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Archives of Pharmacal Research

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https://www.readbyqxmd.com/read/29043603/epigenetic-modifications-of-gene-expression-by-lifestyle-and-environment
#1
REVIEW
Qudeer Ahmed Abdul, Byung Pal Yu, Hae Young Chung, Hyun Ah Jung, Jae Sue Choi
Epigenetics oftenly described as the heritable changes in gene expression independent of changes in DNA sequence. Various environmental factors such as nutrition-dietary components, lifestyle, exercise, physical activity, toxins, and other contributing factors remodel the genome either in a constructive or detrimental way. Since epigenetic changes are reversible and nutrition is one of the many epigenetic regulators that modify gene expression without changing the DNA sequence, dietary nutrients and bioactive food components contribute to epigenetic phenomena either by directly suppressing DNA methylation or histone catalyzing enzymes or by changing the availability of substrates required for enzymatic reactions...
October 17, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29043602/fluorinated-pyrrole-incorporated-2-thiazolyl-hydrazone-motifs-a-new-class-of-antimicrobial-and-anti-tuberculosis-agents
#2
P V Sowmya, Boja Poojary, Vasantha Kumar, U Vishwanatha, Premalatha Shetty
In aim of obtaining novel bio-active compounds, a new series of fluorinated 1-(4-(aryl)thiazol-2-yl)-2-((1-(aryl)-2,5-dimethyl-1H-pyrrol-3-yl)methylene)hydrazines (5a-t) and 1-(4-(4-aryl)thiazol-2-yl)-2-((3-(2,4-dichlorophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)hydrazines (8a-d) were synthesized and screened for their antibacterial and antifungal activities. The potent compounds were further screened in vitro for anti-tuberculosis activity against Mycobacterium tuberculosis H37Rv strain. Compounds 5a, 5c-5h and 5m were found to be good inhibitors of B...
October 17, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29032487/pathological-and-therapeutic-roles-of-innate-lymphoid-cells-in-diverse-diseases
#3
REVIEW
Jisu Kim, Geon Kim, Hyeyoung Min
Innate lymphoid cells (ILCs) are a recently defined type of innate-immunity cells that belong to the lymphoid lineage and have lymphoid morphology but do not express an antigen-specific B cell or T-cell receptor. ILCs regulate immune functions prior to the formation of adaptive immunity and exert effector functions through a cytokine release. ILCs have been classified into three groups according to the transcription factors that regulate their development and function and the effector cytokines they produce...
October 14, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29027637/vaccine-adjuvants-smart-components-to-boost-the-immune-system
#4
REVIEW
Rakesh Bastola, Gyubin Noh, Taekwang Keum, Santosh Bashyal, Jo-Eun Seo, Jaewoong Choi, Yeonsu Oh, YoungSik Cho, Sangkil Lee
Vaccination is an effective approach to prevent the consequences of infectious diseases. Vaccines strengthen immunity and make individuals resistant to infections with pathogens. Although conventional vaccines are highly immunogenic, they are associated with some safety issues. Subunit vaccines are safe, but they require adjuvants to stimulate the immune system because of their weaker immunogenicity. Adjuvants are entities incorporated into vaccines to increase the immunogenic responses of antigens. They play a crucial role in increasing the potency and efficacy of vaccines...
October 13, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29027136/oligonol-promotes-glucose-uptake-by-modulating-the-insulin-signaling-pathway-in-insulin-resistant-hepg2-cells-via-inhibiting-protein-tyrosine-phosphatase-1b
#5
Himanshu Kumar Bhakta, Pradeep Paudel, Hajime Fujii, Atsuya Sato, Chan Hum Park, Takako Yokozawa, Hyun Ah Jung, Jae Sue Choi
Insulin resistance and protein tyrosine phosphatase 1B (PTP1B) overexpression are strongly associated with type 2 diabetes mellitus (T2DM), which is characterized by defects in insulin signaling and glucose intolerance. In a previous study, we demonstrated oligonol inhibits PTP1B and α-glucosidase related to T2DM. In this study, we examined the molecular mechanisms underlying the anti-diabetic effects of oligonol in insulin-resistant HepG2 cells. Glucose uptake was assessed using a fluorescent glucose tracer, 2-[N-(7-nitrobenz-2-oxa-1,3-diazol-4-yl)amino]-2-deoxyglucose, and the signaling pathway was investigated by western blotting...
October 12, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29027133/combination-of-a-chemopreventive-agent-and-paclitaxel-in-cd44-targeted-hybrid-nanoparticles-for-breast-cancer-treatment
#6
Bao Ngoc Tran, Hanh Thuy Nguyen, Jong Oh Kim, Chul Soon Yong, Chien Ngoc Nguyen
The CD44 receptor, which is upregulated in many cancer cells, provides a selective cellular surface for targeted drug delivery systems. We developed a hybrid nanocarrier for the CD44-targeted delivery of ibuprofen (IBU) and paclitaxel (PTX). The solid lipid nanoparticles (SLNs) were prepared by a hot-melt oil/water emulsion technique and then coated with hyaluronic acid (HA) by electrostatic interactions. The final SLN were spherical with a hydrodynamic diameter (Z) of 72.16 ± 2.9 nm, polydispersity index (PDI) of 0...
October 12, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29027119/mollugin-enhances-the-osteogenic-action-of-bmp-2-via-the-p38-smad-signaling-pathway
#7
Seong-Hee Moon, Ikyon Kim, Seong Hwan Kim
Bone morphogenetic protein 2 (BMP-2) has been used clinically to encourage bone regeneration; although, there can be major side effects with larger doses. Therefore, there is a need to identify new small molecules to potentiate the osteogenic action of BMP-2. In this study, we investigated the effect of mollugin on bone formation in murine bi-potential mesenchymal progenitor C2C12 cells by combination with BMP-2. We found mollugin could enhance the BMP-2-mediated osteoblast differentiation of C2C12 cells. This was accompanied by the induction of other osteogenic BMPs...
October 12, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29022192/a-positive-circuit-of-vegf-increases-glut-1-expression-by-increasing-hif-1%C3%AE-gene-expression-in-human-retinal-endothelial-cells
#8
Yoon Kyung Choi
Treatment of human retinal microvascular endothelial cells (HRMECs) with vascular endothelial growth factor 165 (VEGF165) increased hypoxia-inducible factor 1α (HIF-1α), VEGF, and glucose transporter 1 (Glut-1) mRNA expression and Glut-1 protein localization to the membrane. In contrast, treatment of human retinal pigment epithelium cells with VEGF165 did not induce HIF-1α, VEGF, and Glut-1 gene expression. Microvascular endothelial cells are surrounded by astrocytic end feet in the retina. Astrocyte-derived A-kinase anchor protein 12 overexpression during hypoxia downregulated VEGF secretion, and this conditioned medium reduced VEGF and Glut-1 expression in HRMECs, suggesting that communications between astrocytes and endothelial cells may be the determinants of the blood vessel network...
October 11, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29019022/distribution-of-lacosamide-in-the-rat-brain-assessed-by-in-vitro-slice-technique
#9
Zsolt Gáll, Szende Vancea
Lacosamide is a newer anticonvulsant and is the only one that enhances the slow inactivation of voltage gated sodium channels. It is also claimed to have disease-modifying potential, but its pharmacokinetic properties have been much less discussed in the literature. In rats, lacosamide shows restricted distribution to tissues, and the brain-to-plasma partition coefficient (Kp) is only 0.553. In this study, the brain disposition of lacosamide was evaluated in rat brains, and its neuropharmacokinetic parameters (i...
October 10, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28965327/standardization-of-extract-mixture-of-chaenomeles-sinensis-and-phyllostachys-bambusoides-for-anti-obesity-by-hplc-uv
#10
Yan Zhao, Hong Xu Li, Young Ho Kim, Cheong-Weon Cho, Sung Yeoun Hwang, Hyun-A Oh, Kyung Tae Kim, Jong Seong Kang
JM-101 is a developed functional food formula using water extract of Chaenomeles sinensis and Phyllostachys bambusoides for anti-obesity. Standardization and quality control of herb mixture is more difficult than those of single herb. Additionally, the estimation of mixing ratio is an essential requirement for standardization. This study aimed to develop an efficient analytical method for the standardization of JM-101 based on C. sinensis and P. bambusoides. Protocatechuic acid and p-coumaric acid were selected as marker compounds of JM-101...
September 30, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28952032/neuroprotective-strategies-to-prevent-and-treat-parkinson-s-disease-based-on-its-pathophysiological-mechanism
#11
REVIEW
Yujeong Lee, Min-Sun Kim, Jaewon Lee
Parkinson's disease (PD) is the second most common progressive neurodegenerative disease after Alzheimer's disease. PD exhibits clinical symptoms that include tremors, rigidity, and bradykinesia. Many drugs are available to treat PD, such as, L-dopa, COMT inhibitor, MAO-B inhibitor, and dopamine agonists, but these drugs simply compensate for dopamine loss in PD, and therefore, cannot completely suppress its symptoms or progression. Although the causes of PD are not clearly understood, common pathophysiological pathways, such as, oxidative stress, mitochondrial dysfunction, and neuroinflammation are considered to be etiological factors, and thus, many treatments and interventions have been developed to target these pathophysiological factors...
September 26, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28940173/liquiritigenin-ameliorates-memory-and-cognitive-impairment-through-cholinergic-and-bdnf-pathways-in-the-mouse-hippocampus
#12
Yong-Hyun Ko, Seung-Hwan Kwon, Seok-Yong Lee, Choon-Gon Jang
Liquiritigenin (LQ), a flavonoid extracted from the radix of Glycyrrhiza, has anti-inflammatory and neuroprotective properties. In this study, we evaluated the cognitive enhancing effects of LQ on learning and memory impairments induced by scopolamine (0.5 mg/kg, i.p.), a muscarinic antagonist, using the Y-maze, passive avoidance, and novel object recognition tests. A single administration of LQ significantly improved scopolamine-induced cognitive impairments in these behavioral tests. In addition, LQ dramatically inhibited acetylcholinesterase and thiobarbituric acid reactive substance activities in the hippocampus of scopolamine-induced mice in a dose-dependent manner...
September 22, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28940036/toxicarioside-n-induces-apoptosis-in-human-gastric-cancer-sgc-7901-cell-by-activating-the-p38mapk-pathway
#13
Huan-Ge Zhao, Song-Lin Zhou, Ying-Ying Lin, Hao-Fu Dai, Feng-Ying Huang
Natural plant compounds with potent proliferation inhibition and apoptosis induction properties have been screened as novel anticancer drugs. Toxicarioside N (Tox N) was isolated from the seeds of the tropical plant Antiaris toxicaria in Hainan province, China. To our knowledge, the effects that Tox N has on the apoptosis of SGC-7901 cells and its potential mechanism have never been investigated. In this study, we detected the anticancer activities of Tox N and explored the potential mechanism in the human gastrointestinal cancer cell line SGC-7901...
September 22, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28936788/isorhamnetin-derivatives-and-piscidic-acid-for-hypercholesterolemia-cholesterol-permeability-hmg-coa-reductase-inhibition-and-docking-studies
#14
Asma Ressaissi, Nebil Attia, Pedro Luis Falé, Rita Pacheco, Bruno L Victor, Miguel Machuqueiro, Maria Luísa M Serralheiro
Bioactive compounds, such as isorhamnetin and piscidic acid, were obtained from decoctions of cladodes (stem pads from Opuntia ficus-indica). The effect of these phenolic compounds, in a fiber-free extract, were evaluated as inhibitors of cholesterol permeation through a Caco-2 cell monolayer and as 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor. A reduction of 38% in cholesterol permeation through the Caco-2 cell monolayer was obtained, and the phenolic compounds all permeated between 6 and 9%. A mixture of these compounds showed an IC50 of 20...
September 21, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28918561/marine-polysaccharides-therapeutic-efficacy-and-biomedical-applications
#15
REVIEW
Young-Eun Lee, Hyeongmin Kim, Changwon Seo, Taejun Park, Kyung Bin Lee, Seung-Yup Yoo, Seong-Chul Hong, Jeong Tae Kim, Jaehwi Lee
The ocean contains numerous marine organisms, including algae, animals, and plants, from which diverse marine polysaccharides with useful physicochemical and biological properties can be extracted. In particular, fucoidan, carrageenan, alginate, and chitosan have been extensively investigated in pharmaceutical and biomedical fields owing to their desirable characteristics, such as biocompatibility, biodegradability, and bioactivity. Various therapeutic efficacies of marine polysaccharides have been elucidated, including the inhibition of cancer, inflammation, and viral infection...
September 16, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28918452/pro-oxidant-status-and-nrf2-levels-in-psoriasis-vulgaris-skin-tissues-and-dimethyl-fumarate-treated-hacat-cells
#16
Yoon Jin Lee, Jin Ho Bae, Sang-Gue Kang, Sung Woo Cho, Dong-Il Chun, Seung Min Nam, Chul Han Kim, Hae Seon Nam, Seon Hwa Lee, Sang Han Lee, Moon Kyun Cho
Reactive oxygen species (ROS) contribute to pathogenesis of many inflammatory skin diseases, including psoriasis. The aim of this study is to compare antioxidant protein expression in psoriasis vulgaris (PV) skin tissues with that in normal skin tissues in vivo and to evaluate the effects of dimethyl fumarate (DMF), used for the treatment of psoriasis, on ROS generation and apoptosis in a human keratinocyte cell line HaCaT. Compared with normal skin tissues, PV skin tissues showed increased protein oxidation as well as down-regulation of Nrf2 and its regulatory proteins such as HO-1 and AKR1C3...
September 16, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28914418/spermidine-rescues-proximal-tubular-cells-from-oxidative-stress-and-necrosis-after-ischemic-acute-kidney-injury
#17
Jinu Kim
Kidney ischemia and reperfusion injury (IRI) is associated with a high mortality rate, which is attributed to tubular oxidative stress and necrosis; however, an effective approach to limit IRI remains elusive. Spermidine, a naturally occurring polyamine, protects yeast cells against aging through the inhibition of oxidative stress and necrosis. In the present study, spermidine supplementation markedly attenuated increases in plasma creatinine concentration and tubular injury score after IRI. In addition, exogenous spermidine potently inhibited oxidative stress, especially lipid peroxidation after IRI in kidneys and exposure to hydrogen peroxide in kidney proximal tubular cells, suppressing plasma membrane disruption and necrosis...
September 15, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28900896/fusion-of-gelonin-and-anti-insulin-like-growth-factor-1-receptor-igf-1r-affibody-for-enhanced-brain-cancer-therapy
#18
Songhee Ham, Kyoung Ah Min, Jae Wook Yang, Meong Cheol Shin
Owing to the extraordinary potency in inhibiting protein translation that could eventually lead to apoptosis of tumor cells, ribosome-inactivating proteins (RIPs) such as gelonin have been considered attractive drug candidates for cancer therapy. However, due to several critical obstacles (e.g., severe toxicity issues caused by a lack of selectivity in their mode of action and the low cytotoxicity via poor cellular uptake, etc.), clinical application of RIPs is yet far from being accomplished. To overcome these challenges, in the present study, we engineered gelonin fusion proteins with anti-insulin-like growth factor-1 receptor (IGF-1R) affibody ("IAFF") via the genetic recombinant method and the SpyCatcher/SpyTag-mediated conjugation method...
September 12, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28895057/triterpenoid-saponins-from-clinopodium-chinense-benth-o-kuntze-and-their-biological-activity
#19
Yin-Di Zhu, Jing-Yi Hong, Feng-Da Bao, Na Xing, Ling-Tian Wang, Zhong-Hao Sun, Yun Luo, Hai Jiang, Xu-Dong Xu, Nai-Liang Zhu, Hai-Feng Wu, Gui-Bo Sun, Jun-Shan Yang
Four new ursane-type triterpenoid saponins, clinopoursaponins A-D (1-4), six new oleanane-type triterpenoid saponins, clinopodiside VII-XII (5-10), as well as eight known triterpene analogues (11-18), were isolated from the aerial parts of Clinopodium chinense (Benth.) O. Kuntze. The structures of the new compounds were determined based on extensive spectral analyses, including 1D ((1)H and (13)C) and 2D NMR experiments (COSY, NOESY, HSQC, 2D TOCSY, HSQC-TOCSY and HMBC), HR-ESI-MS and chemical methods. Compounds 1-18 were evaluated for their protective effects against anoxia/reoxygenation-induced apoptosis in H9c2 cells and cytotoxicities against murine mammary carcinoma cell line 4T1...
September 11, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28887616/amitriptyline-plays-important-roles-in-modifying-the-ovarian-morphology-and-improving-its-functions-in-rats-with-estradiol-valerate-induced-polycystic-ovary
#20
Xinqiang Li, Shufen Wang, Li Zhang, Lei Zhang, Jiali Liu, Haoshu Luo, Kemian Gou, Sheng Cui
Previous studies demonstrated that depression is more prevalent in women with polycystic ovary syndrome (PCOS). In this study, we aimed to determine whether amitriptyline (AMT), an antidepressant drug, plays a role in preventing PCOS. The results showed that AMT modified ovarian morphology improved the ovarian functions and estrus cycle in estradiol valerate (EV)-induced polycystic ovary (PCO). AMT restored the levels of estradiol (E2), testosterone (T) and progesterone (P4) to normal, and elevated the level of luteinizing hormone (LH) in EV-induced PCO...
September 8, 2017: Archives of Pharmacal Research
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