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Archives of Pharmacal Research

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https://www.readbyqxmd.com/read/29460135/simvastatin-reduces-adrenal-catecholamine-secretion-evoked-by-stimulation-of-cholinergic-nicotinic-and-angiotensinergic-at-1-receptors
#1
Young-Kwon Koh, Ki-Hwan Kim, Mee-Sung Choi, Young-Youp Koh, Dong-Yoon Lim
We investigated the influence of simvastatin, a statin, on the secretion of catecholamines (CA) in rat adrenal glands, and clarified its action mechanism. Simvastatin suppressed acetylcholine (ACh)-evoked CA release in a dose- and time-dependent fashion. In the presence of simvastatin, CA secretion evoked by 1.1-dimethyl-4-phenyl piperazinium iodide (DMPP), angiotensin II, high K+ , veratridine, and Bay-K-8644 was time-dependently inhibited. However, in the simultaneous presence of simvastatin and Nω-nitro-L-arginine methyl ester hydrochloride, CA secretion evoked by angiotensin II and DMPP recovered to control levels...
February 19, 2018: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29450862/recent-progress-in-dendrimer-based-nanomedicine-development
#2
REVIEW
Yejin Kim, Eun Ji Park, Dong Hee Na
Dendrimers offer well-defined nanoarchitectures with spherical shape, high degree of molecular uniformity, and multiple surface functionalities. Such unique structural properties of dendrimers have created many applications for drug and gene delivery, nanomedicine, diagnostics, and biomedical engineering. Dendrimers are not only capable of delivering drugs or diagnostic agents to desired sites by encapsulating or conjugating them to the periphery, but also have therapeutic efficacy in their own. When compared to traditional polymers for drug delivery, dendrimers have distinct advantages, such as high drug-loading capacity at the surface terminal for conjugation or interior space for encapsulation, size control with well-defined numbers of peripheries, and multivalency for conjugation to drugs, targeting moieties, molecular sensors, and biopolymers...
February 15, 2018: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29397551/finasteride-inhibits-melanogenesis-through-regulation-of-the-adenylate-cyclase-in-melanocytes-and-melanoma-cells
#3
Jae Ok Seo, Silvia Yumnam, Kwang Won Jeong, Sun Yeou Kim
Finasteride is a well-known 5α-reductase inhibitor used for treatment of alopecia and prostate cancer. But the effect of finasteride in regulating melanogenesis is still unclear. In the present study the role of finasteride on melanogenesis was investigated. Finasteride decrease melanin level in melanocyte melan-a cells and B16F10 melanoma cells without inducing cytotoxicity. MC1R (melanocortin 1 receptor) protein expression was also inhibited by finasteride thereby decreasing the expression of adenylate cyclase, MITF (Melanogenesis associated transcription factor), tyrosinases, TRP (tyrosinase-related protein) -1 and -2...
February 3, 2018: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29397550/linear-diarylheptanoids-as-potential-anticancer-therapeutics-synthesis-biological-evaluation-and-structure-activity-relationship-studies
#4
A F M Motiur Rahman, Yang Lu, Hwa-Jong Lee, Hyunji Jo, Wencui Yin, Mohammad Sayed Alam, Hyochang Cha, Adnan A Kadi, Youngjoo Kwon, Yurngdong Jahng
In efforts to develop effective anticancer therapeutics with greater selectivity toward cancerous cell and reduced side-effects, such as emetic effects due to detrimental action of the drug toward the intestinal flora, a series of linear diarylheptanoids (LDHs) were designed and synthesized in 7 steps with good-to-moderate yields. All synthesized compounds were evaluated for their antibacterial, antiproliferative, and topoisomerase-I and -IIα inhibitory activity. Overall, all compounds showed little to no activity against the bacterial strains tested...
February 3, 2018: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29392509/anti-inflammatory-effects-of-sinapic-acid-on-2-4-6-trinitrobenzenesulfonic-acid-induced-colitis-in-mice
#5
Ji-Yun Lee
This study was conducted to evaluate the effect of sinapic acid, a cinnamic acid derivative, on inflammatory changes in a mouse model of colitis. Colitis was induced by intracolonic instillation of 2,4,6-trinitrobenzenesulfonic acid (TNBS). Sinapic acid (10, 30, and 100 mg/kg) and dexamethasone (2 mg/kg) were orally administered to Balb/c female mice after TNBS instillation. The anti-inflammatory effect of sinapic acid on colonic injury or damage was assessed by clinical, macroscopic, microscopic, and biochemical analyses...
February 1, 2018: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29332183/identification-of-n-arylsulfonylpyrimidones-as-anticancer-agents
#6
Santhosh Subramanian, Pulla Reddy Boggu, Jieun Yun, Sang-Hun Jung
For confirming the role of five membered ring of imidazolidinone moiety of N-arylsulfonylimidazolidinones (7) previously reported with highly potent anticancer agent, a series of N-arylsulfonylpyrimidones (10a-g) and N-arylsulfonyltetrahydropyrimidones (11a-e) were prepared and their anti-proliferating activity was measured against human cancer cell lines (renal ACHN, colon HCT-15, breast MDA-MB-231, lung NCI-H23, stomach NUGC-3, and prostate PC-3) using XTT assay. Among them, 1-(1-acetylindolin-5-ylsulfonyl)-4-phenyltetrahydropyrimidin-2(1H)-one (11d, mean GI50 = 3...
January 13, 2018: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29275496/dihydropyranoaurone-compound-damaurone-d-inhibits-lps-induced-inflammation-and-liver-injury-by-inhibiting-nf-%C3%AE%C2%BAb-and-mapk-signaling-independent-of-ampk
#7
Zheng Wang, Sun-O Ka, Young Taek Han, Eun Ju Bae
Recently, we reported the synthesis of damaurone D (DD), originally derived from Rosa damascene, and its anti-inflammatory effect in macrophages. Here, we investigated the molecular mechanism underlying the anti-inflammatory effect of DD in macrophages and further tested whether DD is protective against lipopolysaccharide (LPS)-induced liver injury. DD inhibited LPS-stimulated expression of pro-inflammatory genes and cytokine/chemokine secretion in a concentration-dependent manner in RAW 264.7 cells and thioglycolate-elicited mouse peritoneal macrophages...
December 23, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29243040/protective-effect-of-acacetin-on-sepsis-induced-acute-lung-injury-via-its-anti-inflammatory-and-antioxidative-activity
#8
Li-Chao Sun, Hong-Bo Zhang, Cheng-Dong Gu, Shi-Dong Guo, Gang Li, Rui Lian, Yao Yao, Guo-Qiang Zhang
Sepsis is a clinical syndrome with no effective protective or therapeutic treatments. Acacetin, a natural flavonoid compound, has anti-oxidative and anti-inflammatory effects which can potentially work to reduce sepsis. We investigated the potential protective effect of acacetin on sepsis-induced acute lung injury (ALI) ALI and dissect out the underlying mechanisms. Mice were divided into five groups: a sham group, a sepsis-induced ALI group, and three sepsis groups pre-treated with 20, 40, and 80 mg/kg body weight of acacetin...
December 14, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29243039/alkaloids-from-narcissus-poeticus-cv-pink-parasol-of-various-structural-types-and-their-biological-activity
#9
Marcela Šafratová, Anna Hošťálková, Daniela Hulcová, Kateřina Breiterová, Veronika Hrabcová, Marta Machado, Diana Fontinha, Miguel Prudêncio, Jiří Kuneš, Jakub Chlebek, Daniel Jun, Martina Hrabinová, Lucie Nováková, Radim Havelek, Martina Seifrtová, Lubomír Opletal, Lucie Cahlíková
Fifteen Amaryllidaceae alkaloids (1-15) of various structural types were isolated by standard chromatographic methods from fresh bulbs of Narcissus poeticus cv. Pink Parasol. The chemical structures were elucidated by MS, and 1D and 2D NMR spectroscopic analyses, and by comparison with literature data. Narcipavline (5) and narcikachnine (6) are reported here for the first time. In their structure are combined two basic structural types of Amaryllidaceae alkaloids (galanthamine- and galanthindole-structural types), which represent a new structural type of these compounds...
December 14, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29230690/dihydroxanthyletin-type-coumarins-from-angelica-decursiva-that-inhibits-the-formation-of-advanced-glycation-end-products-and-human-recombinant-aldose-reductase
#10
Md Yousof Ali, Hyun Ah Jung, Susoma Jannat, Jae Sue Choi
The formation of advanced glycation end-products (AGE) and aldose reductase activity have been implicated in the development of diabetic complications. The present study was aimed to evaluate human recombinant aldose reductase (HRAR) and AGE inhibitory activity of seven natural dihydroxanthyletin-type coumarins, 4-hydroxy Pd-C-III (1), 4'-methoxy Pd-C-I (2), Pd-C-I (3), Pd-C-II (4), Pd-C-III (5), decursidin (6), and (+)-trans-decursidinol (7) from Angelica decursiva. Coumarins 1-7 showed potent HRAR and AGE inhibitory activities with ranges of IC50 values of 1...
December 11, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29230689/the-combination-of-curcumin-and-5-fluorouracil-in-cancer-therapy
#11
REVIEW
Yumeng Wei, Panjing Yang, Shousong Cao, Ling Zhao
5-Fluorouracil (5-FU) alone or in combination with other therapeutic drugs has been widely used for clinical treatment of various cancers. However, 5-FU-based chemotherapy has limited anticancer efficacy in clinic due to multidrug resistance and dose-limiting cytotoxicity. Some molecules and genes in cancer cells, such as nuclear factor kappa B, insulin-like growth factor-1 receptor, epidermal growth factor receptor, cyclooxygenase-2, signal transducer and activator of transcription 3, phosphatase and tensin homolog deleted on chromosome ten and Bcl-2 etc...
December 11, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29230688/therapeutic-effects-of-histone-deacetylase-inhibitors-on-kidney-disease
#12
REVIEW
Pusoon Chun
Increasing evidence has shown the involvement of histone deacetylases (HDACs) in the development and progression of various renal diseases, highlighting its inhibition as a promising therapeutic strategy to prevent kidney diseases. Accordingly, numerous studies have shown that HDAC inhibitors protect the kidneys from various diseases through their effects on multiple pathways, such as suppression of transforming growth factor-β signaling pathway and nuclear factor-κB signaling pathways, augmentation of apoptosis, and inhibition of angiogenesis...
December 11, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29214601/emerging-potential-of-stimulus-responsive-nanosized-anticancer-drug-delivery-systems-for-systemic-applications
#13
REVIEW
Hima Bindu Ruttala, Thiruganesh Ramasamy, Thiagarajan Madeshwaran, Tran Tuan Hiep, Umadevi Kandasamy, Kyung Taek Oh, Han-Gon Choi, Chul Soon Yong, Jong Oh Kim
The development of novel drug delivery systems based on well-defined polymer therapeutics has led to significant improvements in the treatment of multiple disorders. Advances in material chemistry, nanotechnology, and nanomedicine have revolutionized the practices of drug delivery. Stimulus-responsive material-based nanosized drug delivery systems have remarkable properties that allow them to circumvent biological barriers and achieve targeted intracellular drug delivery. Specifically, the development of novel nanocarrier-based therapeutics is the need of the hour in managing complex diseases...
December 6, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29214600/apoptosis-induction-by-alantolactone-in-breast-cancer-mda-mb-231-cells-through-reactive-oxygen-species-mediated-mitochondrion-dependent-pathway
#14
Li Cui, Weiquan Bu, Jie Song, Liang Feng, Tingting Xu, Dan Liu, Wenbo Ding, Jianhua Wang, Changyang Li, Binge Ma, Yi Luo, Ziyu Jiang, Chengcheng Wang, Juan Chen, Jian Hou, Hongmei Yan, Lei Yang, Xiaobin Jia
Alantolactone is a sesquiterpene lactone isolated from Inula helenium L. Although alantolactone possesses anti-inflammation and apoptosis-induction activities, the underlying mechanism of anti-cancer effect on human breast cancer cells remains largely unknown. In this study, we explored the possibility of alantolactone as an apoptosis-inducing cytotoxic agent using MDA-MB-231 cells as in vitro model. Alantolactone significantly induced its apoptosis, demonstrated by cell cycle analysis, annexin V-APC/7-AAD double staining and dUTP nick end labeling...
December 6, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29214599/protein-tyrosine-phosphatase-1b-inhibitors-from-natural-sources
#15
REVIEW
Bing Tian Zhao, Duc Hung Nguyen, Duc Dat Le, Jae Sue Choi, Byung Sun Min, Mi Hee Woo
Since PTP1B enzyme was discovered in 1988, it has captured the research community's attention. This landmark discovery has stimulated numerous research studies on a variety of human diseases, including cancer, inflammation, and diabetes. Tremendous progress has been made in finding PTP1B inhibitors and exploring PTP1B regulatory mechanisms. This review investigates for the natural PTP1B inhibitors, and focuses on the common characteristics of the discovered structures and structure-activity relationships. To facilitate understanding, all the natural compounds are here divided into five different classes (fatty acids, phenolics, terpenoids, steroids, and alkaloids), according to their skeletons...
December 6, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29196918/nafamostat-mesilate-negatively-regulates-the-metastasis-of-triple-negative-breast-cancer-cells
#16
Sunam Mander, Dong-Joo You, Sumi Park, Dong Hwi Kim, Hyo Jeong Yong, Dong-Sik Kim, Curie Ahn, Yun-Hee Kim, Jae Young Seong, Jong-Ik Hwang
Triple-negative breast cancer (TNBC) lacking of oestrogen receptor, progesterone receptor, and epidermal growth factor receptor type 2 is a highly malignant disease which results in a poor prognosis and rare treatment options. Despite the use of conventional chemotherapy for TNBC tumours, resistance and short duration responses limit the treatment efficacy. Therefore, a need exists to develop a new chemotherapy for TNBC. The aim of this study was to examine the anti-cancer effects of nafamostat mesilate (NM), a previously known serine protease inhibitor and highly safe drug on breast cancer cells...
December 1, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29196917/development-of-a-linear-dual-column-hplc-ms-ms-method-and-clinical-genetic-evaluation-for-tramadol-and-its-phase-i-and-ii-metabolites-in-oral-fluid
#17
Hyerim Yu, Seongkuk Hong, Chul-Ho Jeong, Jung-Woo Bae, Sooyeun Lee
Tramadol is a centrally acting synthetic opioid analgesic and has received special attention due to its abuse potential and unexpected responses induced by CYP2D6 polymorphism. Oral fluid is an advantageous biofluid for drug analysis due to non-invasive sampling and high correlation of drug concentrations with plasma. However, few studies have been performed on distribution of tramadol and its metabolites in oral fluid. In the present study, a linear dual column HPLC-MS/MS method was developed and fully validated for the simultaneous determination of tramadol and its phase I [O-desmethyltramadol (ODMT), N-desmethyltramadol (NDMT) and N,O-didesmethyltramadol (NODMT)] and II metabolites in oral fluid...
December 1, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29181640/impact-of-gut-microbiota-on-drug-metabolism-an-update-for-safe-and-effective-use-of-drugs
#18
REVIEW
Keumhan Noh, You Ra Kang, Mahesh Raj Nepal, Rajina Shakya, Mi Jeong Kang, Wonku Kang, Sangkyu Lee, Hye Gwang Jeong, Tae Cheon Jeong
The intestinal mucosa and liver have long been considered as the main sites of drug metabolism, and the contribution of gut microbiota to drug metabolism has been under-estimated. However, it is now generally accepted that the gut microbiota plays an important role in drug metabolism prior to drug absorption or during enterohepatic circulation via various microbial enzymatic reactions in the intestine. Moreover, some drugs are metabolized by gut microbiota to specific metabolite(s) that cannot be formed in the liver...
November 27, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29177586/phenolic-amides-from-tribulus-terrestris-and-their-inhibitory-effects-on-nitric-oxide-production-in-raw-264-7-cells
#19
Hyung Sik Kim, Jin Woo Lee, Hari Jang, Thi Phuong Linh Le, Jun Gu Kim, Moon Soon Lee, Jin Tae Hong, Mi Kyeong Lee, Bang Yeon Hwang
A new phenolic amide, named cis-terrestriamide (7), together with ten known compounds (1-6, 8-11), were isolated from the methanolic extract of the fruits of Tribulus terrestris. The structure of 7 was elucidated on the basis of extensive analyses of 1D and 2D nuclear magnetic resonance spectroscopic and high resolution mass spectrometry data. Compounds 1, 2, 5, 6, 8, 9, and 11 exhibited inhibitory effects on the lipopolysaccharide-stimulated nitric oxide production in RAW 264.7 cells, with IC50 values of 18...
November 25, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29177585/the-role-of-exercise-induced-myokines-in-regulating-metabolism
#20
REVIEW
Joo Young Huh
Exercise has beneficial effects in ameliorating metabolic disorders, and a combined therapeutic regimen of regular exercise and pharmaceutical treatment is often recommended. Exercise biology is complex and it involves various metabolic and molecular changes that translate into changes in substrate utilization, enzyme activation, and alternatively, improvement in exercise performance. Besides the effect of exercise on muscle metabolism, it has recently been discovered that contracting muscle can induce secretion of molecules called myokines...
November 25, 2017: Archives of Pharmacal Research
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