AMPA和海人藻酸的诱导电流。结果 :司帕沙星 1mmol·L- 1对GABA诱导的电流有迅速可逆的抑制作用 ,抑制率为 (4 7.6±s2 .9) % ,而联苯乙酸 10 μmol·L- 1无抑制作用。但联苯乙酸 (10 μmol·L- 1)与司帕沙星 1mmol·L- 1合用时 ,稍稍增强抑制作用 ,司帕沙星单用或合用联苯乙酸 (10 μmol·L- 1)对GABA诱导电流的IC50 分别为 (2 38± 2 1) μmol·L- 1和 (89± 5 ) μmol·L- 1。司帕沙星、联苯乙酸或司帕沙星合用联苯乙酸对NM DA ,AMPA和海人藻酸诱导的电流无明显作用。结论 :提示司帕沙星 ,或与联苯乙酸合用时所产生的中枢神经毒性可能与抑制GABA诱导的电流有关 ,而与NMDA ,AMPA和海人藻酸诱导的电流无关。     

Blood-Brain Barrier Permeability of Asiaticoside,Madecassoside and Asiatic Acid in Porcine Brain Endothelial Cell Model

Neurotherapeutic potentials of Centella asiatica and its reputation to boost memory, prevent cognitive deficits and improve brain functions are widely acknowledged. The plant's bioactive compounds, i.e. asiaticoside, madecassoside and asiatic acid were reported to have central nervous system (CNS) actions, particularly in protecting the brain against neurodegenerative disorders. Hence, it is important for these compounds to cross the blood-brain barrier (BBB) to be clinically effective therapeutics. This study aimed to explore the capability of asiaticoside, madecassoside and asiatic acid to cross the BBB using in vitro BBB model from primary porcine brain endothelial cells (PBECs). Our findings showed that asiaticoside, madecassoside and asiatic acid are highly BBB permeable with apparent permeability (P_app) of 70.61 ± 6.60, 53.31 ± 12.55 and 50.94 ± 10.91 × 10^?6 cm/s respectively. No evidence of cytotoxicity and tight junction disruption of the PBECs were observed in the presence of these compounds. Asiatic acid showed cytoprotective effect towards the PBECs against oxidative stress. This study reported for the first time that Centella asiatica compounds demonstrated high capability to cross the BBB, comparable to central nervous system drugs, and therefore warrant further development as therapeutics for the treatment of neurodegenerative diseases.     

Proper Fitting and Use of Crutches

In brief: Injured athletes who need crutches must be fitted correctly and taught their proper use to help prevent further injury, undue complications, and discouragement. Crutches should reach to about two finger widths below the armpit, and the handgrip should be adjusted so the elbow is flexed 25° to 30° with the wrist straight. The weight should be supported through the palms on the handgrips. The three-point gait is used when only one foot, ankle, or knee is injured. Proper instruction is extremely important for negotiating stairs.     

Nobiletin and its derivatives overcome multidrug resistance (MDR) in cancer: total synthesis and discovery of potent MDR reversal agents

Our recent studies demonstrated that the natural product nobiletin (NOB) served as a promising multidrug resistance (MDR) reversal agent and improved the effectiveness of cancer chemotherapy in vitro. However, low aqueous solubility and difficulty in total synthesis limited its application as a therapeutic agent. To tackle these challenges, NOB was synthesized in a high yield by a concise route of six steps and fourteen derivatives were synthesized with remarkable solubility and efficacy. All the compounds showed improved sensitivity to paclitaxel (PTX) in P-glycoprotein (P-gp) overexpressing MDR cancer cells. Among them, compound 29d exhibited water solubility 280-fold higher than NOB. A drug-resistance A549/T xenograft model showed that 29d, at a dose of 50 mg/kg co-administered with PTX (15 mg/kg), inhibited tumor growth more effective than NOB and remarkably increased PTX concentration in the tumors via P-gp inhibition. Moreover, Western blot experiments revealed that 29d inhibited expression of NRF2, phosphorylated ERK and AKT in MDR cancer cells, thus implying 29d of multiple mechanisms to reverse MDR in lung cancer.