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Archives of Pharmacal Research

Zheng-Xi Zhang, Kun Feng, Xian-Jin Sui, Wen-Shu Wang, Lin Wang, Dong-Hong Wang, Xiao-Min Luo, Xiao-Fei Chen
Four new acylated triterpene glycosides with aliphatic chains (4-7) as well as five known triterpenoids were isolated from the flower buds of Staphylea bumalda with bioassay guidance. Their structures were determined on the basis of spectral techniques, including IR, 1D and 2D NMR, and HR-APCI-MS. Most compounds (except 8) were isolated from S. bumalda for the first time. Additionally, the neuroprotective effects of 1 and 4-9 on suckling rat primary cultured hippocampal neurons against H2 O2 -induced injury were evaluated in vitro...
October 30, 2018: Archives of Pharmacal Research
Gil-Im Mun, Seoyoung Kim, Eun Choi, Cha Soon Kim, Yun-Sil Lee
Radiotherapy is one of the most efficient ways to treat cancer. However, deleterious effects, such as acute and chronic toxicities that reduce the quality of life, may result. Naturally occurring compounds have been shown to be non-toxic over wide dose ranges and are inexpensive and effective. Additionally, pharmacological strategies have been developed that use radioprotectors to inhibit radiation-induced toxicities. Currently available radioprotectors have several limitations, including toxicity. In this review, we present the mechanisms of proven radioprotectors, ranging from free radical scavenging (the best-known mechanism of radioprotection) to molecular-based radioprotection (e...
October 25, 2018: Archives of Pharmacal Research
Huy X Luong, Do-Hee Kim, Bong-Jin Lee, Young-Woo Kim
We previously reported a series of amphipathic helices of stapled heptapeptides as membrane-lytic antimicrobial peptides. These peptides possess three lysine residues as the sole cationic amino acid residues in their hydrophilic face of the helix. Lysine-to-arginine substitution is often shown to increase antimicrobial activity of many natural AMPs due to the more favorable interactions of guanidinium moiety of arginine with membranes. In an effort to further improve the pharmacological properties of our novel AMP series, we here examined the impact of lysine-to-arginine substitution on their structures and antimicrobial and hemolytic activities...
October 25, 2018: Archives of Pharmacal Research
Young Eun Du, Jin Su Lee, Hye Mi Kim, Ji-Hye Ahn, In Ho Jung, Jong Hoon Ryu, Jung-Hye Choi, Dae Sik Jang
A new phenylpropanoid (1), a new alkaloid (11), and a new natural polyacetylene (17), together with nine phenolic compounds (2-10), five alkaloids (12-16), three polyacetylenes (18-20), three triterpenoidal saponins (21-23), one phenylethanoid glycoside (24), and three hexyl glycosides (25-27) with previous known structures, were isolated from the roots of Codonopsis lanceolata. All of the isolates 1-27 were evaluated for their inhibitory effects on LPS-induced nitric oxide (NO) production in RAW 264.7 macrophages and cell viability in A2780 human ovarian cancer cells...
September 27, 2018: Archives of Pharmacal Research
Pil-Hoon Park
Adipose tissue acts as a dynamic endocrine organ playing critical roles in many metabolic and immune responses. Endocrine functions by adipose tissue are achieved by secretion of diverse cytokines and hormones, collectively called adipokines. Adiponectin and leptin the most abundantly expressed adipokines within adipose tissue have an impact on various physiological responses. While both adiponectin and leptin are secreted from the same location, their physiological functions are not identical. Adiponectin possesses potent anti-inflammatory properties and anti-tumor activities, whereas leptin acts as a pro-inflammatory hormone and generates tumor-promoting effects...
September 27, 2018: Archives of Pharmacal Research
Jinha Yu, Gyudong Kim, Dnyandev B Jarhad, Hyuk Woo Lee, Jiyoun Lee, Chong Woo Park, Hunjoo Ha, Lak Shin Jeong
Truncated 4'-thionucleosides 1-4 and 4'-oxonucleosides 5-8 as potent and selective A3 AR antagonists were synthesized from D-mannose and D-erythronic acid γ-lactone, respectively. These nucleosides were evaluated for their anti-fibrotic renoprotective activity in TGF-β1-treated murine proximal tubular (mProx) cells. Their antagonistic activities for A3 AR were proportional to their inhibitory activities against TGF-β1-induced collagen I upregulation in mProx cells. This result suggests that the binding affinity of A3 AR antagonists is closely correlated with their anti-fibrotic activity...
September 27, 2018: Archives of Pharmacal Research
Shinhyun Kim, Yinhua Zhang, Chunmei Jin, Yeunkum Lee, Yoonhee Kim, Kihoon Han
In the mammalian brain, neuronal excitatory synaptic development, function, and plasticity largely rely on dynamic, activity-dependent changes in the macromolecular protein complex called the postsynaptic density (PSD). Activity-dependent Lys48-linked polyubiquitination and subsequent proteasomal degradation of key proteins in the PSD have been reported. However, investigations into the functions and regulatory mechanisms of Lys63-linked polyubiquitination, the second most abundant polyubiquitin form in synapses, have recently begun...
September 26, 2018: Archives of Pharmacal Research
Haonan Li, Baojia Sun, Mingying Wang, Xu Hu, Xiang Gao, Shengtao Xu, Yongnan Xu, Jinyi Xu, Huiming Hua, Dahong Li
Diterpenoids are important and widely distributed natural compounds with various biological effects, including antitumor, anti-inflammatory and so on. Great efforts have been put in phytochemistry research on diterpenoids. A number of structural modified derivatives and pharmacophore incorporated hybrids were also designed and synthesized with promising therapeutic effects. Among the hopefuls, enmein-type 6,7-seco-ent-kaurane diterpenoids with unique ring system and stereogenic centers exhibit attractive activities...
September 21, 2018: Archives of Pharmacal Research
Jung-Hyun Cho, Ah Hyun Kim, Seulah Lee, Yujeong Lee, Won Jong Lee, Seung-Cheol Chang, Jaewon Lee
Bisphenol A (BPA) is an environmental toxin widely used in manufacturing industries. Studies conducted on the neurotoxicity of BPA demonstrated that at excessive, high concentrations (≥ 200 µM) adverse responses occurred which were not detectable using traditional toxicity tests at lower chemical quantities than 200 µM. Thus, a method capable of effectively detecting neurotoxicity at low concentrations (≤ 100 µM) was devised. Bisphenol A-mediated neurotoxicity was examined in primary cultured neurons using various methods, including Western blot, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) cytotoxicity and reactive oxygen species assays...
September 20, 2018: Archives of Pharmacal Research
Kwangsik Park, Juyoung Park, Handule Lee, Jonghye Choi, Wook-Joon Yu, Jinsoo Lee
Toxicity and target organ distribution of cerium oxide nanoparticles (CeNPs) were investigated via single intravenous injection and single oral administration, respectively. Rats were sacrificed at 24 h after treatment with doses of 30 and 300 mg/kg, and cerium concentrations were measured in liver, kidney, spleen, lung, blood, urine and feces. Results revealed cerium levels in blood and tissues were considerably low in oral treated groups and most cerium was detected in feces, meaning CeNPs would not be absorbed in the gastro-intestinal system...
September 3, 2018: Archives of Pharmacal Research
Yun-Shan Fang, Ming-Hui Yang, Le Cai, Jia-Peng Wang, Tian-Peng Yin, Jing Yu, Zhong-Tao Ding
Two new phenylpropanoids, retusiusines A (1) and B (2), and a pair of new phenylpropyl enantiomers, (±)-retusiusine C (3a and 3b), together with eight known compounds, dihydroconiferyl dihydro-p-coumarate (4), methyl 3-(4-hydroxyphenyl) propionate (5), 3-(4-hydroxyphenyl)-propanoic acid (6), dihydroferulic acid (7), methyl 3-(4-methoxyphenyl) propionate (8), 3-(3,4-dimethoxyphenyl)-2-propenal (9), trans-p-coumaric acid (10) and dihydroconiferyl alcohol (11), were isolated from the tubers of Bulbophyllum retusiusculum...
August 27, 2018: Archives of Pharmacal Research
Juhee Lim, Yeojin Bang, Hyun Jin Choi
Parkinson's disease (PD) is a common progressive neurodegenerative disorder characterized by motor dysfunction, including bradykinesia, tremor, rigidity, and postural instability. Recent clinical findings recognize PD as a complex disease with diverse neuropsychiatric complications. Depression is the most frequent non-motor psychiatric symptom experienced in PD, and it is associated with poor quality of life. While the pathophysiology of PD-associated depression is not directly related to neurodegenerative processes in the substantia nigra, underlying mechanisms remain unclear and there are few symptomatic treatments...
October 2018: Archives of Pharmacal Research
Yoonjin Nam, Young Sil Min, Uy Dong Sohn
Irritable bowel syndrome (IBS), a common gastrointestinal (GI) disorder, is associated with various factors, including lifestyle, infection, stress, intestinal flora, and related diseases. The pharmacotherapeutic stimulation of receptors and downstream signaling pathways is effective in reducing IBS symptoms; however, it is still associated with adverse effects. Various receptors related to GI motility and visceral hypersensitivity should be considered to enhance the benefit/risk ratio of IBS treatments. This review discusses recent pharmacological advances in IBS management...
October 2018: Archives of Pharmacal Research
Xue Zhu, Ke Wang, Fanfan Zhou, Ling Zhu
Abnormal accumulation of the free-form all-trans-retinal (atRAL), a major intermediate of human visual cycle, is considered to be a key cause of retinal pigment epithelial (RPE) dysfunction in the pathogenesis of retinal degenerative diseases such as age-related macular degeneration (AMD). Paeoniflorin (PF), a monoterpene glucoside isolated from Paeonia lactiflora Pall., has been used in clinical treatment of retinal degenerative diseases in China for several years; however, the underlying mechanism remains unclear...
October 2018: Archives of Pharmacal Research
Mina Kim, Young Sil Min, Uy Dong Sohn
Indomethacin is a non-steroidal anti-inflammatory drug with clearly known side effects on the gastrointestinal tract. The purpose of the present study was to investigate whether eupatilin inhibit cell injury induced by indomethacin in cultured feline esophageal epithelial cells (EECs). EECs were used to investigate the ability of eupatilin to induce the expression of heat shock proteins (HSP27 and HSP70) and analyze its cytoprotective effect against indomethacin-induced damage. The treatment of EECs with indomethacin for 8 h decreased cell viability...
October 2018: Archives of Pharmacal Research
Ji-Young Byeon, Young-Hoon Kim, Choong-Min Lee, Se-Hyung Kim, Won-Ki Chae, Eui-Hyun Jung, Chang-Ik Choi, Choon-Gon Jang, Seok-Yong Lee, Jung-Woo Bae, Yun Jeong Lee
Cytochrome P450 (CYP) 2D6 is present in less than about 2% of all CYP enzymes in the liver, but it is involved in the metabolism of about 25% of currently used drugs. CYP2D6 is the most polymorphic among the CYP enzymes. We determined alleles and genotypes of CYP2D6 in 3417 Koreans, compared the frequencies of CYP2D6 alleles with other populations, and observed the differences in pharmacokinetics of metoprolol, a prototype CYP2D6 substrate, depending on CYP2D6 genotype. A total of 3417 unrelated healthy subjects were recruited for the genotyping of CYP2D6 gene...
September 2018: Archives of Pharmacal Research
Ji-Yeong Byeon, Young-Hoon Kim, Se-Hyung Kim, Choong-Min Lee, Eui-Hyun Jung, Won-Ki Chae, Choon-Gon Jang, Seok-Yong Lee, Yun Jeong Lee
Zolpidem is predominantly metabolized by CYP3A4, and to a lesser extent by CYP2C9, CYP1A2, CYP2D6 and CYP2C19. The aim of this study was to identify the effects of CYP2C9*3 allele on the pharmacokinetics of zolpidem. Healthy male subjects were divided into two genotype groups, CYP2C9*1/*1 and CYP2C9*1/*3. They received a single oral dose of 5 mg zolpidem, and the plasma concentrations of zolpidem were determined up to 12 h after drug administration. In addition, since zolpidem is metabolized at a high rate by CYP3A4, the effect of CYP2C9*3 allele on the pharmacokinetics of zolpidem was also observed in the condition where CYP3A4 was sufficiently inhibited by the steady-state concentration of clarithromycin, a potent CYP3A4 inhibitor...
September 2018: Archives of Pharmacal Research
Seung Hwa Kim, Kyung Hwa Cho, Yu Na Kim, Bo Young Jeong, Chang Gyo Park, Gang Min Hur, Hoi Young Lee
Unfortunately, there are some errors in Fig. 1b and Fig. 3a of the article.
September 2018: Archives of Pharmacal Research
Wook-Ha Park, Young-Chul Kang, Ying Piao, Daniel Hyungseok Pak, Youngmi Kim Pak
We regret that there is an error in the labeling of Fig. 4 of the published original article. The concentration of MPP+ should be corrected to 1.0 mM instead of 0.5 mM. The corrected figure should be.
September 2018: Archives of Pharmacal Research
Hyojeong Choi, Aree Moon
Unfortunately, there is an error in the original version of the article. The original published article contains an incomplete 'Acknowledgements' section. Please find the full 'Acknowledgements' section below.
September 2018: Archives of Pharmacal Research
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