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Effect of Powdered Cellulose Nanofiber with Different Particle Sizes on the Physical Properties of Tablets Manufactured via Direct Compression
Chem Pharm Bull (Tokyo). 2023;71(12):887-896. doi: 10.1248/cpb.c23-00587.ABSTRACTDirect compression is a tableting technique that involves a few steps in non-demanding manufacturing conditions. High strength and rapid disintegration of tablet formulations were previously achieved through the addition of cellulose nanofibers (CNFs), which have recently attracted attention as a high-performance biomass material. However, CNF addition results in greater variation in tablet weight and drug content, potentially due to differences in particle size between CNF and other additives. Herein, we used pulverized CNF to evaluate the ef...
Source: Chemical and Pharmaceutical Bulletin - December 3, 2023 Category: Drugs & Pharmacology Authors: Shohei Nakamura Mai Jinno Momoka Hamaoka Ayumi Sakurada Takatoshi Sakamoto Source Type: research

In Silico Identification of Inhibitory Compounds for SARS-Cov-2 Papain-Like Protease
Chem Pharm Bull (Tokyo). 2023;71(12):897-905. doi: 10.1248/cpb.c23-00622.ABSTRACTVirtual screening with high-performance computers is a powerful and cost-effective technique in drug discovery. A chemical database is searched to find candidate compounds firmly bound to a target protein, judging from the binding poses and/or binding scores. The severe acute respiratory syndrome coronavirus 2 (SARS-Cov-2) infectious disease has spread worldwide for the last three years, causing severe slumps in economic and social activities. SARS-Cov-2 has two viral proteases: 3-chymotrypsin-like (3CL) and papain-like (PL) protease. While ap...
Source: Chemical and Pharmaceutical Bulletin - December 3, 2023 Category: Drugs & Pharmacology Authors: Kazunori Miwa Yan Guo Masayuki Hata Yoshinori Hirano Norio Yamamoto Tyuji Hoshino Source Type: research

Palatability Evaluation of Sulfamethoxazole/Trimethoprim with Sweetener Using the Two-Bottle Choice Test
In this study, a new two-bottle choice test was performed in rats to evaluate bitterness masking and determine the drug-to-sweetener ratio that significantly improves palatability. Sulfamethoxazole and trimethoprim were used as model bitter drugs, and sucralose was used as sweetener. The addition of sucralose and trimethoprim at a 0.13 : 1 ratio resulted in the greatest improvement in preference. This method is a useful new technique for evaluating the palatability of drug formulations.PMID:38044143 | DOI:10.1248/cpb.c23-00428 (Source: Chemical and Pharmaceutical Bulletin)
Source: Chemical and Pharmaceutical Bulletin - December 3, 2023 Category: Drugs & Pharmacology Authors: Haruka Shinotsuka Naoya Mizutani Shohei Aikawa Go Kimura Source Type: research

Porcine Acellular Dermal Matrix Promotes Migration and Suppresses Inflammation of Keratinocytes by Mediating the AKT Signaling Pathway
In conclusion, pADM promotes cell migration and inhibits inflammation by activating the AKT pathway under oxidative stress. These findings support the use of pADM for post-traumatic therapy and reveal a novel underlying mechanism of action.PMID:38044138 | DOI:10.1248/cpb.c23-00379 (Source: Chemical and Pharmaceutical Bulletin)
Source: Chemical and Pharmaceutical Bulletin - December 3, 2023 Category: Drugs & Pharmacology Authors: Xing He Dongmei Li Tianqing Chen Source Type: research

Discovery of Novel Chromenopyridine Derivatives as Readthrough-Inducing Drugs
Chem Pharm Bull (Tokyo). 2023;71(12):859-878. doi: 10.1248/cpb.c23-00488.ABSTRACTHurler syndrome, a type of Mucopolysaccharidosis type I, is an inherited disorder caused by the accumulation of glycosaminoglycans (GAG) due to a deficiency in lysosomal α-L-iduronidase (IDUA), resulting in multiorgan dysfunction. In many patients with Hurler syndrome, IDUA proteins are not produced due to nonsense mutations in their genes; therefore, readthrough-inducing compounds, such as gentamycin, are expected to restore IDUA proteins by skipping the premature termination codon. In the present study, we synthesized a series of chromenopy...
Source: Chemical and Pharmaceutical Bulletin - December 3, 2023 Category: Drugs & Pharmacology Authors: Shota Kawai Shunsuke Takashima Masafumi Ando Sayaka Shintaku Shigemitsu Takeda Kazuya Otake Yuma Ito Masaki Fukui Megumi Yamamoto Yoshimichi Shoji Hiroaki Shirahase Tatsuya Kitao Source Type: research

Exploratory Studies of Effective Inhibitors against the SARS-CoV-2 Main Protease by Halogen Incorporation and Amide Bond Replacement
Chem Pharm Bull (Tokyo). 2023;71(12):879-886. doi: 10.1248/cpb.c23-00562.ABSTRACTIn the development of anti-severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) drugs, its main protease (Mpro), which is an essential enzyme for viral replication, is a promising target. To date, the Mpro inhibitors, nirmatrelvir and ensitrelvir, have been clinically developed by Pfizer Inc. and Shionogi & Co., Ltd., respectively, as orally administrable drugs to treat coronavirus disease of 2019 (COVID-19). We have also developed several potent inhibitors of SARS-CoV-2 Mpro that include compounds 4, 5, TKB245 (6), and TKB248 (7),...
Source: Chemical and Pharmaceutical Bulletin - December 3, 2023 Category: Drugs & Pharmacology Authors: Kohei Tsuji Takuya Kobayakawa Takahiro Ishii Nobuyo Higashi-Kuwata Chika Azuma Kouki Shinohara Yutaro Miura Kenichi Yamamoto Soshi Nishimura Shin-Ichiro Hattori Haydar Bulut Hiroaki Mitsuya Hirokazu Tamamura Source Type: research

Semisynthesis and in Vitro Anti-cancer Effect of New Magnolol Derivatives on the Cell Proliferation, Apoptosis, Migration, and Invasion of Human Hepatocellular Carcinoma SMMC-7721 Cells
Chem Pharm Bull (Tokyo). 2023;71(11):798-803. doi: 10.1248/cpb.c23-00215.ABSTRACTFour new magnolol derivatives were synthesized and evaluated for their in vitro anti-cancer properties. Among these, compound 3 showed the most potent cytotoxic activity against the SMMC-7721, SUN-449, and HepG2 human hepatocellular carcinoma cell lines, with IC50 values of 3.39, 4.11, and 6.88 µM, respectively. Compound 3 also induced apoptosis of SMMC-7721 cells by down-regulating Bcl-2 and Akt protein levels, up-regulating of Bax protein level, and cleaving caspase-9 and -3. In addition, transwell assays showed that compound 3 significantl...
Source: Chemical and Pharmaceutical Bulletin - November 1, 2023 Category: Drugs & Pharmacology Authors: Na-Na He Jian-An Wang Di Huang Xiao-Long Sun Feng Ding Long Zhao Yu-Xin Zhang Hong-Mei Li Cheng-Zhu Wu Source Type: research

Chiral Recognition of Diketopiperazine Containing Proline Residues by (-)-Epigallocatechin-3-O-gallate in Water
Chem Pharm Bull (Tokyo). 2023;71(11):804-811. doi: 10.1248/cpb.c23-00369.ABSTRACTThe stoichiometry and precipitate yield of a complex of (-)-epigallocatechin-3-O-gallate (EGCg) and cyclo(Pro-Xxx) (Xxx = phenylalanine (Phe), tyrosine (Tyr)) were evaluated using integrated values of their proton signals by quantitative 1H-NMR (q NMR). It was determined to be a 1 : 1 complex of EGCg and cyclo(Pro-Xxx). The change in the chemical shift value of proton signals of cyclo(Pro-Xxx) in 1H-NMR spectra by adding standard amounts of EGCg was investigated. Differences in chemical shift values of H8α, H7αβ, H8β, H10, H9, and H3 proto...
Source: Chemical and Pharmaceutical Bulletin - November 1, 2023 Category: Drugs & Pharmacology Authors: Takashi Ishizu Yuka Fujitani Runa Nishio Haruka Kamei Source Type: research

Production of Dihydroisocoumarins by Callus Induction from Hydrangea macrophylla var. thunbergii Leaves
Chem Pharm Bull (Tokyo). 2023;71(11):832-837. doi: 10.1248/cpb.c23-00499.ABSTRACTDihydroisocoumarins, hydrangenol 8-O-β-D-glucopyranoside (1), phyllodulcin 8-O-β-D-glucopyranoside (2), hydrangenol (3), and phyllodulcin (4), are well-known as the major secondary metabolites in the leaves of Hydrangea macrophylla var. thunbergii. Dihydroisocoumarins are pharmaceutical compounds with diverse bioactivity. Although dihydroisocoumarins are commonly isolated from Hydrangea plants or via organic chemical synthesis, their production via callus induction is considered a promising alternative. In the present study, callus induction...
Source: Chemical and Pharmaceutical Bulletin - November 1, 2023 Category: Drugs & Pharmacology Authors: Junko Tsukioka Tomoka Takami Yuki Ario Seikou Nakamura Source Type: research

Determination of the Solid Content of Active Pharmaceutical Ingredient Powders in Suspension-Type Pharmaceutical Oral Jelly Using Time-Domain NMR
This study determined the content of solid active pharmaceutical ingredient (API) powders dispersed in suspension-type pharmaceutical oral jellies using a low-field time-domain NMR (TD-NMR). The suspended jellies containing a designated API content were prepared and tested. Acetaminophen (APAP), indomethacin (IMC) and L-valine were used as test APIs. First, this study measured the T2 relaxation rate (the reciprocal of T2 relaxation time) by the Carr-Purcell-Meiboom-Gill (CPMG) pulse sequence, and then evaluated whether the API content could be determined by the acquired T2 relaxation rate. The T2 relaxation rate negatively...
Source: Chemical and Pharmaceutical Bulletin - November 1, 2023 Category: Drugs & Pharmacology Authors: Ryosuke Kobayashi Takashi Ono Shungo Kumada Kotaro Okada Yoshinori Onuki Source Type: research

Anti-hepatitis C Virus Activity of Juglorubin Derivatives
In this study, the derivatives of juglorubin, 1-O-acetyljuglorubin dimethyl ester and juglorubin dimethyl ester, were found to exhibit antiviral activity against hepatitis C virus (HCV) without exerting any remarkable cytotoxicity against host Huh-7 cells. They also inhibited liver X receptor α activation and lipid droplet accumulation in Huh-7 cells. These findings suggest that 1-O-acetyljuglorubin dimethyl ester and juglorubin dimethyl ester targeted the host factors required for HCV production.PMID:37914261 | DOI:10.1248/cpb.c23-00489 (Source: Chemical and Pharmaceutical Bulletin)
Source: Chemical and Pharmaceutical Bulletin - November 1, 2023 Category: Drugs & Pharmacology Authors: Hirofumi Ohashi Kazane Nishioka Tomoki Kurihara Kou Nakamura Masako Yamasaki Yuuka Ibayashi Kanta Fuchiyama Shogo Kamo Yuuki Furuyama Kenji Ohgane Maiko Okada Shinji Kamisuki Koichi Watashi Kouji Kuramochi Source Type: research