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Acta Pharmaceutica Sinica. B

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https://www.readbyqxmd.com/read/28119815/synthesis-of-hydroxycinnamic-acid-derivatives-as-mitochondria-targeted-antioxidants-and-cytotoxic-agents
#1
Jiyu Li, Dian He, Baitao Wang, Ling Zhang, Kun Li, Qinjian Xie, Lifang Zheng
In order to develop agents with superior chemopreventive and chemotherapeutic properties against hepatocellular carcinomas, mitochondria-targeted hydroxycinnamic acids (MitoHCAs) were synthesized by conjugation with a triphenylphosphonium cation. These synthetic compounds were evaluated for their antioxidant activities in hepatic mitochondria, including against OH(∙-) and ROO(∙-) induced lipid peroxidation. H2O2 production was decreased significantly by increasing glutathione peroxidase and catalase activities...
January 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28119814/structure-of-the-40s-ribosomal-subunit-of-plasmodium-falciparum-by-homology-and-de-novo-modeling
#2
Harrison Ndung'u Mwangi, Peter Wagacha, Peterson Mathenge, Fredrick Sijenyi, Francis Mulaa
Generation of three dimensional structures of macromolecules using in silico structural modeling technologies such as homology and de novo modeling has improved dramatically and increased the speed by which tertiary structures of organisms can be generated. This is especially the case if a homologous crystal structure is already available. High-resolution structures can be rapidly created using only their sequence information as input, a process that has the potential to increase the speed of scientific discovery...
January 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28119813/c0818-a-novel-curcumin-derivative-interacts-with-hsp90-and-inhibits-hsp90-atpase-activity
#3
Yingjuan Fan, Yang Liu, Lianru Zhang, Fang Cai, Liping Zhu, Jianhua Xu
The aims of the present study were to estimate the affinity between 3,5-(E)-bis(3-methoxy-4-hydroxybenzal)-4-piperidinone hydrochloride (C0818) and heat shock protein 90 (Hsp90) and to investigate the inhibitory effects of this compound on Hsp90 ATPase activity. Fluorescence spectroscopy was used to examine the affinity between varying concentrations of C0818 and Hsp90, N-Hsp90, M-Hsp90 and C-Hsp90. Fluorescence intensities were recorded in the range of 290-510 nm at 293, 303 and 310 K, respectively. A colorimetric assay for inorganic phosphate (based on the formation of a phosphomolybdate complex and the subsequent reaction with malachite green) were used to examine the inhibitory effects of C0818 on Hsp90 ATPase activity...
January 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28119812/inhalable-oridonin-loaded-poly-lactic-co-glycolic-acid-large-porous-microparticles-for-in-situ-treatment-of-primary-non-small-cell-lung-cancer
#4
Lifei Zhu, Miao Li, Xiaoyan Liu, Lina Du, Yiguang Jin
Non-small cell lung cancer (NSCLC) accounts for about 85% of all lung cancers. Traditional chemotherapy for this disease leads to serious side effects. Here we prepared an inhalable oridonin-loaded poly(lactic-co-glycolic)acid (PLGA) large porous microparticle (LPMP) for in situ treatment of NSCLC with the emulsion/solvent evaporation/freeze-drying method. The LPMPs were smooth spheres with many internal pores. Despite a geometric diameter of ~10 µm, the aerodynamic diameter of the spheres was only 2.72 µm, leading to highly efficient lung deposition...
January 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28119811/2-3-diaryl-3h-imidazo-4-5-b-pyridine-derivatives-as-potential-anticancer-and-anti-inflammatory-agents
#5
Erin Marie Kirwen, Tarun Batra, Chandrabose Karthikeyan, Girdhar Singh Deora, Vandana Rathore, Chaitanya Mulakayala, Naveen Mulakayala, Amy Catherine Nusbaum, Joel Chen, Haneen Amawi, Kyle McIntosh, Sahabjada, Neelam Shivnath, Deepak Chowarsia, Nisha Sharma, Md Arshad, Piyush Trivedi, Amit K Tiwari
In this study we examined the suitability of the 3H-imidazo[4,5-b]pyridine ring system in developing novel anticancer and anti-inflammatory agents incorporating a diaryl pharmacophore. Eight 2,3-diaryl-3H-imidazo[4,5-b]pyridine derivatives retrieved from our in-house database were evaluated for their cytotoxic activity against nine cancer cell lines. The results indicated that the compounds showed moderate cytotoxic activity against MCF-7, MDA-MB-468, K562 and SaOS2 cells, with K562 being the most sensitive among the four cancer cell lines...
January 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28119810/asiatic-acid-inhibits-lung-cancer-cell-growth-in-vitro-and-in-vivo-by-destroying-mitochondria
#6
Tiancong Wu, Ji Geng, Wenjie Guo, Jing Gao, Xixu Zhu
Asiatic acid (AA), a pentacyclic triterpene found in Centella asiatica, displays significant anti-proliferative effects on cancer cells in vitro although the underlying mechanism of this effect remains unknown. This study investigated the efficacy and mechanism of action of AA against lung cancer both in vivo and in vitro. Using the MTT assay, AA was found to induce apoptosis in a dose- and time-dependent manner, an effect enhanced by pretreatment with an autophagy inhibitor. It also elevated expression of microtubule-associated protein 1 light chain 3 (LC3) and decreased the expression of p62...
January 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28119809/euphorbia-factor-l2-induces-apoptosis-in-a549-cells-through-the-mitochondrial-pathway
#7
Minting Lin, Sili Tang, Chao Zhang, Hubiao Chen, Wenjing Huang, Yun Liu, Jianye Zhang
Euphorbia factor L2, a lathyrane diterpenoid isolated from caper euphorbia seed (the seeds of Euphorbia lathyris L.), has been traditionally applied to treat cancer. This article focuses on the cytotoxic activity of Euphorbia factor L2 against lung carcinoma A549 cells and the mechanism by which apoptosis is induced. We analyzed the cytotoxicity and related mechanism of Euphorbia factor L2 with an MTT assay, an annexin V-FITC/PI test, a colorimetric assay, and immunoblotting. Euphorbia factor L2 showed potent cytotoxicity to A549 cells...
January 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28119808/lx2-32c-a-novel-semi-synthetic-taxane-exerts-antitumor-activity-against-prostate-cancer-cells-in-vitro-and-in-vivo
#8
Guangyao Lv, Dengjun Sun, Jingwen Zhang, Xiaoxia Xie, Xiaoqiong Wu, Weishuo Fang, Jingwei Tian, Chunhong Yan, Hongbo Wang, Fenghua Fu
Tubulin has been shown to be an effective target for the development of cytotoxic agents against prostate cancer. Previously, we reported that Lx2-32c is an anti-tubulin agent with high binding affinity to tubulin. In this study, we investigated the potential of Lx2-32c to act as an effective cytotoxic agent in the treatment of prostate cancer. MTT assays showed that Lx2-32c was cytotoxic to all tested prostate cancer cell lines. The Lx2-32c-treated cells typically exhibited a rounded morphology associated with the onset of apoptosis, as evidenced by immunocytochemical staining...
January 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28119807/regulation-of-multidrug-resistance-by-micrornas-in-anti-cancer-therapy
#9
REVIEW
Xin An, Cesar Sarmiento, Tao Tan, Hua Zhu
Multidrug resistance (MDR) remains a major clinical obstacle to successful cancer treatment. Although diverse mechanisms of MDR have been well elucidated, such as dysregulation of drugs transporters, defects of apoptosis and autophagy machinery, alterations of drug metabolism and drug targets, disrupti on of redox homeostasis, the exact mechanisms of MDR in a specific cancer patient and the cross-talk among these different mechanisms and how they are regulated are poorly understood. MicroRNAs (miRNAs) are a new class of small noncoding RNAs that could control the global activity of the cell by post-transcriptionally regulating a large variety of target genes and proteins expression...
January 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28119806/class-i-phosphatidylinositol-3-kinase-inhibitors-for-cancer-therapy
#10
REVIEW
Wennan Zhao, Yuling Qiu, Dexin Kong
The phosphatidylinositol 3-kinase (PI3K) pathway is frequently activated in human cancers. Class I PI3Ks are lipid kinases that phosphorylate phosphatidylinositol 4,5-bisphosphate (PIP2) at the 3-OH of the inositol ring to generate phosphatidylinositol 3,4,5-trisphosphate (PIP3), which in turn activates Akt and the downstream effectors like mammalian target of rapamycin (mTOR) to play key roles in carcinogenesis. Therefore, PI3K has become an important anticancer drug target, and currently there is very high interest in the pharmaceutical development of PI3K inhibitors...
January 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28119805/how-to-unleash-mitochondrial-apoptotic-blockades-to-kill-cancers
#11
REVIEW
Jing Deng
Apoptosis, especially the intrinsic mitochondrial cell death pathway, is regulated by the BCL-2 family of proteins. Defects in apoptotic machinery are one of the main mechanisms that cells employ to evade cell death and become cancerous. Targeting the apoptotic defects, either by direct inhibition of BCL-2 family proteins or through modulation of regulatory pathways, can restore cell sensitivity to cell death. This review will focus on the aspects of BCL-2 family proteins, their interactions with kinase pathways, and how novel targeted agents can help overcome the apoptotic blockades...
January 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28119804/targeting-calcium-signaling-in-cancer-therapy
#12
REVIEW
Chaochu Cui, Robert Merritt, Liwu Fu, Zui Pan
The intracellular calcium ions (Ca(2+)) act as second messenger to regulate gene transcription, cell proliferation, migration and death. Accumulating evidences have demonstrated that intracellular Ca(2+) homeostasis is altered in cancer cells and the alteration is involved in tumor initiation, angiogenesis, progression and metastasis. Targeting derailed Ca(2+) signaling for cancer therapy has become an emerging research area. This review summarizes some important Ca(2+) channels, transporters and Ca(2+)-ATPases, which have been reported to be altered in human cancer patients...
January 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28119803/editorial-for-targets-and-anticancer-drug-research
#13
EDITORIAL
(no author information available yet)
No abstract text is available yet for this article.
January 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28119802/editor-profile-guest-editor-of-special-issue-on-targets-and-anticancer-drug-research
#14
EDITORIAL
Liwu Fu
No abstract text is available yet for this article.
January 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/27818930/effect-of-isopropyl-myristate-on-the-viscoelasticity-and-drug-release-of-a-drug-in-adhesive-transdermal-patch-containing-blonanserineffect-of-isopropyl-myristate-on-the-viscoelasticity-and-drug-release-of-a-drug-in-adhesive-transdermal-patch-containing-blonanserinretain
#15
Chunyi Zhao, Peng Quan, Chao Liu, Qiaoyun Li, Liang Fang
The purpose of this study was to investigate the effect of isopropyl myristate (IPM), a penetration enhancer, on the viscoelasticity and drug release of a drug-in-adhesive transdermal patch containing blonanserin. The patches were prepared with DURO-TAK(®) 87-2287 as a pressure-sensitive adhesive (PSA) containing 5% (w/w) of blonanserin and different concentrations of IPM. An in vitro release experiment was performed and the adhesive performance of the drug-in-adhesive patches with different concentrations of IPM was evaluated by a rolling ball tack test and a shear-adhesion test...
November 2016: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/27818929/cloning-and-expression-of-sgcyp450-4-from-siraitia-grosvenorii
#16
Dongping Tu, Xiaojun Ma, Huan Zhao, Changming Mo, Qi Tang, Liuping Wang, Jie Huang, Limei Pan
CYP450 plays an essential role in the development and growth of the fruits of Siraitia grosvenorii. However, little is known about the SgCYP450-4 gene in S. grosvenorii. Here, based on transcriptome data, a full-length cDNA sequence of SgCYP450-4 was cloned by reverse transcriptase-polymerase chain reaction (RT-PCR) and rapid-amplification of cDNA ends (RACE) strategies. SgCYP450-4 is 1677 bp in length (GenBank accession No. AEM42985.1) and contains a complete open reading frame (ORF) of 1422 bp. The deduced protein was composed of 473 amino acids, the molecular weight is 54...
November 2016: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/27818928/effect-of-hydrogen-bond-formation-replacement-on-solubility-characteristics-gastric-permeation-and-pharmacokinetics-of-curcumin-by-application-of-powder-solution-technology
#17
Vijay Sharma, Kamla Pathak
The present research aimed to improve the dissolution rate and bioavailability of curcumin using the potential of liquisolid technology. Twelve drug-loaded liquisolid systems (LS-1 to LS-12) were prepared using different vehicles (PEG 200, PEG 400 and Tween 80) and curcumin concentrations in vehicle (40%, 50%, 60% and 70%, w/w). The carrier [microcrystalline cellulose (MCC) PH102] to coat (Aerosil(®)) ratio was 20 in all formulations. The systems were screened for pre-compression properties before being compressed to liquisolid tablets (LT-1 to LT-12)...
November 2016: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/27818927/simultaneous-quantification-of-ginsenoside-rg1-and-its-metabolites-by-hplc-ms-ms-rg1-excretion-in-rat-bile-urine-and-feces
#18
Chiyu He, Ru Feng, Yupeng Sun, Shifeng Chu, Ji Chen, Chao Ma, Jie Fu, Zhenxiong Zhao, Min Huang, Jiawen Shou, Xiaoyang Li, Yuzhu Wang, Jinfeng Hu, Yan Wang, Juntian Zhang
Ginsenoside Rg1 (Rg1), the major effective component of ginseng, has been shown to have multiple bioactivities, but low oral bioavailability. The aim of this study was to develop a simple, sensitive and rapid high performance liquid chromatography-tandem mass spectrometry (LC-MS/MS) method, which could be used to validate and quantify the concentrations of Rg1 and its metabolites in Sprague-Dawley rat bile, urine, and feces after oral administration (25 mg/kg). Calibration curves offered satisfactory linearity (r>0...
November 2016: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/27818926/pharmacokinetic-evaluation-of-shenfu-injection-in-beagle-dogs-after-intravenous-drip-administration
#19
Yuqiao Zhang, Dali Tian, Yuyou Huang, Ling Li, Juan Mao, Juan Tian, Jinsong Ding
Shenfu Injection (SFI) is a well-defined Chinese herbal formulation that is obtained from red ginseng and processed aconite root. The main active constituents in SFI are ginsenosides and aconitum alkaloids. In this work, ginsenosides (ginsenoside Rg1, ginsenoside Rb1 and ginsenoside Rc) and aconitum alkaloids (benzoylmesaconine and fuziline) were used as the index components to explore the pharmacokinetic behavior of SFI. A selective and sensitive HPLC-MS/MS method was developed for the quantification of ginsenosides and aconitum alkaloids in dog plasma and was used to characterize the pharmacokinetics of the five index components after intravenous drip of three different dosages of SFI in beagle dogs...
November 2016: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/27818925/pharmacokinetics-of-h002-a-novel-s1pr1-modulator-and-its-metabolites-in-rat-blood-using-liquid-chromatography-tandem-mass-spectrometry
#20
Jiaqi Mi, Manman Zhao, Shu Yang, Shuang Yang, Jing Jin, Xiaojian Wang, Qiong Xiao, Jinping Hu, Yan Li
A rapid and sensitive liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed and validated for the simultaneous determination of H002 and its phosphorylated metabolite, H002-P and hydroxylated metabolite H002-M, in rat blood. H001, an analogue of H002, was used as the internal standard. Blood samples were prepared by simple protein precipitation. The analytes and internal standard were separated on a Zorbax SB-C18 column with a gradient mobile phase consisting of methanol and water containing 0...
November 2016: Acta Pharmaceutica Sinica. B
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