Potential role of ATP-binding cassette transporters in the intestinal transport of rhein

Rhein, a lipophilic anthraquinone, exhibits anti-inflammatory and anti-tumor activities; however, it is hepatotoxic. ATP-binding cassette transporters, including P-glycoprotein (P-gp), breast cancer resistance protein (BCRP) and multidrug resistance-associated protein 2 (MRP2), can pump toxicants from gut epithelial cells back into the intestinal lumen to prevent poisoning. We investigated their roles in rhein transport using a rat intestinal perfusion model and Caco-2, MDCKII-MDR1 (high expression of P-gp), MDCKII-BCRP (high expression of BCRP) and MDCKII-MRP2 (high expression of MRP2) cell models. The permeability of rhein in the duodenum significantly increased with increasing perfused concentration of rhein in the rat model, suggesting that efflux transporters were involved in rhein transport. In the Caco-2 cells, the permeability of rhein from the basolateral (B) to the apical (A) was significantly higher than that from A to B. In the presence of BCRP or MRP2 inhibitor, the permeability of rhein significantly decreased from B to A direction. In the MDCKII-BCRP cells, rhein was more permeable in B to A side than that in the opposite side. However, no significant differences of rhein permeability were observed in two directions in both MDCKII-MDR1 and MDCKII-MRP2 cells. Taken together, these results suggested that only BCRP was involved in rhein transport.     

治疗耐多药结核病新药贝达喹啉

结核病是一种严重危害人类健康的慢性传染病,而其中的耐多药结核已成为结核病控制工作的巨大挑战之一。贝达喹啉(bedaquiline)作为美国食品与药物管理局批准的首个治疗耐多药结核病药物,必将在结核病防治领域发挥巨大作用。本文依据最新文献报道,从作用机制、临床研究、安全性等方面综述了新药贝达喹啉在治疗耐多药结核病方面的优缺点,对其合成路线进行了评述,最后对该药的临床应用前景进行了展望。     

The accumulation study of 90Sr in fish from a fishpond of northern Taiwan

Three kinds of fish from a natural fishpond in the north of Taiwan were collected and analyzed in this study. The three species were non-predatory Ctenopharyn odon idellus, predatory Aristichthys nobilis and predatory Mylopharyngodon piceus. The activity concentrations of ⁹⁰Sr in bone and edible flesh of fish, as well as in water and soil of fishpond were measured by using the radiochemical analysis. Additionally, the concentration of stable calcium in fish bone, [Ca]_bone, and that of stable strontium in fish bone, [Sr]_bone, were measured by ICP-AES. From the results, the concentration factors of ⁹⁰Sr, CF(⁹⁰Sr), in fish bone was no statistic difference between non-predatory and predatory fish. Besides, the accumulation of ⁹⁰Sr in the non-predatory fish remarkably decreased with increasing the fish weight. As for the predatory fish, they both showed no statistically significant correlations between the ⁹⁰Sr activity concentration and the fish weight. Regarding the activity concentrations of ⁹⁰Sr in fish bone, all the fish were observed positively correlated with the measured [Sr]_bone.     

巴马神酒调节免疫及抗脂质过氧化药理作用研究

摘 要 目的： 观察巴马神酒对小鼠免疫功能、肝脏脂质过氧化损伤及游泳耐力的药理作用。方法: 采用碳粒廓清实验法及环磷酰胺致小鼠免疫低下模型评价巴马神酒对免疫功能的作用;建立四氯化碳致小鼠急性肝损伤模型,以血清中丙氨酸氨基转移酶（ALT）、天门冬氨酸转移酶（AST）、超氧化物歧化酶（SOD）以及丙二醛（MDA）的水平,评价巴马神酒抗肝脏脂质过氧化损伤作用;以小鼠负重游泳的持续时间,评价巴马神酒提高游泳耐力的功能。结果: 巴马神酒能提高小鼠吞噬指数K及吞噬系数α（与空白组比较,P<0.01或P<0.05）;对环磷酰胺诱发的胸腺、脾脏脏器指数的下降有一定的提高（与模型组比较,P<0.05）;能够降低四氯化碳致小鼠急性肝损伤血清中AST、ALT含量,降低血清MDA的含量,增强SOD的活性（与模型组比较,P<0.01或P<0.05）;可以延长小鼠负重游泳时间（与空白组比较,P<0.01或P<0.05）。结论: 巴马神酒具有提升小鼠巨噬细胞吞噬能力、保护免疫低下小鼠的胸腺和脾脏指数的作用,并具有抗肝脏脂质过氧化损伤和提高游泳耐力的作用。     

Pharmacogenomics and personalized medicine: a review focused on their application in the Chinese population

The field of pharmacogenomics was initiated in the 1950s and began to thrive after the completion of the human genome project 10 years ago. Thus far, more than 100 drug labels and clinical guidelines referring to pharmacogenomic biomarkers have been published, and several key pharmacogenomic markers for either drug safety or efficacy have been identified and subsequently adopted in clinical practice as pre-treatment genetic tests. However, a tremendous variation of genetic backgrounds exists between different ethnic groups. The application of pharmacogenomics in the Chinese population is still a long way off, since the published guidelines issued by the organizations such as US Food and Drug Administration require further confirmation in the Chinese population. This review highlights important pharmacogenomic discoveries in the Chinese population and compares the Chinese population with other nations regarding the pharmacogenomics of five most commonly used drugs, ie, tacrolimus, cyclosporine A, warfarin, cyclophosphamide and azathioprine.     

Correction: A colorimetric and far-red fluorescent probe for the highly sensitive detection of silver(i)

Correction for ‘A colorimetric and far-red fluorescent probe for the highly sensitive detection of silver(i)’ by Yong-jun Wang et al., RSC Adv., 2017, 7, 55567–55570.

The published article incorrectly indicates four corresponding authors. The two corresponding authors should be Jin-wu Yan and Lei Zhang. In addition, a link to the equal contribution footnote, confirming that Yong-jun Wang and Jing-gong Liu contributed equally to the work, is missing in the published article. These errors are corrected herein.The Royal Society of Chemistry apologises for these errors and any consequent inconvenience to authors and readers.     

A coumarin Schiff's base two-photon fluorescent probe for hypochlorite in living cells and zebrafish

Selective and sensitive fluorescent probes for ClO⁻ are desirable due to the importance of ClO⁻ in biological processes. Here, a coumarin Schiff''s base, compound 1, has been developed and successfully used as a one- and two-photon fluorescent probe for ClO⁻ with high selectivity. This probe can recognize ClO⁻ with obvious color change from yellow-green to colorless and green to blue fluorescence emission, which can be observed by the naked eye. The properties of low cytotoxicity and good cell permeability allow it to be used for ClO⁻ detection in living cells and zebrafish by both one- and two-photon microscopy imaging. All these results indicate that the compound is a sensitive probe with potential for analysis of ClO⁻ in biological samples. The mechanism by which probe 1 recognizes ClO⁻ is possibly nucleophilic addition followed by hydrolysis.

A coumarin Schiff''s base compound can selectively recognize ClO⁻ and can be successfully applied to the detection of ClO⁻ in living cells and zebrafish by one- and two-photon fluorescence modes.     

Synthesis,electronic structures,and photoluminescence properties of an efficient and thermally stable red-emitting phosphor Ca3ZrSi2O9:Eu3+,Bi3+ for deep UV-LEDs

A series of red-emitting Ca₃ZrSi₂O₉:Eu³⁺,xBi³⁺ phosphors was synthesized using a conventional high temperature solid-state reaction method, for the purpose of promoting the emission efficiency of Eu³⁺ in a Ca₃ZrSi₂O₉ host. The site preference of Bi³⁺ and Eu³⁺ in the Ca₃ZrSi₂O₉ host was evaluated by formation energy. The effects of Bi³⁺ on electronic structure, luminescent properties, and related mechanisms were investigated. The inner quantum yield of the optimized sample increased to 72.9% (x = 0.08) from 34.6% (x = 0) at 300 nm ultraviolet light excitation. The optimized sample (x = 0.08) also showed excellent thermal stability, and typically, 84.2% of the initial emission intensity was maintained when the temperature increased to 150 °C from 25 °C, which is much higher than that without Bi³⁺ doping (70.1%). The mechanisms of emission properties and thermal stability enhancement, as well as the redshift of the charge transfer band (CTB) induced by Bi³⁺ doping in the Ca₃ZrSi₂O₉:Eu³⁺ phosphor, were discussed. This study elucidates the photoluminescence properties of Bi³⁺-doped Ca₃ZrSi₂O₉:Eu³⁺ phosphor, and indicates that it is a promising luminescent material that can be used in ultraviolet light-emitting diodes.

A red-emitting phosphor Ca₃ZrSi₂O₉:Eu³⁺,Bi³⁺ with high quantum yield and thermal stability was developed by introducing Bi³⁺ as an efficient sensitizer.