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Archives of Pharmacal Research

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https://www.readbyqxmd.com/read/29998374/synthesis-and-structure-activity-relationship-of-n-piperidin-4-yl-benzamide-derivatives-as-activators-of-hypoxia-inducible-factor-1-pathways
#1
Zhi-Ning Huang, Han Liang, Hong Qiao, Bao-Rui Wang, Ning Qu, Hua Li, Run-Run Zhou, Li-Juan Wang, Shan-Hua Li, Fu-Nan Li
Guided by bioisosterism and pharmacokinetic parameters, we designed and synthesized a series of novel benzamide derivatives. Preliminary in vitro studies indicated that compounds 10b and 10j show significant inhibitory bioactivity in HepG2 cells (IC50 values of 0.12 and 0.13 μM, respectively). Compounds 10b and 10j induced the expression of HIF-1α protein and downstream target gene p21, and upregulated the expression of cleaved caspase-3 to promote tumor cells apoptosis.
July 11, 2018: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29992400/autophagy-plays-a-protective-role-against-apoptosis-induced-by-toxicarioside-n-via-the-akt-mtor-pathway-in-human-gastric-cancer-sgc-7901-cells
#2
Huan-Ge Zhao, Song-Lin Zhou, Ying-Ying Lin, Hua Wang, Hao-Fu Dai, Feng-Ying Huang
Toxicarioside N (Tox N), a natural product extract from Antiaris toxicaria, has been reported to induce apoptosis in human gastric cancer cells. However, the mechanism and actual role of autophagy in Tox N-induced apoptosis of human gastric cancer cells remains poorly understood. In the current study, we demonstrated that Tox N could induce autophagy by inhibiting the Akt/mTOR signaling pathway in SGC-7901 cells. Moreover, we found that the inhibition of autophagy by 3-methyladenine, an autophagy inhibitor, enhanced Tox N-induced apoptotic cell death...
July 10, 2018: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29978428/lifespan-extending-property-of-6-shogaol-from-zingiber-officinale-roscoe-in-caenorhabditis-elegans
#3
Eun Byeol Lee, Jun Hyeong Kim, Yeong Jee Kim, Yun Jeong Noh, Su Jin Kim, In Hyun Hwang, Dae Keun Kim
Aging is a key risk factor for many diseases, understanding the mechanism of which is becoming more important for drug development given the fast-growing aging population. In the course of our continued efforts to discover anti-aging natural products, the active constituent 6-shogaol was isolated from Zingiber officinale Roscoe. The chemical structure of 6-shogaol was identified by comparison of its NMR data with literature values. The lifespan-extending effect of 6-shogaol was observed in a dose-dependent manner in Caenorhabditis elegans that has been widely used as a model organism for human aging studies...
July 6, 2018: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29978427/role-of-silibinin-in-the-management-of-diabetes-mellitus-and-its-complications
#4
REVIEW
Chun Chu, Dahong Li, Shicheng Zhang, Takashi Ikejima, Ying Jia, Dongkai Wang, Fanxing Xu
Diabetes mellitus is globally approaching epidemic proportions and acts as a major cause of a number of serious health problems diagnosed as diabetic complications. The current oral drugs in the treatment of diabetes and its complications could meet some but not all of the patients' needs, and the development of novel drugs with a hypoglycemic effect is urgently required. Silibinin, a flavonolignan traditionally used for the treatment of gallbladder and hepatic diseases, was reported to improve glycemic homeostasis by improving the activity of pancreatic β-cells, increasing insulin sensitivity of liver and muscle cells, and decreasing lipid deposition in adipocytes...
July 6, 2018: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29974342/in-vivo-genome-editing-targeted-towards-the-female-reproductive-system
#5
REVIEW
Masahiro Sato, Masato Ohtsuka, Shingo Nakamura, Takayuki Sakurai, Satoshi Watanabe, Channabasavaiah B Gurumurthy
The discovery of sequence specific nucleases such as ZFNs, TALENs, and CRISPR/Cas9 has revolutionized genome editing. The CRISPR/Cas9 system has particularly emerged as a highly simple and efficient approach towards generating genome-edited animal models of most of the experimental species. The limitation of these novel genome editing tools is that, till date, they depend on traditional pronuclear injection (PI)-based transgenic technologies developed over the last three decades. PI requires expensive micromanipulator systems and the equipment operators must possess a high level of skill...
July 4, 2018: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29961196/crosstalk-between-cancer-cells-and-endothelial-cells-implications-for-tumor-progression-and-intervention
#6
REVIEW
Hyojeong Choi, Aree Moon
Communication between tumor cells and stromal cells is crucial to tumor development and progression. Fibroblasts and macrophages are the most common stromal cells in the tumor microenvironment. Endothelial cells are another type of stromal cell in the tumor microenvironment required for angiogenesis via interaction with tumor cells. Tumor angiogenesis provides not only oxygen and nutrients for tumor cells but also the necessary anchorage to facilitate tumor metastasis. The present review summarizes studies on the crosstalk between cancer cells and endothelial cells with a focus on implications for tumor progression...
June 30, 2018: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29961195/anti-inflammatory-activity-of-compounds-from-the-rhizome-of-cnidium-officinale
#7
Huynh Nguyen Khanh Tran, Thao Quyen Cao, Jeong Ah Kim, Ui Joung Youn, Sanghee Kim, Mi Hee Woo, Byung Sun Min
Five new compounds, 9,3'-dimethoxyhierochin A (1), 6-oxo-trans-neocnidilide (2), (±)-(3E)-trans-6-hydroxy-7-methoxydihydroligustilide (3), (±)-cnidiumin (4), and 6-(1-oxopentyl)-salicylic acid methyl ester (5), together with twenty known compounds (6-25), were isolated from the rhizome of Cnidium officinale. The chemical structures of new compounds were established by NMR spectroscopic techniques, mass spectrometry, Mosher's method, and CD spectrum. Their anti-inflammatory activities were evaluated against lipopolysaccharide (LPS)-induced nitric oxide (NO) production in macrophage RAW 264...
June 30, 2018: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29961194/preparation-characterization-and-pharmacokinetics-of-liposomal-docetaxel-for-oral-administration
#8
Jung Ha Kim, Dae Hwan Shin, Jin-Seok Kim
A docetaxel (DTX) liposomal formulation composed of egg phosphatidylcholine, sodium deoxycholate, and stearylamine was developed. Eudragit (0.5%) was coated to deliver the drug to the region between the distal small intestine and the colon. Lyophilized trehalose and mannitol were used as cryoprotectants because they preserve the particle integrity and good appearance. In vitro release studies showed that the amount of drug released from the coated liposomes was low in solution 1, which simulated the pH condition of the stomach...
June 30, 2018: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29922878/aspirin-inspired-acetyl-donating-hdacs-inhibitors
#9
Jiah Lim, Yoojin Song, Jung-Hee Jang, Chul-Ho Jeong, Sooyeun Lee, Byoungduck Park, Young Ho Seo
Aspirin is one of the oldest drugs for the treatment of inflammation, fever, and pain. It is reported to covalently modify COX-2 enzyme by acetylating a serine amino acid residue. By virtue of aspirin's acetylating potential, we for the first time developed novel acetyl-donating HDAC inhibitors. In this study, we report the design, synthesis, in silico docking study, and biological evaluation of acetyl-donating HDAC inhibitors. The exposure of MDA-MB-231 cells with compound 4c significantly promotes the acetylation of α-tubulin and histone H3, which are substrates of HDAC6 and HDAC1, respectively...
June 20, 2018: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29948772/effect-of-thiazolidinedione-phenylacetate-derivatives-on-wound-healing-activity
#10
So Hee Park, Dubok Choi, Hoon Cho
The aim of this work was to evaluate the synthesis and structure-activity relationship of 4-((2,4-dioxothiazolidin-5-ylidene)methyl)phenyl 2-phenylacetate derivatives as potential wound-healing agents. The IC50 values of the lead compounds ranged from 0.01 to 0.05 µM. These compounds also increased the levels of extracellular prostaglandin E2 (PGE2 ) in A549 cells. Among the synthesized compounds, compounds 66, 67, 69, and 86 increased PGE2 levels 3- to 4-fold of those achieved with the negative control. Introduction of a halogen at the intermediate phenyl ring, compounds 66, 67, 69, and 86 resulted in higher IC50 values, which indicated lower cytotoxicity than that observed upon the introduction of other substituents at the same position...
June 8, 2018: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29948771/two-new-naphthalenic-lactone-glycosides-from-cassia-obtusifolia-l-seeds
#11
Srijan Shrestha, Pradeep Paudel, Su Hui Seong, Byung Sun Min, Eun Kyoung Seo, Hyun Ah Jung, Jae Sue Choi
Two new naphthalenic lactone glycosides, (3S)-9,10-dihydroxy-7-methoxy-3-methyl-1-oxo-3,4-dihydro-1H-benzo[g]isochromene-3-carboxylic acid 9-O-β-D-glucopyranoside (1) and (3R)-cassialactone 9-O-β-D-glucopyranoside (2) were isolated from seeds of Cassia obtusifolia Linn., along with five known compounds: (3R)-cassialactone 9-O-β-D-gentiobioside (3), emodin 1-O-β-gentiobioside (4), 1-hydroxyl-2-acetyl-3,8-dimethoxy-naphthalene 6-O-β-D-apiofuranosyl-(1 → 2)-β-D-glucopyranoside (5), rubrofusarin 6-O-β-D-gentiobioside (6), rubrofusarin 6-O-β-D-triglucoside (7)...
June 8, 2018: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29948770/effect-of-rufinamide-on-the-kainic-acid-induced-excitotoxic-neuronal-death-in-the-mouse-hippocampus
#12
Jin-A Park, Choong-Hyun Lee
Rufinamide (RUF) is a structurally unique anti-epileptic drug, used in the treatment of seizure disorders such as Lennox-Gastaut syndrome. In the present study, we investigated whether RUF protected against excitotoxic neuronal damage in the mouse hippocampal CA3 region after intraperitoneal kainic acid (KA) injection. Treatment with 25, 50 and 100 mg/kg RUF significantly decreased the KA-induced neuronal death in the hippocampal CA3 region in a dose-dependent manner. In addition, 100 mg/kg RUF treatment reduced the KA-induced oxidative stress-related increase of MDA level and decrease of total SOD activity in the hippocampus...
June 8, 2018: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29858981/drug-induced-hyperglycaemia-and-diabetes-pharmacogenomics-perspectives
#13
REVIEW
Mou-Ze Liu, Hai-Yan He, Jian-Quan Luo, Fa-Zhong He, Zhang-Ren Chen, Yi-Ping Liu, Da-Xiong Xiang, Hong-Hao Zhou, Wei Zhang
Drug-induced diabetes is widely reported in clinical conditions, and it is becoming a global issue because of its potential to increase the risk of severe cardiovascular complications. However, which drug mechanisms exert their diabetogenic effects and why the effects present significant inter-individual differences remain largely unknown. Pharmacogenomics, which is the study of how genomic variation influences drug responses, provides an explanation for individual differences in drug-induced diabetes. We highlight that pharmacogenomics can be involved in regulating the expression of genes in signaling pathways related to the pharmacokinetics or pharmacodynamics of drugs or the pathogenesis of diabetes, contributing to the differences in drug-induced glucose impairment...
June 1, 2018: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29855892/efficient-genome-editing-by-facs-enrichment-of-paired-d10a-cas9-nickases-coupled-with-fluorescent-proteins
#14
Ramu Gopalappa, Myungjae Song, Arun Pandian Chandrasekaran, Soumyadip Das, Saba Haq, Hyun Chul Koh, Suresh Ramakrishna
Targeted genome editing by clustered regularly interspaced short palindromic repeats (CRISPR-Cas9) raised concerns over off-target effects. The use of double-nicking strategy using paired Cas9 nickase has been developed to minimize off-target effects. However, it was reported that the efficiency of paired nickases were comparable or lower than that of either corresponding nuclease alone. Recently, we conducted a systematic comparison of the efficiencies of several paired Cas9 with their corresponding Cas9 nucleases and showed that paired D10A Cas9 nickases are sometimes more efficient than individual nucleases for gene disruption...
May 31, 2018: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29777358/generation-of-genetically-engineered-animals-using-engineered-endonucleases
#15
REVIEW
Jong Geol Lee, Young Hoon Sung, In-Jeoung Baek
The key to successful drug discovery and development is to find the most suitable animal model of human diseases for the preclinical studies. The recent emergence of engineered endonucleases is allowing for efficient and precise genome editing, which can be used to develop potentially useful animal models for human diseases. In particular, zinc finger nucleases, transcription activator-like effector nucleases, and the clustered regularly interspaced short palindromic repeat systems are revolutionizing the generation of diverse genetically-engineered experimental animals including mice, rats, rabbits, dogs, pigs, and even non-human primates that are commonly used for preclinical studies of the drug discovery...
May 17, 2018: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29804279/pro-apoptotic-peptides-based-cancer-therapies-challenges-and-strategies-to-enhance-therapeutic-efficacy
#16
REVIEW
Kyoung Ah Min, Pooja Maharjan, Songhee Ham, Meong Cheol Shin
Cancer is a leading cause of death worldwide. Despite many advances in the field of cancer therapy, an effective cure is yet to be found. As a more potent alternative for the conventional small molecule anti-cancer drugs, pro-apoptotic peptides have emerged as a new class of anticancer agents. By interaction with certain members in the apoptotic pathways, they could effectively kill tumor cells. However, there remain bottleneck challenges for clinical application of these pro-apoptotic peptides in cancer therapy...
June 2018: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29804278/anthraquinone-and-naphthopyrone-glycosides-from-cassia-obtusifolia-seeds-mediate-hepatoprotection-via-nrf2-mediated-ho-1-activation-and-mapk-modulation
#17
Pradeep Paudel, Hyun Ah Jung, Jae Sue Choi
Cassia obtusifolia L. seed is one of the most popular traditional Chinese medicine for mutagenicity, genotoxicity, hepatotoxicity, and acute inflammatory diseases. We evaluated the hepatoprotective activity of anthraquinone and naphthopyrone glycosides isolated from the butanol fraction of C. obtusifolia seeds and explored their effects on cell signaling pathways. Continuous chromatographic separation led to the isolation of 1-desmethylaurantio-obtusin 2-O-β-D-glucopyranoside (1), rubrofusarin 6-O-β-D-apiofuranosyl-(1 → 6)-O-β-D-glucopyranoside (2) and rubrofusarin 6-O-β-gentiobioside (3)...
June 2018: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29777359/regulatory-mechanisms-of-thiol-based-redox-sensors-lessons-learned-from-structural-studies-on-prokaryotic-redox-sensors
#18
REVIEW
Sang Jae Lee, Dong-Gyun Kim, Kyu-Yeon Lee, Ji Sung Koo, Bong-Jin Lee
Oxidative stresses, such as reactive oxygen species, reactive electrophilic species, reactive nitrogen species, and reactive chlorine species, can damage cellular components, leading to cellular malfunction and death. In response to oxidative stress, bacteria have evolved redox-responsive sensors that enable them to simultaneously monitor and eradicate potential oxidative stress. Specifically, redox-sensing transcription regulators react to oxidative stress by means of modifying the thiol groups of cysteine residues, functioning as part of an efficient survival mechanism for many bacteria...
June 2018: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29797242/estrogenic-effects-of-phytoestrogens-derived-from-flemingia-strobilifera-in-mcf-7-cells-and-immature-rats
#19
Si-Yeon Jeong, Minsun Chang, Sang-Ho Choi, Sei-Ryang Oh, Hong-Hua Wu, Yan Zhu, Xiu-Mei Gao, Xiaoying Wang, Baojin Zhang, Da-Sol Lim, Joon Young Lee, So-Dam Kim, Yun Seon Song
Phytoestrogen (PE) has received considerable attention due to the physiological significance of its estrogenicity. Flemingia strobilifera (FS) has been used as a folk medicine in Asia for the treatment of inflammation, cancer, and infection; however, the estrogenic effects and chemical components of FS have not yet been reported. We aimed to uncover the estrogenic properties and PEs derived from FS using phytochemical and pharmacological evaluation. PEs from FS extract (FSE) were analyzed by NMR, HPLC, and MS...
May 2018: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29732490/chemical-constituents-from-sanguisorba-officinalis-l-and-their-inhibitory-effects-on-lps-stimulated-pro-inflammatory-cytokine-production-in-bone-marrow-derived-dendritic-cells
#20
Xiang Dong Su, Irshad Ali, Madeeha Arooj, Young Sang Koh, Seo Young Yang, Young Ho Kim
Sanguisorba officinalis L. (Rosaceae) is a perennial herbaceous plant and its roots have been used as an important astringent medicine in Eastern Asian countries over many thousand years. In this phytochemical research, 23 compounds (1-23) were isolated from the roots of S. officinalis. Their chemical structures were identified by extensive spectroscopic methods, including 1D and 2D NMR experiments. The anti-inflammatory effects of extracts and isolated compounds were investigated by measuring the production of pro-inflammatory cytokine IL-12 p40, IL-6 and TNF-α in LPS-stimulated bone marrow-derived dendritic cell...
May 2018: Archives of Pharmacal Research
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