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Effect of Ag and Ni-Doped Cerium Oxide Nanoparticles on the Formation of ROS and Evaluation as an Alternative Physical Sunscreen Material
Chem Pharm Bull (Tokyo). 2024;72(2):220-225. doi: 10.1248/cpb.c23-00512.ABSTRACTCeO2 nanoparticles (nanoceria) were proposed as an alternative physical sunscreen agent with antioxidant properties and comparable UV absorption performance. Green synthesis of nanoceria with Ag and Ni dopants resulted in doped nanoceria with lower catalytic activity and biologically-safe characteristics. The doped nanoceria was characterized using X-ray diffraction (XRD), transmission electron microscopy (TEM), Rancimat Instrument, and UV-Vis Spectrophotometer for SPF (Sun Protection Factor) determination. XRD and TEM analysis showed that nano...
Source: Chemical and Pharmaceutical Bulletin - February 21, 2024 Category: Drugs & Pharmacology Authors: Agnes Giovanni Marsius Satria Hidayat Damar Rastri Adhika Akhmad Zein Eko Mustofa Veinardi Suendo Heni Rachmawati Source Type: research

Antiproliferative Activities of Cynaropicrin and Related Compounds against Cancer Stem Cells
In this study, we evaluated the antiproliferative activities of 21 sesquiterpenoids against human GBM U-251 MG CSCs and U-251 MG non-CSCs. Particularly, the guaianolide sesquiterpene lactone cynaropicrin (1) showed strong antiproliferative activity against U-251 MG CSCs (IC50 = 20.4 µM) and U-251 MG non-CSCs (IC50 = 10.9 µM). Accordingly, we synthesized six derivatives of 1 and investigated their structure-activity relationships. Most of the guaianolide sesquiterpene lactones with the α-methylene-γ-butyrolactone moiety showed antiproliferative activities against U-251 MG cells. We conclude that the 5,7,5-ring and the �...
Source: Chemical and Pharmaceutical Bulletin - February 21, 2024 Category: Drugs & Pharmacology Authors: Kousuke Araki Minami Hara Shohei Hamada Takahiro Matsumoto Seikou Nakamura Source Type: research

Nucleophilic Deprotection of p-Methoxybenzyl Ethers Using Heterogeneous Oxovanadium Catalyst
Chem Pharm Bull (Tokyo). 2024;72(2):213-219. doi: 10.1248/cpb.c23-00897.ABSTRACTNucleophilic deprotection of p-methoxybenzyl (PMB) [p-methoxyphenylmethyl (MPM)] ethers was developed using a heterogeneous oxovanadium catalyst V-MPS4 and a thiol nucleophile. The deprotection method had a wide reaction scope, including PMB ethers of primary, secondary, and tertiary alcohols bearing various functional groups. In addition, the PMB ether of an oxidation-labile natural product was successfully removed by V-MPS4 catalysis, while a common oxidative method of PMB deprotection afforded a complex mixture. The V-MPS4 catalyst was reusa...
Source: Chemical and Pharmaceutical Bulletin - February 21, 2024 Category: Drugs & Pharmacology Authors: Rei Ikeda Tomoya Nishio Kyohei Kanomata Shuji Akai Source Type: research

Improved Dissolution Properties of Co-amorphous Probucol with Atorvastatin Calcium Trihydrate Prepared by Spray-Drying
Chem Pharm Bull (Tokyo). 2024;72(2):190-199. doi: 10.1248/cpb.c23-00673.ABSTRACTA co-amorphous model drug was prepared by the spray-drying (SD) of probucol (PC) and atorvastatin calcium trihydrate salt (ATO) as low water solubility and co-former components, respectively. The physicochemical properties of the prepared samples were characterized by powder X-ray diffraction (PXRD) analysis, thermal analysis, Fourier transform infrared spectroscopy (FTIR), and dissolution tests. Stability tests were also conducted under a stress environment of 40 °C and 75% relative humidity. The results of PXRD measurements and thermal analy...
Source: Chemical and Pharmaceutical Bulletin - February 18, 2024 Category: Drugs & Pharmacology Authors: Shinji Oyama Noriko Ogawa Kaori Kawai Kanako Iwai Toshiya Yasunaga Hiromitsu Yamamoto Source Type: research

Sulfonate Derivatives Containing a Kakuol Moiety as Potential Fungicidal Candidates: Design, Synthesis and Antifungal Activity Evaluation
Chem Pharm Bull (Tokyo). 2024;72(2):186-189. doi: 10.1248/cpb.c23-00857.ABSTRACTAs a part of our continuing exploration to discover new potential promising fungicide candidates, eighteen sulfonate derivatives (3a-3r) containing a kakuol moiety were designed and synthesized. Synthetic sulfonate derivatives were tested comprehensively for antifungal activities against four plant pathogenic fungi (Botrytis (B.) cinerea, Valsa (V.) mali, Fusarium (F.) graminearum, Sclerotinia (S.) sclerotiorum), and their structure activity relationships were summarized. Especially, derivatives 3i and 3j exhibited remarkable activity against V...
Source: Chemical and Pharmaceutical Bulletin - February 12, 2024 Category: Drugs & Pharmacology Authors: Guoqing Sui Lili Shu Ailing Zhang Dan Li Shuhua Cao Source Type: research

Protective mechanisms of Juncus effusus and Carbonized Juncus effusus against d-galactosamine-induced acute liver injury in mice
This study investigated the hepatoprotective effects of Juncus effusus (J. effusus) and Carbonized J. effusus against liver injury caused by D-galactosamine (D-GalN) in mice. J. effusus and Carbonized J. effusus were administered by gavage once daily starting seven days before the D-GalN treatment. The results of the study indicated that J. effusus and Carbonized J. effusus suppressed the D-GalN-induced generation of serum alanine transaminase (ALT), aspartate aminotransferase (AST), hepatic malondialdehyde (MDA) and tumor necrosis factor-alpha (TNF-α) was observed. The values of superoxide dismutase (SOD) exhibited an in...
Source: Chemical and Pharmaceutical Bulletin - February 7, 2024 Category: Drugs & Pharmacology Authors: Xiangming Wang Menghui Zhao Chengguo Ju Hui Gao Wei Wang Source Type: research

Total Synthesis of Marine Polyketide Plakortone Q
Chem Pharm Bull (Tokyo). 2024;72(2):179-185. doi: 10.1248/cpb.c23-00876.ABSTRACTThe total synthesis of the natural bicyclo[3.3.0]furanolactone polyketide, plakortone Q, was achieved in 24 steps from (R)-Roche ester. The main feature of this synthetic strategy is the stereoselective construction of a central tetrahydrofuran moiety with four consecutive stereoisomeric centers using the Upjohn dihydroxylation of oxiranyl-substituted alkenes and acid-mediated 5-endo-tet cyclization.PMID:38311392 | DOI:10.1248/cpb.c23-00876 (Source: Chemical and Pharmaceutical Bulletin)
Source: Chemical and Pharmaceutical Bulletin - February 4, 2024 Category: Drugs & Pharmacology Authors: Shinnosuke Okazaki Kaho Senda Ayaka Tokuta Misa Inagaki Kazuo Kamaike Koichiro Ota Hiroaki Miyaoka Source Type: research

Near-Infrared Fluorescent Silica Nanoparticles Based on Gold-Silver Alloy Nanoclusters for Clinical Diagnosis
In this study, we developed fluorescent silica nanoparticles using gold-silver alloy nanoclusters and chitosan (CS) (NH2-SiO2@Au@CS@AuAg) by the layer-by-layer method. Under UV-light irradiation at 365 nm, the emission wavelength of NH2-SiO2@Au@CS@AuAg reached 750 nm in the near-IR region. Scanning electron microscopy images revealed that the shape of NH2-SiO2@Au@CS@AuAg was uniform and spherical. The fluorescence spectrum of horse blood obtained in the presence of NH2-SiO2@Au@CS@AuAg contained a specific fluorescence peak attributed to NH2-SiO2@Au@CS@AuAg, which was distinguishable from the autofluorescence peaks. These r...
Source: Chemical and Pharmaceutical Bulletin - January 31, 2024 Category: Drugs & Pharmacology Authors: Hiroaki Ichimaru Shigetoshi Kikuchi Source Type: research

Design, Synthesis, and Biological Evaluation of Water-Soluble Prodrugs of C5-Curcuminoid GO-Y030 Based on Reversible Thia-Michael Reaction
This study describes the development of water-soluble prodrugs of GO-Y030, a potent antitumor C5-curcuminoid, in an attempt to enhance its bioavailability. These prodrugs release the parent compound via a retro-thia-Michael reaction. To endow sufficient hydrophilicity onto GO-Y030 via a single thia-Michael reaction of an aqueous entity, we used a modified glycoconjugate with a thiol group. The water-solubilizing motif was installed on GO-Y030 by the thia-Michael reaction of propargyl-polyethylene glycol (PEG)-thiol and subsequent click chemistry (CuAAC) reaction with 1-glycosyl azide. Turbidity measurements revealed a sign...
Source: Chemical and Pharmaceutical Bulletin - January 31, 2024 Category: Drugs & Pharmacology Authors: Hiroyuki Yamakoshi Michihiro Fukuda Hiro Ikeda Shogo Fujiki Aki Kohyama Shota Nagasawa Hanae Shinozaki Hiroyuki Shibata Yoshiharu Iwabuchi Source Type: research