Inhibitory effect of clofibrate on arginine-induced insulin secretion in chemical diabetes

Summary Clofibrate, 3g/die for 10 consecutive days, significantly reduced arginine-induced IRI release in chemical diabetics and in normal controls, whether of normal body weight or obese. Blood glucose levels were not affected by clofibrate. In agreement with previous findings, it would appear that clofibrate, administered for short periods, does not lead to a decrease in glucose tolerance. However, studies relating to the effect of chronic clofibrate administration in chemical diabetes are needed in order to be sure that prolonged inhibition of IRI secretion does not lead to overt diabetes.     

肝细胞损伤的分子生物学机制

随着医学研究的不断进展,我们对各种肝脏疾病的病因有了更加深入的了解,对疾病的治疗也渐渐从对症治疗转移到病因治疗,但是,在强调病因学治疗的同时,不应忽略对肝细胞的保护,因为肝细胞损伤是各型肝病共同的病理基础,是各种原因引起肝脏疾病的共同的表现.     

Pulmonary protective efficacy of S-2[2-aminoethylamino] ethyl phenyl sulphide (DRDE-07) and its analogues against sulfur mustard induced toxicity in mice

Our previous study showed that percutaneous sulfur mustard (SM) exposure induced pulmonary toxicity, which was attenuated by DRDE-07 (S-2[2-aminoethylamino] ethyl phenyl sulphide) pretreatment. The present study aimed to evaluate the protective efficacy of DRDE-07 and its analogues viz., DRDE-30 (S-2(2-aminoethyl amino)ethyl propyl sulphide) and DRDE-35 (S-2(2-aminoethyl amino)ethyl butyl sulphide) against SM. Thirty minutes before percutaneous SM (0.8 LD₅₀) exposure, female Swiss mice were orally gavaged with DRDE-07 and its analogues(0.2 LD₅₀). Animals were sacrificed on day 3 and 7, BAL fluid (BALF) and lung tissue were collected for biochemical, histopathological studies. As results, DRDE-07 and its analogues were beneficial in reducing the number of BALF inflammatory cells, protein level, lactate dehydrogenase (LDH) activity, myeloperoxidase (MPO) and β-glucuronidase activity, while content of BALF and lung reduced glutathione level (GSH) were significantly protected. The pretreatment of DRDE-07 and its analogues inhibited the recruitment of inflammatory cells into the lung. The beneficial effects of DRDE-07 and its analogues were attributed to their antioxidant and anti-inflammatory activity. Among the analogues, DRDE-30 exhibited significant beneficial effects as compared to the other two compounds. These analogues may be considered as prototype candidate molecules as there is no effective antidote for SM toxicity.     

Chemical constituents from Trichosanthes cucumeroides

One new triterpenoid, 3β-[(E)-caffeoyloxy]-D:C-friedooleana-7,9(11)-dien-29-oic acid (1) and nine known triterpenoidsidentified as cucurbitacin B (2), 23,24-dihydrocucurbitacin B (3), 23,24-dihydrocu-curbitacin D (4), cucurbitacin D (5), cucurbalsaminol A (6), 3-epi-isocucurbitacin D (7), curbitacin G (8), cucurbitacin J (9) and cucurbitacin I (10)were purified from Trichosanthes cucumeroides. Their structures were confirmed by spectroscopic data analysis and comparison with previous literature. All compounds were obtained from T.cucumeroides for the first time.     

中药炮制对中药化学成分及药效影响的研究进展

中药炮制是中华民族的宝贵财富,是在长时间的临床实践过程中总结出来的。中药材经过炮制加工以后会发生各种化学变化,其化学成分也会发生复杂的变化。本文针对大部分药材所含主要成分,比如苷类、挥发油类、生物碱以及蛋白质类等在炮制前后发生的变化进行归纳总结,同时本文从增效、减毒、缓和药性及产生新功效等方面阐述中药炮制对药效的影响,以期能为相关工作提供参考。     

光磁双模态探针钆-[4,7-双-羧甲基-10-(2-荧光素硫脲乙基)-1,4,7,10-四氮杂环十二烷-1-基]-乙酸络合物合成方法的改进

目的:改进光磁双模态分子探针钆-[4,7-双-羧甲基-10-(2-荧光素硫脲乙基)-1,4,7,10-四氮杂环十二烷-1-基]-乙酸络合物(Gd-DO3A-EA-FITC)的合成及纯化方法。方法:1,4,7,10-四氮杂环十二烷(DOTA)经过取代反应、水解反应、偶联反应、与金属络合反应,合成Gd-DO3A-EA-FITC。结果:改进了Gd-DO3A-EA-FITC的合成路线,分别通过取代反应、水解反应、偶联反应、络合反应得到了光磁双模态分子探针,该反应总收率为34.6%,与原路线(18.0%)相比,总收率增加,各化合物通过核磁共振氢谱、核磁共振碳谱和质谱分析法鉴定后结果正确。改进后的路线避免了取代反应不易控制的缺点,且在纯化分离方面,将载样量少、成本高的制备型高效液相色谱纯化改进为载样量多、简便易操作的柱色谱。结论:改进后的路线改善了反应条件的可控性,并且使化合物纯化分离过程变得更加简易,同时使总收率明显提升。光磁双模态探针可同时将活体磁共振成像与离体光学成像相结合,实现光磁双重同步检测,使二者的检测结果相互验证。可将光磁双模态分子探针应用于脑结构及其功能相关研究,并且经静脉途径给药后可以对脑肿瘤进行研究,因此在脑肿瘤和脑血管相关疾病的药物治疗中能够发挥重要的作用。     

Health Risks Associated with Crude Oil Spill Exposure

Background

Human exposure to crude oil spills is associated with multiple adverse health effects including hematopoietic, hepatic, renal, and pulmonary abnormalities. The purpose of this study was to assess the hematological and liver function indices among the subjects participating in the Gulf oil spill cleanup operations in comparison with the standardized normal range reference values.

Methods

Using medical charts, clinical data (including white blood cell [WBC] count, platelet count, hemoglobin, hematocrit, blood urea nitrogen [BUN] creatinine, alkaline phosphatase [ALP], aspartate amino transferase [AST], alanine amino transferase [ALT], and urinary phenol) were gathered for the subjects who were exposed to the Gulf oil spill and analyzed.

Results

A total of 117 subjects exposed to the oil spill were included. Over 77% of subjects had WBC counts in the mid range (6-10 × 10³ per μL), while none of the subjects had the upper limit of the normal range (11 × 10³ per μL). A similar pattern was seen in the platelet counts and BUN levels among the oil spill-exposed subjects. Conversely, over 70% of the subjects had creatinine levels toward the upper limit of the normal range and 23% of subjects had creatinine levels above the upper limit of the normal range (>1.3 mg per dL). Similarly, hemoglobin and hematocrit levels were toward the upper limit of normal in more than two thirds of the subjects. AST and ALT levels above the upper limit of normal range (>40 IU per L) were seen in 15% and 31% of subjects, respectively. Over 80% of subjects had urinary phenol levels higher than detectable levels (2 mg per L).

Conclusion

The results of this study support our earlier study findings in which we found that people who participated in oil spill cleanup activities are at risk of developing alterations in hematological profile and liver function.