abstract：:An investigation into the methanol extracts obtained from the stems of Dodonaea viscosa led to the isolation of one nor-clerodane diterpene (1) and two labdane diterpenes (2, 3), as well as 17 known compounds (4-20). The structures of these compounds were elucidated based on chemical and spectral evidence. The stereoc...

journal_title：Chemical & pharmaceutical bulletin

authors： Sagara T,Sugimoto S,Yamano Y,Nehira T,Masuda K,Otsuka H,Matsunami K

更新日期：2021-01-01 00:00:00

abstract：:The purpose of this study was to elucidate the effect of high-temperature storage on the stability of ranitidine, specifically with respect to the potential formation of N-nitrosodimethylamine (NDMA), which is classified as a probable human carcinogen. Commercially available ranitidine reagent powders and formulations...

journal_title：Chemical & pharmaceutical bulletin

authors： Abe Y,Yamamoto E,Yoshida H,Usui A,Tomita N,Kanno H,Masada S,Yokoo H,Tsuji G,Uchiyama N,Hakamatsuka T,Demizu Y,Izutsu KI,Goda Y,Okuda H

更新日期：2020-10-01 00:00:00

abstract：:This study demonstrates the structure-activity relationship of Col-003, a potent collagen-heat-shock protein 47 (Hsp47) interaction inhibitor. Col-003 analogues were successfully synthesized by Pd(0)-catalyzed cross-coupling reactions of 5-bromosalicylaldehyde derivatives with alkyl-metal species, and the inhibitory a...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshida M,Saito M,Ito S,Ogawa K,Goshima N,Nagata K,Doi T

更新日期：2020-03-01 00:00:00

abstract：:Oiling-out is a unique phenomenon that the liquid phase is separated into two parts during crystallization. The emergence of new liquid phase changes the environment where crystals nucleate and grow, we call "mother phase," because target material and impurities become distributed to each phase according to their own ...

journal_title：Chemical & pharmaceutical bulletin

authors： Tanaka K,Takiyama H

更新日期：2020-01-01 00:00:00

abstract：:In line with the recent globalization of the drug supply chain and promotion of the use of generic drugs worldwide, quality assurance is required for drugs globally. In particular, controlling impurities is one of the biggest areas of interest regarding pharmaceutical quality, and it is desirable that the latest scien...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsuhama M,Saito R,Miyazaki S

更新日期：2020-01-01 00:00:00

abstract：:Zerumbone is a multifunctional compound which shows various biological activities, such as antitumor activity, anti-inflammatory activity, antiulcer activity, etc. However, to use Zerumbone as functional foods or medicines, its pharmaceutical properties such as solubility should be improved. In the present study, we p...

journal_title：Chemical & pharmaceutical bulletin

authors： Hassan MM,Mohammed AFA,Elamin KM,Devkota HP,Ohno Y,Motoyama K,Higashi T,Imai T

更新日期：2020-01-01 00:00:00

abstract：:Diphenhydramine, a sedating antihistamine, is an agonist of human bitter taste receptor 14 (hTAS2R14). Diphenhydramine hydrochloride (DPH) was used as a model bitter medicine to evaluate whether the umami dipeptides (Glu-Glu and Asp-Asp) and their constituent amino acids (Glu, Asp) could suppress its bitterness intens...

journal_title：Chemical & pharmaceutical bulletin

authors： Okuno T,Morimoto S,Nishikawa H,Haraguchi T,Kojima H,Tsujino H,Arisawa M,Yamashita T,Nishikawa J,Yoshida M,Habara M,Ikezaki H,Uchida T

更新日期：2020-01-01 00:00:00

abstract：:Enzymatic and post-translational modifications (PTMs) such as ubiquitination, acetylation, and methylation occur at lysine residues. The PTMs play critical roles in the regulation of the protein functions, and thus, various cellular processes. In addition, aberrations of the PTMs are associated with various diseases, ...

journal_title：Chemical & pharmaceutical bulletin

authors： Itoh Y

更新日期：2020-01-01 00:00:00

abstract：:Polycomb repressive complex 2 (PRC2) is an attractive drug target for anti-cancer treatment. Among the three core subunits (EZH2, EED and SUZ12) of PRC2, EZH2 is the catalytic subunit that methylates histone H3 lysine 27 (H3K27), while EED is the regulatory subunit. Besides the small-molecule inhibitors of EZH2, those...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhu K,Du D,Yang R,Tao H,Zhang H

更新日期：2020-01-01 00:00:00

abstract：:α,β-Unsaturated amides were incorporated as viable dipolarophiles in a catalytic asymmetric 1,3-dipolar cycloaddition of azomethine imines. The use of a 7-azaindoline auxiliary was essential to acquire sufficient reactivity with excellent diastereoselectivity, likely due to the chelating activation of the amide by the...

journal_title：Chemical & pharmaceutical bulletin

authors： Li Z,Kumagai N,Shibasaki M

更新日期：2020-01-01 00:00:00

abstract：:Recently, owing to their pharmaceutical and clinical utility, mini-tablets have been well studied by researchers. Mini-tablets are usually manufactured by compression molding using a multiple-tip tool in a rotary tableting machine. Owing to their special structure, ensuring uniformity is a very important challenge in ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kurashima H,Uchida S,Kashiwagura Y,Tanaka S,Namiki N

更新日期：2020-01-01 00:00:00

abstract：:The aim of this study was to evaluate the effects of Magnolin (MGL) on inhibition of human breast cancer cells, and explore the underlying molecular mechanisms. The viability of the treated cells was assessed with the Cell Counting Kit-8 (CCK-8) assay, and the proliferation was analyzed in terms of EdU uptake, colony ...

journal_title：Chemical & pharmaceutical bulletin

authors： Wang J,Zhang S,Huang K,Shi L,Zhang Q

更新日期：2020-01-01 00:00:00

abstract：:C1q/tumor necrosis factor (TNF)-related protein 12 (CTRP12) is a secretory protein that participates in the regulation of glucose and lipid metabolism in obesity and diabetes. Its role in cardiovascular disease, particularly sepsis-induced cardiac injury, is unclear. Here, we stimulated cardiomyocytes with lipopolysac...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhou MQ,Jin E,Wu J,Ren F,Yang YZ,Duan DD

更新日期：2020-01-01 00:00:00

abstract：:The discovery of a novel class of state-dependent voltage-gated sodium channel (NaV)1.7 inhibitors is described. By the modification of amide or urethane bond in NaV1.7 blocker III, structure-activity relationship studies that led to the identification of novel NaV1.7 inhibitor 2i (DS01171986) were performed. Compound...

journal_title：Chemical & pharmaceutical bulletin

authors： Tanaka K,Kobayashi H,Suzuki S,Shibuya S,Kimoto H,Domon Y,Kubota K,Kitano Y,Yokoyama T,Shimizugawa A,Koishi R,Fujiwara C,Asano D,Shinozuka T

更新日期：2020-01-01 00:00:00

abstract：:Herba Cistanche, known as Rou Cong Rong in Chinese, is a very valuable Chinese herbal medicine that has been recorded in the Chinese Pharmacopoeia. Rou Cong Rong has been extensively used in clinical practice in traditional herbal formulations and has also been widely used as a health food supplement for a long time i...

journal_title：Chemical & pharmaceutical bulletin

authors： Lei H,Wang X,Zhang Y,Cheng T,Mi R,Xu X,Zu X,Zhang W

更新日期：2020-01-01 00:00:00

abstract：:Hydrophobically modified hydroxypropyl methylcellulose (HM-HPMC), a polymer in which a small amount of HPMC is stearoxyl substituted, was used as an emulsifier of emulsion-type lotion. A high-pressure homogenizer (microfluidizer) was used. The viscosity of the 1% HM-HPMC aqueous gel decreased after passing through the...

journal_title：Chemical & pharmaceutical bulletin

authors： Fujii M,Wada F,Honda N,Miura K,Hashizaki K,Taguchi H,Koizumi N,Watanabe Y

更新日期：2020-01-01 00:00:00

abstract：:Tranilast, a lipophilic drug with various ophthalmic applications, was used as a model drug to establish the possibility of delivering lipophilic drugs through the eyelid skin. Pharmacokinetics and tissue distribution studies were conducted employing three application methods (topical application onto eyelid skin, eye...

journal_title：Chemical & pharmaceutical bulletin

authors： See GL,Arce F Jr,Itakura S,Todo H,Sugibayashi K

更新日期：2020-01-01 00:00:00

abstract：:We have developed a catalytic aerobic oxidative dimerization reaction of benzofuranones using a Pd(II)-µ-hydroxo complex. Radical-radical cross-coupling of the resulting dimers with azo compounds enabled the one-pot synthesis of structurally congested benzofuranones having two distinct vicinal all-carbon quaternary ce...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohnishi R,Sugawara M,Ezawa T,Sohtome Y,Sodeoka M

更新日期：2020-01-01 00:00:00

abstract：:The tumor microenvironment is considered as one of the important targets for anticancer drug discovery. In particular, nutrient deficiency may be observed in tumor microenvironment; biakamides A-D (1-4) isolated from marine sponge Petrosaspongia sp. as growth inhibitors against cancer cells adapted to glucose-deprived...

journal_title：Chemical & pharmaceutical bulletin

authors： Ishida R,Matsumoto H,Ichii S,Kobayashi M,Arai M,Kotoku N

更新日期：2019-03-01 00:00:00

abstract：:Targeted protein degradation by small molecules is an emerging modality with significant potential for drug discovery. We previously developed chimeric molecules, termed specific and non-genetic inhibitor of apoptosis protein (IAP)-dependent protein erasers (SNIPERs), which induce the ubiquitylation and proteasomal de...

journal_title：Chemical & pharmaceutical bulletin

authors： Ohoka N,Ujikawa O,Shimokawa K,Sameshima T,Shibata N,Hattori T,Nara H,Cho N,Naito M

更新日期：2019-03-01 00:00:00

abstract：:Mutant activin receptor-like kinase-2 (ALK2) was reported to be closely associated with the pathogenesis of fibrodysplasia ossificans progressiva (FOP) and diffuse intrinsic pontine glioma (DIPG), and therefore presents an attractive target for therapeutic intervention. Through in silico virtual screenings and structu...

journal_title：Chemical & pharmaceutical bulletin

authors： Sekimata K,Sato T,Sakai N,Watanabe H,Mishima-Tsumagari C,Taguri T,Matsumoto T,Fujii Y,Handa N,Honma T,Tanaka A,Shirouzu M,Yokoyama S,Miyazono K,Hashizume Y,Koyama H

更新日期：2019-01-01 00:00:00

abstract：:Helicobacter pylori (H. pylori) infection is common and can result in gastric and duodenal ulcers, and in some cases, gastric lymphoma and cancer. Omeprazole (OMP)-in combination with clarithromycin (CLR), amoxicillin (AMX), tinidazole (TND), or metronidazole (MET)-is used in double or triple combination therapy for e...

journal_title：Chemical & pharmaceutical bulletin

authors： Attia TZ,Yamashita T,Tsujino H,Derayea SM,Tsutsumi Y,Uno T

更新日期：2019-01-01 00:00:00

abstract：:Orally disintegrating tablets (ODTs), which are administered without water, are beneficial for elderly patients and patients with dysphagia. Masking the unpleasant taste of a drug is an important factor associated with adherence of patients consuming ODTs. We prepared cocoa powder-containing ODTs of bitter-tasting reb...

journal_title：Chemical & pharmaceutical bulletin

authors： Takano H,Uchida S,Kashiwagura Y,Tanaka S,Hakamata A,Odagiri K,Inui N,Watanabe H,Namiki N

更新日期：2019-01-01 00:00:00

abstract：:Solifenacin (Sol), an antimuscarinic agent has been widely used for the treatment of overactive bladder. Transdermal formulations can be administered without water as well as absorbed slowly into the blood over a long period of time. The aim of this study was to develop cream and tape formulations of Sol, and evaluate...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshida M,Uchida S,Kashiwagura Y,Tanaka S,Matsui R,Namiki N

更新日期：2019-01-01 00:00:00

abstract：:We studied the possibility of using ursodeoxycholic acid (UDCA) as an excipient to create an amorphous composite that can be administered to animals in preclinical studies of experimental drugs. Three UDCA-based amorphous samples composed of nifedipine (NIF), indomethacin (IND), and naproxen (NAP) were found by screen...

journal_title：Chemical & pharmaceutical bulletin

authors： Tanida S,Yoshimoto A,Yoshida M,Uchiyama H,Kadota K,Tozuka Y

更新日期：2019-01-01 00:00:00

abstract：:The Michael reaction of malonates with maleates afforded the corresponding adducts in high yields with high enantioselectivities (up to 98% enantiomeric excess (ee)) by using dilithium 3,3'-dichlorobinaphtholate as a catalyst. The obtained Michael adducts could be converted to optically active tricarboxylic acid (TCA)...

journal_title：Chemical & pharmaceutical bulletin

authors： Sakamoto M,Kaneko T,Orito Y,Shimoda Y,Nakajima M

更新日期：2019-01-01 00:00:00

abstract：:A series of 8-methoxy or 8-methylquinolones bearing novel 3-aminooctahydrocyclopenta[c]pyrrole derivatives at the C-7 position was synthesized, and the pharmacological, physicochemical, and toxicological properties of the individual compounds were evaluated. Novel 8-methylquinolone 7, which includes a 3-amino-7-fluoro...

journal_title：Chemical & pharmaceutical bulletin

authors： Komoriya S,Odagiri T,Inagaki H,Nagamochi M,Miyauchi R,Yoshida KI,Kitamura T,Takahashi H

更新日期：2019-01-01 00:00:00

abstract：:Licorice is one of the ancient and most frequently applied herbs for its diverse phytochemicals. At present, wild resources of licorice have rapidly declined with increasing demand and the proportion of cultivated products in the market is quickly growing. However, the different level in chemical composition between t...

journal_title：Chemical & pharmaceutical bulletin

authors： Wang C,Cai Z,Shi J,Chen S,Tan M,Chen J,Chen L,Zou L,Chen C,Liu Z,Liu X

更新日期：2019-01-01 00:00:00

abstract：:Diabetic embryopathy is a diabetic complication, in which maternal hyperglycemia in early pregnancy causes birth defects in newborn infants. Under maternal diabetic conditions, hyperglycemia disturbs intracellular molecular activities and organelles functions. These include protein misfolding in the endoplasmic reticu...

journal_title：Chemical & pharmaceutical bulletin

authors： Han L,Jiang Z,Zheng X,Qiu J,Hu Y,Li X

更新日期：2019-01-01 00:00:00

abstract：:We report a three-dimensional quantitative structure-activity relationship (3D-QSAR) analysis of CDK2 inhibitors using fragment molecular orbital (FMO) calculations and partial least squares (PLS) regression. In our analysis, fragment binding energies of individual amino acids and fragment binding energy of a single l...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshida T,Hirono S

更新日期：2019-01-01 00:00:00

abstract：:Recently, active pharmaceutical ingredients (APIs) have been dramatically expanding from low-molecular weight drugs to peptides, proteins, antibodies, genes, oligonucleotides, cells, and machines. Therefore to develop pharmaceutical technologies and drug delivery systems (DDS) for these APIs, advanced molecules and no...

journal_title：Chemical & pharmaceutical bulletin

authors： Higashi T

更新日期：2019-01-01 00:00:00

abstract：:Dissolution kinetics of a bilayer direct compress tablet was evaluated by using degassing cyclic flow UV-visible (Vis) spectroscopy with chemometrics. The model bilayer nicotinamide (NA)-pyridoxine hydrochloride (PH) 100.0 mg tablets were prepared via the dual compress method. The fast diffusion layer of the bilayer t...

journal_title：Chemical & pharmaceutical bulletin

authors： Otsuka Y,Ito A,Takahashi T,Matsumura S,Takeuchi M,Tanaka H

更新日期：2019-01-01 00:00:00

abstract：:The 1-BuOH-soluble fraction of the methanol (MeOH) extract of Diospyros maritima was separated by chromatographic techniques to give three new oleanane-type and one new ursane-type triterpene glucoside, named ebenamariosides A-D (1-4); two megastigmanes were also isolated. The structures of triterpene glucosides was e...

journal_title：Chemical & pharmaceutical bulletin

authors： Kawakami S,Miura E,Nobe A,Inagaki M,Nishimura M,Matsunami K,Otsuka H,Aramoto M

更新日期：2019-01-01 00:00:00

abstract：:Among the muscarinic acetylcholine receptor (mAChR) subtypes, the M4 receptor has been investigated as a promising drug target for the treatment of schizophrenia. These investigations have been based on findings from M4-deficient mice studies as well as on the results of a clinical trial that used xanomeline, an M1/M4...

journal_title：Chemical & pharmaceutical bulletin

authors： Takai K,Enomoto T

更新日期：2018-01-01 00:00:00

abstract：:When 8-bromoadenosine was incubated with cysteine at pH 7.2 and 37°C, an exclusive product was generated. This product was identified as a cysteine substitution derivative of adenosine at the 8 position, 8-S-L-cysteinyladenosine. The reaction accelerated as pH increased from mildly acidic to basic conditions. The isol...

journal_title：Chemical & pharmaceutical bulletin

authors： Suzuki T,Ogishi A,Shinohara T,Suito S

更新日期：2018-01-01 00:00:00

abstract：:The admixture of a steroid ointment and a moisturizing cream is frequently prescribed to patients suffering from atopic dermatitis. For the mixing operation, a revolution/rotation-type hybrid mixer is widely used in pharmacy. The purpose of this study was to monitor the mixed state of the admixtures during the mixing ...

journal_title：Chemical & pharmaceutical bulletin

authors： Yokokawa M,Setoyama H,Okada K,Hayashi Y,Machida Y,Onuki Y,Obata Y

更新日期：2018-01-01 00:00:00

abstract：:We developed a rapid and efficient analytical technique for cyclosporine A using HPLC on a column packed with 2-µm nonporous octadecylsilyl silica particles. Under optimized conditions, cyclosporine A was separated with high resolution from other cyclic peptides within 3 min, because the mass transfer resistance in th...

journal_title：Chemical & pharmaceutical bulletin

authors： Sakai-Kato K,Nanjo K,Goda Y

更新日期：2018-01-01 00:00:00

abstract：:Asymmetric epoxidation reactions of chalcone derivatives catalyzed by chiral calcium complexes using hydrogen peroxide were developed. The epoxidation reactions proceeded smoothly to afford the desired products in good yields with good enantioselectivities. This is the first example of chiral calcium-catalyzed asymmet...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamashita Y,Macor JA,Fushimi S,Tsubogo T,Kobayashi S

更新日期：2018-01-01 00:00:00

abstract：:Ginsenoside Rb1 is an important saponin of ginseng(s); however, Rb1, with 3-O- and 20-O-sugar moieties, has low bioavailability. Here, we report the derivatization of ginsenoside Rb1 to completely generate six types of highly bioactive minor ginsenoside Rg3 and its derivatives by FeCl3 catalysis, the reaction conditio...

journal_title：Chemical & pharmaceutical bulletin

authors： Yu H,Wang Y,Liu C,Yang J,Xu L,Li G,Song J,Jin F

更新日期：2018-01-01 00:00:00

abstract：:A vaginal suppository containing ulinastatin (UTI) was developed as a hospital pharmacy product from UTI injection solution and Witepsol® S-55. After mixing at 50°C for 0-8 h, UTI suppositories were prepared, which had good UTI content uniformity. Because 2% surfactant was contained in S-55, the UTI injection solution...

journal_title：Chemical & pharmaceutical bulletin

authors： Kishino T,Inoue Y,Inoue K,Saito K,Kondo M,Otsuka K,Terukina T,Hattori Y,Otsuka M

更新日期：2018-01-01 00:00:00