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Acta Pharmaceutica Sinica. B

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https://www.readbyqxmd.com/read/28924554/molecular-cloning-and-functional-identification-of-sterol-c24-methyltransferase-gene-from-tripterygium-wilfordii
#1
Hongyu Guan, Yujun Zhao, Ping Su, Yuru Tong, Yujia Liu, Tianyuan Hu, Yifeng Zhang, Xianan Zhang, Jia Li, Xiaoyi Wu, Luqi Huang, Wei Gao
Sterol C24-methyltransferase (SMT) plays multiple important roles in plant growth and development. SMT1, which belongs to the family of transferases and transforms cycloartenol into 24-methylene cycloartenol, is involved in the biosynthesis of 24-methyl sterols. Here, we report the cloning and characterization of a cDNA encoding a sterol C24-methyltransferase from Tripterygium wilfordii (TwSMT1). TwSMT1 (GenBank access number KU885950) is a 1530 bp cDNA with a 1041 bp open reading frame predicted to encode a 346-amino acid, 38...
September 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28924553/amino-functionalized-poloxamer-407-with-both-mucoadhesive-and-thermosensitive-properties-preparation-characterization-and-application-in-a-vaginal-drug-delivery-system
#2
Liqian Ci, Zhigang Huang, Yu Liu, Zhepeng Liu, Gang Wei, Weiyue Lu
Lack of mucoadhesive properties is the major drawback to poloxamer 407 (F127)-based in situ hydrogels for mucosal administration. The objective of the present study was to construct a novel mucoadhesive and thermosensitive in situ hydrogel drug delivery system based on an amino-functionalized poloxamer for vaginal administration. First, amino-functionalized poloxamer 407 (F127-NH2) was synthesized and characterized with respect to its micellization behavior and interaction with mucin. Then using acetate gossypol (AG) as model drug, AG-loaded F127-NH2-based in situ hydrogels (NFGs) were evaluated with respect to rheology, drug release, ex vivo vaginal mucosal adhesion, in vivo intravaginal retention and local irritation after vaginal administration to healthy female mice...
September 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28924552/schisandra-sphenanthera-extract-wuzhi-tablet-protects-against-chronic-binge-and-acute-alcohol-induced-liver-injury-by-regulating-the-nrf2-are-pathway-in-mice
#3
Xuezhen Zeng, Xi Li, Chenshu Xu, Fulin Jiang, Yufei Mo, Xiaomei Fan, Yaoting Li, Yiming Jiang, Dongshun Li, Min Huang, Huichang Bi
Alcohol abuse leads to alcoholic liver disease and no effective therapy is currently available. Wuzhi Tablet (WZ), a preparation of extract from Schisandra sphenanthera that is a traditional hepato-protective herb, exerted a significant protective effect against acetaminophen-induced liver injury in our recent studies, but whether WZ can alleviate alcohol-induced toxicity remains unclear. This study aimed to investigate the contribution of WZ to alcohol-induced liver injury by using chronic-binge and acute models of alcohol feeding...
September 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28924551/identification-and-characterization-of-loop7-motif-and-its-role-in-regulating-biological-function-of-human-apobec3g-through-molecular-modeling-and-biological-assay
#4
Congjie Zhai, Ling Ma, Zhixin Zhang, Jiwei Ding, Jing Wang, Yongxin Zhang, Xiaoyu Li, Fei Guo, Liyan Yu, Jinming Zhou, Shan Cen
Human APOBEC3G (hA3G) is a cytidine deaminase which inhibits HIV-1 replication. The HIV-1 accessory protein viral infectivity factor (Vif) counteracts with hA3G by targeting it for proteasomal degradation. In this work, we constructed and optimized molecular models of the hA3G dimer and the hA3G-Vif complex. The molecular modeling study revealed that the loop7 motif of hA3G appears on the interfaces of both the hA3G-Vif complex and the hA3G dimer. Biochemical analysis provided evidence suggesting that binding of Vif to hA3G results in steric blocking of hA3G dimerization, implying that monomeric hA3G serves as a substrate for Vif-mediated degradation...
September 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28924550/establishment-and-characterization-of-arsenic-trioxide-resistant-kb-ato-cells
#5
Yun-Kai Zhang, Chunling Dai, Chun-Gang Yuan, Hsiang-Chun Wu, Zhijie Xiao, Zi-Ning Lei, Dong-Hua Yang, X Chris Le, Liwu Fu, Zhe-Sheng Chen
Arsenic trioxide (ATO) is used as a chemotherapeutic agent for the treatment of acute promyelocytic leukemia. However, increasing drug resistance is reducing its efficacy. Therefore, a better understanding of ATO resistance mechanism is required. In this study, we established an ATO-resistant human epidermoid carcinoma cell line, KB/ATO, from its parental KB-3-1 cells. In addition to ATO, KB/ATO cells also exhibited cross-resistance to other anticancer drugs such as cisplatin, antimony potassium tartrate, and 6-mercaptopurine...
September 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28924549/potassium-2-1-hydroxypentyl-benzoate-attenuates-neuronal-apoptosis-in-neuron-astrocyte-co-culture-system-through-neurotrophy-and-neuroinflammation-pathway
#6
Dongmei Liu, Man Zhang, Xianfang Rong, Jiang Li, Xiaoliang Wang
Potassium 2-(1-hydroxypentyl)-benzoate (d,l-PHPB), a new drug candidate for ischemic stroke at the phase II clinic trial, has been shown to protect neurons by inhibiting oxidative injury and reducing neuron apoptosis in previous studies. But the mechanisms of d,l-PHPB remain to be studied. In this study, a neuron-astrocytes co-culture system was used to elucidate the roles of astrocytes in neuroprotection of d,l-PHPB under oxygen-glucose deprivation/reoxygenation (OGD/R) condition. Our data showed that d,l-PHPB reduced neuronal apoptosis in mono-culture system and this effect was enhanced in neuron-astrocyte co-culture system under the OGD/R condition...
September 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28924548/remodeling-the-blood-brain-barrier-microenvironment-by-natural-products-for-brain-tumor-therapy
#7
REVIEW
Xiao Zhao, Rujing Chen, Mei Liu, Jianfang Feng, Jun Chen, Kaili Hu
Brain tumor incidence shows an upward trend in recent years; brain tumors account for 5% of adult tumors, while in children, this figure has increased to 70%. Moreover, 20%-30% of malignant tumors will eventually metastasize into the brain. Both benign and malignant tumors can cause an increase in intracranial pressure and brain tissue compression, leading to central nervous system (CNS) damage which endangers the patients' lives. Despite the many approaches to treating brain tumors and the progress that has been made, only modest gains in survival time of brain tumor patients have been achieved...
September 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28752041/isocartormin-a-novel-quinochalcone-c-glycoside-from-carthamus-tinctorius
#8
Feng Li, Zhisheng He, Yang Ye
A new semi-quinonechalcone C-glycoside isocartormin along with cartormin and safflomin C were isolated from the water extract of Carthamus tinctorius L. The structure of isocartormin was determined by extensive analysis of HR-MS, 1D- and 2D NMR data, and by comparison with those of cartormin reported previously by our group. Isocartormin was identified as a diastereoisomer of cartormin with a reverse configuration at C-18.
July 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28752040/the-reaction-of-cinnamaldehyde-and-cinnam-o-yl-derivatives-with-thiols
#9
Alessandro Autelitano, Alberto Minassi, Alberto Pagani, Orazio Taglialatela-Scafati, Giovanni Appendino
Spurred by the alleged relevance of the thia-Michael reaction in the bioactivity of various classes of cinnam(o)yl natural products and by the development of a quick NMR assay to study this reaction, we have carried out a systematic study of the "native" reactivity of these compounds with dodecanethiol and cysteamine as models, respectively, of simple thiols and reactive protein thiols that can benefit from iminium ion catalysis in Michael reactions. Cinnamoyl esters and amides, as well as cinnamyl ketones and oximes, did not show any reactivity with the two probe thiols, while cinnamaldehyde (1a) reacted with cysteamine to afford a mixture of a thiazoline derivative and compounds of multiple addition, and with aliphatic thiols to give a single bis-dithioacetal (6)...
July 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28752039/arylamine-n-acetyltransferase-2-genotype-dependent-n-acetylation-of-isoniazid-in-cryopreserved-human-hepatocytes
#10
Mark A Doll, Raúl A Salazar-González, Srineil Bodduluri, David W Hein
Cryopreserved human hepatocytes were used to investigate the role of arylamine N-acetyltransferase 2 (NAT2; EC 2.3.1.5) polymorphism on the N-acetylation of isoniazid (INH). NAT2 genotype was determined by Taqman allelic discrimination assay and INH N-acetylation was measured by high performance liquid chromatography. INH N-acetylation rates in vitro exhibited a robust and highly significant (P<0.005) NAT2 phenotype-dependent metabolism. N-acetylation rates in situ were INH concentration- and time-dependent...
July 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28752038/steroids-hydroxylation-catalyzed-by-the-monooxygenase-mutant-139-3-from-bacillus-megaterium-bm3
#11
Xing Liu, Jian-Qiang Kong
The search of new substrates with pharmaceutical and industrial potential for biocatalysts including cytochrome P450 enzymes is always challenging. Cytochrome P450 BM3 mutant 139-3, a versatile biocatalyst, exhibited hydroxylation activities towards fatty acids and alkanes. However, there were limited reports about its hydroxylation activity towards steroids. Herein, an Escherichia coli-based whole-cell extract containing the recombinant 139-3 protein was used as the biocatalyst to screen 13 steroids. Results revealed that 139-3 was able to specifically hydroxylate androstenedione (1) at 1α-position, generating a hydroxylated steroid 1α-OH-androstenedione (1a)...
July 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28752037/in-vivo-retention-of-poloxamer-based-in-situ-hydrogels-for-vaginal-application-in-mouse-and-rat-models
#12
Yu Liu, Fujin Yang, Linglin Feng, Long Yang, Lingyun Chen, Gang Wei, Weiyue Lu
The purpose of this study is to evaluate the in vivo retention capabilities of poloxamer-based in situ hydrogels for vaginal application with nonoxinol-9 as the model drug. Two in situ hydrogel formulations, which contained 18% poloxamer 407 plus 1% poloxamer 188 (GEL1, relative hydrophobic) or 6% poloxamer 188 (GEL2, relative hydrophilic), were compared with respect to the rheological properties, in vitro hydrogel erosion and drug release. The vaginal retention capabilities of these hydrogel formulations were further determined in two small animal models, including drug quantitation of vaginal rinsing fluid in mice and isotope tracing with (99m)Tc in rats...
July 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28752036/crystal-structures-absolute-configurations-and-molecular-docking-studies-of-naftopidil-enantiomers-as-%C3%AE-1d-adrenoceptor-antagonists
#13
Wei Xu, Junjun Huang, Renwang Jiang, Mu Yuan
Chiral drug naftopidil (NAF), a specific α1D-adrenoceptor (AR) antagonist for the treatment of benign prostatic hyperplasia, was used in racemic form for several decades. Our recent work declared that NAF enantiomers showed the same antagonistic effects on the α1D-AR, but the binding mechanism of these two stereochemical NAF isomers to the α1D receptor remained unclear. Herein, we reported the crystallographic structures of optically pure NAF stereoisomers for the first time and unambiguously determined their absolute configurations...
July 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28752035/nine-compounds-from-the-root-bark-of-lycium-chinense-and-their-anti-inflammatory-activitieslammatory-activitiesretain
#14
Yanan Yang, Yawen An, Wei Wang, Ning Du, Jinghua Zhang, Ziming Feng, Jianshuang Jiang, Peicheng Zhang
Two new compounds, named lyciumlignan D (1) and lyciumphenyl propanoid A (2), along with seven known compounds, were isolated from the root bark of Lycium chinense. Their structures were elucidated using spectroscopic data (UV, IR, HR-ESI-MS, 1D and 2D NMR, CD), as well as by comparison with those of the literature. Compounds 3-9 were isolated from this genus for the first time. In the in vitro assay, compounds 3, 6, and 7 exhibited stronger anti-inflammatory effects than the positive control curcumin at a concentration of 10 μmol/L...
July 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28752034/phytochemical-study-of-illicium-angustisepalum-and-its-biological-activities
#15
Karina M Szymulanska-Ramamurthy, Ming Zhao, Chun-Tao Che
Sixteen compounds, including two new natural products (1 and 2), were obtained from the twigs of Illicium angustisepalum. The structures were elucidated based on NMR, MS, IR data and optical rotation values. Compounds 4, 5, 6 and 8 displayed moderate antibacterial activities against clinical isolates; compounds 4, 5, 8, 9 and 15 protected neural cells against oxidative stress; and compounds 10 and 14 exhibited anti-acetylcholinesterase activity.
July 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28752033/3-5-bis-arylidene-4-piperidones-as-potential-dengue-protease-inhibitors
#16
Hasnah Osman, Nor Hashima Idris, Ezatul Ezleen Kamarulzaman, Habibah A Wahab, Mohd Zaheen Hassan
Dengue is a severe mosquito-borne viral infection causing half a million deaths annually. Dengue virus NS2B/NS3 protease is a validated target for anti-dengue drug design. A series of hitherto unreported 3,5-bis(arylidene)-4-piperidones analogues 4a-4j were synthesized and screened in silico against DENV2 NS2B/NS3 protease to elucidate their binding mechanism and orientation around the active sites. Results were validated through an in vitro DENV2 NS2B/NS3 protease assay using a fluorogenic Boc-Gly-Arg-Arg-AMC substrate...
July 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28752032/potassium-2-l-hydroxypentyl-benzoate-attenuates-neuroinflammatory-responses-and-upregulates-heme-oxygenase-1-in-systemic-lipopolysaccharide-induced-inflammation-in-mice
#17
Chunyang Zhao, Weizhen Hou, Hui Lei, Longjian Huang, Shan Wang, Dandan Cui, Changhong Xing, Xiaoliang Wang, Ying Peng
A neuroinflammatory response is commonly involved in the progression of many neurodegenerative diseases. Potassium 2-(1-hydroxypentyl)-benzoate (PHPB), a novel neuroprotective compound, has shown promising effects in the treatment of ischemic stroke and Alzheimer׳s disease (AD). In the present study, the anti-inflammatory effects of PHPB were investigated in the plasma and brain of C57BL/6 mice administered a single intraperitoneal (i.p.) injection of lipopolysaccharide (LPS). Levels of iNOS and the cytokines TNFα, IL-1β and IL-10 were elevated in plasma, cerebral cortex and hippocampus after LPS injection and the number of microglia and astrocytes in cortex and hippocampus were increased...
July 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28752031/anti-diabetic-effects-and-mechanisms-of-action-of-a-chinese-herbal-medicine-preparation-jq-r-in-vitro-and-in-diabetic-kk-ay-mice
#18
Quan Liu, Shuainan Liu, Lihui Gao, Sujuan Sun, Yi Huan, Caina Li, Yue Wang, Nan Guo, Zhufang Shen
Refined-JQ (JQ-R) is a mixture of refined extracts from Coptis chinensis (Ranunculaceae), Astragalus membranaceus (Leguminosae) and Lonicera japonica (Caprifoliaceae), the three major herbs of JinQi-JiangTang tablet, a traditional Chinese medicine (TCM) formula. The mechanisms by which JQ-R regulates glucose metabolism and improves insulin sensitivity were studied in type 2 diabetic KK(Ay) mice and insulin-resistant L6 myotubes. To investigate the mechanisms by which JQ-R improves insulin sensitivity, a model of insulin-resistant cells induced with palmitic acid (PA) was established in L6 myotubes...
July 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28752030/syringaresinol-4-o-%C3%AE-d-glucoside-alters-lipid-and-glucose-metabolism-in-hepg2-cells-and-c2c12-myotubes
#19
Shuai Wang, Chongming Wu, Xin Li, Yue Zhou, Quanyang Zhang, Fuchao Ma, Jianhe Wei, Xiaopo Zhang, Peng Guo
Syringaresinol-4-O-β-d-glucoside (SSG), a furofuran-type lignan, was found to modulate lipid and glucose metabolism through an activity screen of lipid accumulation and glucose consumption, and was therefore considered as a promising candidate for the prevention and treatment of metabolic disorder, especially in lipid and glucose metabolic homeostasis. In this study, the effects of SSG on lipogenesis and glucose consumption in HepG2 cells and C2C12 myotubes were further investigated. Treatment with SSG significantly inhibited lipid accumulation by oil red O staining and reduced the intracellular contents of total lipid, cholesterol and triglyceride in HepG2 cells...
July 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28752029/advances-in-ultrasound-targeted-microbubble-mediated-gene-therapy-for-liver-fibrosis
#20
REVIEW
Cuiyuan Huang, Hong Zhang, Ruidan Bai
Hepatic fibrosis develops as a wound-healing scar in response to acute and chronic liver inflammation and can lead to cirrhosis in patients with chronic hepatitis B and C. The condition arises due to increased synthesis and reduced degradation of extracellular matrix (ECM) and is a common pathological sequela of chronic liver disease. Excessive deposition of ECM in the liver causes liver dysfunction, ascites, and eventually upper gastrointestinal bleeding as well as a series of complications. However, fibrosis can be reversed before developing into cirrhosis and has thus been the subject of extensive researches particularly at the gene level...
July 2017: Acta Pharmaceutica Sinica. B
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