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Biological & Pharmaceutical Bulletin

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https://www.readbyqxmd.com/read/28100868/growth-inhibition-of-refractory-human-gallbladder-cancer-cells-by-retinol-and-its-mechanism-of-action
#1
Chuan Li, Masahiko Imai, Shinya Hasegawa, Masahiro Yamasaki, Noriko Takahashi
Among the constituents of the essential nutrient vitamin A, retinol is a potent suppressor of refractory cancer cell growth linked to tumor progression, showing greater efficacy than retinoic acid (RA). However, the mechanisms of retinol action on human refractory cancer are not known well. In the current study, we examined the actions of retinol on proliferation of human gallbladder cancer NOZ C-1 cells. Retinol and RA inhibited the proliferation of human NOZ C-1 cells in dose-dependent manner, while RA was less potent than retinol...
January 18, 2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28100867/effects-of-pre-and-post-administration-of-vitamin-a-on-the-growth-of-refractory-cancers-in-xenograft-mice
#2
Chuan Li, Masahiko Imai, Masahiro Yamasaki, Shinya Hasegawa, Noriko Takahashi
Vitamin A is an essential nutrient that is obtained from the daily diet. The major forms of vitamin A in the body consist of retinol, retinal, retinoic acid (RA), and retinyl esters. Retinal is fundamental for vision and RA is used in clinical therapy of human acute promyelocytic leukemia. The actions of retinol and retinyl palmitate (RP) are not known well. Recently, we found that retinol is a potent anti-proliferative agent against human refractory cancers, including gallbladder cancer, being more effective than RA, while RP was inactive...
January 18, 2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28100866/development-of-intra-knee-joint-sustained-release-gel-formulation-and-evaluation-of-its-pharmacological-efficiency-in-rats
#3
Takehiro Noda, Tomoyuki Okuda, Kousuke Ban, Ryota Mizuno, Tatsuaki Tagami, Tetsuya Ozeki, Hirokazu Okamoto
In the development of a drug for intra-articular administration, a sustained-release formulation is desirable since it is difficult to sustain the effects of conventional injections due to fast drug leakage from the joint cavity. In this study, we prepared sustained release gel formulations for intra-articular administration containing indocyanine green (ICG) as a model drug to follow its fate after intra-articular administration in rats with IVIS. ICG administered as an aqueous solution leaked from the joint cavity in a short time and was excreted out of the body within a day...
January 17, 2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28003606/solubility-testing-of-sucrose-esters-of-fatty-acids-in-international-food-additive-specifications
#4
Yukino Nagai, Satoko Kawano, Kenichiro Motoda, Masaaki Tomida, Chiye Tatebe, Kyoko Sato, Hiroshi Akiyama
We investigated the solubility of 10 samples of sucrose esters of fatty acids (SEFA) products that are commercially available worldwide as food additives (emulsifiers). Although one sample dissolved transparently in both water and ethanol, other samples produced white turbidity and/or precipitates and did not meet the solubility criterion established by the Joint FAO/WHO Expert Committee on Food Additives (JECFA). When the sample solutions were heated, the solubility in both water and ethanol increased. All of the samples dissolved transparently in ethanol, and dispersed and became white without producing precipitates in water...
December 20, 2016: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/27990002/cinepazide-maleate-improves-cognitive-function-and-protects-hippocampal-neurons-in-diabetic-rats-with-chronic-cerebral-hypoperfusion
#5
Yumei Li, Ting Zhang, Xiaojie Zhang, Wenying Zou, Xian Gong, Jianliang Fu
To determine the combined effect of type 2 diabetes (T2D) and chronic cerebral hypoperfusion (CCH) on learning and spatial memory, we developed a rat model of CCH by permanent occlusion of bilateral common carotid arteries (2VO) in high-fat diet (HFD)-fed rats injected with low-dose streptozotocin (STZ). Furthermore, we examined the effect of cinepazide maleate (CM) on cognitive deficits and brain damage in this rat model. Rats were maintained on HFD for 6 weeks and then injected with 35 mg/kg STZ to induce T2D...
December 17, 2016: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/27980245/synthesis-and-characterization-of-8-nitroguanosine-3-5-cyclic-monophosphorothioate-rp-isomer-as-a-potent-inhibitor-of-protein-kinase-g1%C3%AE
#6
Khandaker Ahtesham Ahmed, Tianli Zhang, Katsuhiko Ono, Hiroyasu Tsutsuki, Tomoaki Ida, Soichiro Akashi, Keishi Miyata, Yuichi Oike, Takaaki Akaike, Tomohiro Sawa
Guanosine 3',5'-cyclic monophosphate (cGMP)-dependent protein kinases (PKG) are kinases regulating diverse physiological functions including vascular smooth muscle relaxation, neuronal synaptic plasticity, and platelet activities. Certain PKG inhibitors, such as Rp-diastereomers of derivatives of guanosine 3',5'-cyclic monophosphorothioate (Rp-cGMPS), have been designed and used to study PKG-regulated cell signaling. 8-Nitroguanosine 3',5'-cyclic monophosphate (8-nitro-cGMP) is an endogenous cGMP derivative formed as a result of excess production of reactive oxygen species and nitric oxide...
December 16, 2016: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/27980244/a-clinical-study-on-administration-of-opioid-antagonists-in-terminal-cancer-patients
#7
Yoshihiro Uekuzu, Takashi Higashiguchi, Akihiko Futamura, Akihiro Ito, Naoharu Mori, Miyo Murai, Hiroshi Ohara, Hiroko Awa, Takeshi Chihara
There have been few detailed reports on respiratory depression due to overdoses of opioids in terminal cancer patients. We investigated the situation of treatment with opioid antagonists for respiratory depression that occurred after administration of opioid at optimal doses in terminal cancer patients, to clarify pathological changes as well as causative factors. In 2,443 terminal cancer patients receiving opioids, 7 patients (0.3%) received opioid antagonists: 6, morphine (hydrochloride, 5; sulfate, 1); 1, oxycodone...
December 16, 2016: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/27980242/a-novel-analytical-method-of-cisplatin-using-the-high-performance-liquid-chromatography-with-a-naphthylethyl-group-bonded-with-silica-gel-%C3%AF-nap-column
#8
Ryuji Kato, Takaji Sato, Michiko Kanamori, Mizuho Miyake, Ayumi Fujimoto, Kyohei Ogawa, Daiki Kobata, Tomoya Fujikawa, Yukari Wada, Rintaro Mitsuishi, Kodai Takahashi, Hideki Imano, Yoshio Ijiri, Yoshiki Mino, Masahiko Chikuma, Kazuhiko Tanaka, Tetsuya Hayashi
Cisplatin is the most widely used anticancer drug in the world. Mono-chloro and none-chloro complexes of cisplatin may be believed to be the activated compounds. The separation of these compounds using octa decyl silyl column or aminopropylsilyl silica gel column is difficult because of high-reactivity and structural similarity. In this study, cisplatin, hydroxo complexes, and OH-dimer were determined by high-performance liquid chromatography (HPLC) using a naphthylethyl group bonded with silica gel (π NAP) column...
December 14, 2016: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/27916764/serotonergic-system-does-not-contribute-to-the-hypothermic-action-of-acetaminophen
#9
Akihiro Fukushima, Wakana Sekiguchi, Kizuku Mamada, Yumi Tohma, Hideki Ono
Acetaminophen (AcAP), a widely-used antipyretic and analgesic drug, has been considered to exert its effects via central mechanisms, and many studies have demonstrated that the analgesic action of AcAP involves activation of the serotonergic system. Although the serotonergic system also plays an important role in thermoregulation, the contribution of serotonergic activity to the hypothermic effect of AcAP has remained unclear. In the present study, we examined whether the serotonergic system is involved in AcAP-induced hypothermia...
December 3, 2016: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28049954/no-effect-of-slco1b1-and-cyp3a4-5-polymorphisms-on-the-pharmacokinetics-and-pharmacodynamics-of-ticagrelor-in-healthy-chinese-male-subjects
#10
Mupeng Li, Yaodong Hu, Huilan Li, Zhipeng Wen, Xiaolei Hu, Daoyu Zhang, Yanjiao Zhang, Jian Xiao, Jie Tang, Xiaoping Chen
Ticagrelor is a direct-acting P2Y12 receptor antagonist. It is rapidly absorbed and partly metabolized to the active metabolite AR-C124910XX by CYP3A4 and CYP3A5. Three genetic loci (SLCO1B1, CYP3A4, and UGT2B7) were reported to affect ticagrelor pharmacokinetics. This study aimed to investigate the possible effects of SLCO1B1 and CYP3A4/5 genetic polymorphisms on the pharmacokinetics and pharmacodynamics of ticagrelor in healthy Chinese male volunteers. Eighteen healthy male volunteers who participated in pharmacogenetics study of ticagrelor were genotyped for SLCO1B1 rs113681054, SLCO1B1*5 (rs4149056), CYP3A4*1G (rs2242480), and CYP3A5*3 (rs776746)...
2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28049953/cobalt-chloride-induces-expression-and-function-of-breast-cancer-resistance-protein-bcrp-abcg2-in-human-renal-proximal-tubular-epithelial-cell-line-hk-2
#11
Katsuki Nishihashi, Kei Kawashima, Takami Nomura, Yumiko Urakami-Takebayashi, Makoto Miyazaki, Mikihisa Takano, Junya Nagai
The human breast cancer resistance protein (BCRP/ABCG2), a member of the ATP-binding cassette transporter family, is a drug transporter restricting absorption and enhancing excretion of many compounds including anticancer drugs. The cis-regulatory elements in the BCRP promoter include a hypoxia response element, i.e., the DNA binding site for hypoxia-inducible factor-1 (HIF-1). In this study, we investigated the effect of cobalt chloride, a chemical inducer of HIF-1α, on the expression and function of BCRP in human renal proximal tubular cell line HK-2...
2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28049952/time-series-modeling-and-simulation-for-comparative-cost-effective-analysis-in-cancer-chemotherapy-an-application-to-platinum-based-regimens-for-advanced-non-small-cell-lung-cancer
#12
Yugo Chisaki, Nobuhiko Nakamura, Yoshitaka Yano
The purpose of this study was to propose a time-series modeling and simulation (M&S) strategy for probabilistic cost-effective analysis in cancer chemotherapy using a Monte-Carlo method based on data available from the literature. The simulation included the cost for chemotherapy, for pharmaceutical care for adverse events (AEs) and other medical costs. As an application example, we describe the analysis for the comparison of four regimens, cisplatin plus irinotecan, carboplatin plus paclitaxel, cisplatin plus gemcitabine (GP), and cisplatin plus vinorelbine, for advanced non-small cell lung cancer...
2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28049951/the-solubility-of-microcrystalline-cellulose-in-sodium-hydroxide-solution-is-inconsistent-with-international-specifications
#13
Hanayo Kodama, Yoshinaga Tamura, Ichiro Kamei, Kyoko Sato, Hiroshi Akiyama
Microcrystalline cellulose (MCC) is used globally as an inactive ingredient in food and nutraceutical products and is commonly used as a food additive. To confirm the conformity of MCC to the solubility requirements stipulated in international specifications, the solubilities of commercially available MCC products were tested in sodium hydroxide (NaOH) solution. All of the samples were insoluble in NaOH solution, which is inconsistent with the descriptions provided in international specifications. We also prepared celluloses with different degree of polymerization (DP) values by acid hydrolysis...
2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28049950/anticytotoxin-effects-of-amentoflavone-to-pneumolysin
#14
Xiaoran Zhao, Bowen Liu, Shui Liu, Lin Wang, Jianfeng Wang
Pneumolysin (PLY) is a devastating bacterial protein toxin of Streptococcus pneumoniae that punctures the cytomembrane, leading to pathological reactions, such as cell disruption and inflammation. Drugs capable of closely impacting the toxin are considered advantageous in the treatment of bacterial infections. Amentoflavone (AMF) is a chemical substance extracted from traditional Chinese herbs. Previous studies have demonstrated that AMF has multiple pharmacological effects and mentioned without attenuating pneumolysin-mediated cytotoxicity...
2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28049949/differential-contribution-of-nerve-derived-noradrenaline-to-high-k-induced-contraction-depending-on-type-of-artery
#15
Hirotake Ishida, Shin-Ya Saito, Eita Hishinuma, Tomohisa Ishikawa
High K(+)-induced contraction of arterial smooth muscle is thought to be mediated by membrane depolarization and subsequent activation of voltage-dependent Ca(2+) channels (VDCCs). In line with this, this study found that contraction induced by 80 mM K(+) was almost abolished by nifedipine (1 µM), a VDCC inhibitor, in isolated rat aorta, and was markedly suppressed in the iliac artery. However, nifedipine (1 µM) only partially suppressed high K(+)-induced contraction in the tail artery. The contractions remaining in the arteries were further reduced by non-selective cation channel (NSCC) inhibitors, including 2-aminoethoxydiphenyl borate (2-APB) (100 µM), SK&F96365 (10 µM), and 3,4-dihydro-6,7-dimethoxy-α-phenyl-N,N-bis[2-(2,3,4-trimethoxyphenyl)ethyl]-1-isoquinolineacetamide hydrochloride (LOE908) (10 µM)...
2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28049948/abnormal-n-glycosylation-of-a-novel-missense-creatine-transporter-mutant-g561r-associated-with-cerebral-creatine-deficiency-syndromes-alters-transporter-activity-and-localization
#16
Tatsuki Uemura, Shingo Ito, Yusuke Ohta, Masanori Tachikawa, Takahito Wada, Tetsuya Terasaki, Sumio Ohtsuki
Cerebral creatine deficiency syndromes (CCDSs) are caused by loss-of-function mutations in creatine transporter (CRT, SLC6A8), which transports creatine at the blood-brain barrier and into neurons of the central nervous system (CNS). This results in low cerebral creatine levels, and patients exhibit mental retardation, poor language skills and epilepsy. We identified a novel human CRT gene missense mutation (c.1681 G>C, G561R) in Japanese CCDSs patients. The purpose of the present study was to evaluate the reduction of creatine transport in G561R-mutant CRT-expressing 293 cells, and to clarify the mechanism of its functional attenuation...
2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28049947/stabilization-of-ephedrine-alkaloid-content-in-ephedra-sinica-by-selective-breeding-and-stolon-propagation
#17
Hajime Hiyama, Aya Ozawa, Hiroaki Kumazawa, Osami Takeda
The Ephedra herb, which has been used in Kampo medicines, originates from terrestrial stems of Ephedra species. It is important to establish cultivation methods and cultivars to secure a stable supply of the Ephedra herb that would meet the quality standards for the ephedrine alkaloids content. In this study, we first grew Ephedra sinica plants derived from seeds in the field for 5 years. Then, for selective breeding of cultivars that could meet the quality standards for the ephedrine alkaloids content, we measured the content of total alkaloids (TAs), ephedrine (Eph), and pseudoephedrine (PEph) in individual plants derived from seedlings and grown for 4 years in the field...
2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28049946/ursodeoxycholic-acid-ameliorates-intrahepatic-cholestasis-independent-of-biliary-bicarbonate-secretion-in-vil2-kd-kd-mice
#18
Ryo Hatano, Kotoku Kawaguchi, Fumitaka Togashi, Masato Sugata, Shizuka Masuda, Shinji Asano
Ursodeoxycholic acid (UDCA) is a hydrophilic bile acid that possesses many pharmacological effects, including increasing bile flow, changing the hydrophobicity of the bile acid pool, and modulation of the immune response. UDCA has been approved for treating cholestatic liver disease, such as primary biliary cholangitis. However, several unanticipated severe side effects of UDCA are observed in cholestatic patients, and its pharmacological benefits remain controversial. We reported that ezrin-knockdown (Vil2(kd/kd)) mice exhibited severe hepatic injury because of a functional disorder in bile duct fluidity and alkalinity regulation, resembling human intrahepatic cholestatic disease...
2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28049945/inflammatory-effects-of-nitrogen-containing-bisphosphonates-n-bps-modulation-by-non-n-bps
#19
Kazuhiro Shima, Masahiro Tsuchiya, Takefumi Oizumi, Teruko Takano-Yamamoto, Shunji Sugawara, Yasuo Endo
Bisphosphonates (BPs) are used against diseases with enhanced bone resorption. Those classed as nitrogen-containing BPs (N-BPs) exhibit much stronger anti-bone-resorptive effects than non-nitrogen-containing BPs (non-N-BPs). However, N-BPs carry the risk of inflammatory/necrotic side effects. Depending on their side-chains, BPs are divided structurally into cyclic and non-cyclic types. We previously found in mice that etidronate and clodronate (both non-cyclic non-N-BPs) could reduce the inflammatory effects of all three N-BPs tested (cyclic and non-cyclic types), possibly by inhibiting their entry into soft-tissue cells via SLC20 and/or SLC34 phosphate transporters...
2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28049944/controlled-secretion-of-the-anticancer-protein-mda-7-from-engineered-mesenchymal-stem-cells
#20
Atsunobu Sagara, Takeshi Karasawa, Katsuhide Igarashi, Maky Otsuka, Rei Sugiura, Akihiro Kodama, Mutsumi Yamashita, Minoru Narita, Yoshinori Kato
Mesenchymal stem cells (MSCs) have been explored as a "live" carrier of cytokines for targeted cancer therapy, but, in earlier reports in the literature, the secretion process of therapeutic cytokines was not regulated. The purpose of this study was to generate MSCs to conditionally secrete the melanoma differentiation-associated gene-7 (MDA-7) tumor-suppressor protein. To control the secretion of MDA-7 from MSCs, a well-established tetracycline-controlled transcriptional activation system was incorporated into MDA-7 plasmid...
2017: Biological & Pharmaceutical Bulletin
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