journal
https://read.qxmd.com/read/38382975/effect-of-ag-and-ni-doped-cerium-oxide-nanoparticles-on-the-formation-of-ros-and-evaluation-as-an-alternative-physical-sunscreen-material
#21
JOURNAL ARTICLE
Agnes Giovanni Marsius, Satria Hidayat, Damar Rastri Adhika, Akhmad Zein Eko Mustofa, Veinardi Suendo, Heni Rachmawati
CeO2 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...
2024: Chemical & Pharmaceutical Bulletin
https://read.qxmd.com/read/38382974/nucleophilic-deprotection-of-p-methoxybenzyl-ethers-using-heterogeneous-oxovanadium-catalyst
#22
JOURNAL ARTICLE
Rei Ikeda, Tomoya Nishio, Kyohei Kanomata, Shuji Akai
Nucleophilic 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...
2024: Chemical & Pharmaceutical Bulletin
https://read.qxmd.com/read/38382968/antiproliferative-activities-of-cynaropicrin-and-related-compounds-against-cancer-stem-cells
#23
JOURNAL ARTICLE
Kousuke Araki, Minami Hara, Shohei Hamada, Takahiro Matsumoto, Seikou Nakamura
Glioblastoma (GBM) has a high mortality rate despite the availability of various cancer treatment options. Although cancer stem cells (CSCs) have been associated with poor prognosis and metastasis, and play an important role in the resistance to existing anticancer drugs and radiation; no CSC-targeting drugs are currently approved in clinical practice. Therefore, the development of antiproliferative agents against CSCs is urgently required. In this study, we evaluated the antiproliferative activities of 21 sesquiterpenoids against human GBM U-251 MG CSCs and U-251 MG non-CSCs...
2024: Chemical & Pharmaceutical Bulletin
https://read.qxmd.com/read/38369345/improved-dissolution-properties-of-co-amorphous-probucol-with-atorvastatin-calcium-trihydrate-prepared-by-spray-drying
#24
JOURNAL ARTICLE
Shinji Oyama, Noriko Ogawa, Kaori Kawai, Kanako Iwai, Toshiya Yasunaga, Hiromitsu Yamamoto
A 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 analysis suggested that PC and ATO form a co-amorphous system by SD...
2024: Chemical & Pharmaceutical Bulletin
https://read.qxmd.com/read/38346722/sulfonate-derivatives-containing-a-kakuol-moiety-as-potential-fungicidal-candidates-design-synthesis-and-antifungal-activity-evaluation
#25
JOURNAL ARTICLE
Guoqing Sui, Lili Shu, Ailing Zhang, Dan Li, Shuhua Cao
As 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...
2024: Chemical & Pharmaceutical Bulletin
https://read.qxmd.com/read/38311392/total-synthesis-of-marine-polyketide-plakortone-q
#26
JOURNAL ARTICLE
Shinnosuke Okazaki, Kaho Senda, Ayaka Tokuta, Misa Inagaki, Kazuo Kamaike, Koichiro Ota, Hiroaki Miyaoka
The 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.
2024: Chemical & Pharmaceutical Bulletin
https://read.qxmd.com/read/38296560/identification-of-a-histone-deacetylase-8-inhibitor-through-drug-screenings-based-on-machine-learning
#27
JOURNAL ARTICLE
Atika Nurani, Yasunobu Yamashita, Yuuki Taki, Yuri Takada, Yukihiro Itoh, Takayoshi Suzuki
Histone deacetylase 8 (HDAC8) is a zinc-dependent HDAC that catalyzes the deacetylation of nonhistone proteins. It is involved in cancer development and HDAC8 inhibitors are promising candidates as anticancer agents. However, most reported HDAC8 inhibitors contain a hydroxamic acid moiety, which often causes mutagenicity. Therefore, we used machine learning for drug screening and attempted to identify non-hydroxamic acids as HDAC8 inhibitors. In this study, we established a prediction model based on the random forest (RF) algorithm for screening HDAC8 inhibitors because it exhibited the best predictive accuracy in the training dataset, including data generated by the synthetic minority over-sampling technique (SMOTE)...
2024: Chemical & Pharmaceutical Bulletin
https://read.qxmd.com/read/38296559/in-silico-prediction-of-n-nitrosamine-formation-pathways-of-pharmaceutical-products
#28
JOURNAL ARTICLE
Genichiro Tsuji, Takashi Kurohara, Takuji Shoda, Hidetomo Yokoo, Takahito Ito, Sayaka Masada, Nahoko Uchiyama, Eiichi Yamamoto, Yosuke Demizu
The recent discovery of N-nitrosodimethylamine (NDMA), a mutagenic N-nitrosamine, in pharmaceuticals has adversely impacted the global supply of relevant pharmaceutical products. Contamination by N-nitrosamines diverts resources and time from research and development or pharmaceutical production, representing a bottleneck in drug development. Therefore, predicting the risk of N-nitrosamine contamination is an important step in preventing pharmaceutical contamination by DNA-reactive impurities for the production of high-quality pharmaceuticals...
2024: Chemical & Pharmaceutical Bulletin
https://read.qxmd.com/read/38296558/allosteric-hsp70-modulator-ym-1-induces-degradation-of-brd4
#29
JOURNAL ARTICLE
Yugo Mishima, Shusuke Tomoshige, Shinichi Sato, Minoru Ishikawa
YM-1, an allosteric modulator of heat-shock 70 kDa protein (Hsp70), inhibits cancer cell growth, but the mechanism is not yet fully understood. Here, we show that YM-1 induces the degradation of bromodomain containing 4 (BRD4), which mediates oncogene expression. Overall, our results indicate that YM-1 promotes the binding of HSP70 to BRD4, and this in turn promotes the ubiquitination of BRD4 by C-terminus of Hsc70-interacting protein (CHIP), an E3 ubiquitin ligase working in concert with Hsp70, leading to proteasomal degradation of BRD4...
2024: Chemical & Pharmaceutical Bulletin
https://read.qxmd.com/read/38296557/a-structure-activity-relationship-study-of-snail1-peptides-as-inhibitors-of-lysine-specific-demethylase-1
#30
JOURNAL ARTICLE
Yuri Takada, Kyohei Adachi, Yuka Fujinaga, Yasunobu Yamashita, Yukihiro Itoh, Takayoshi Suzuki
Peptides have recently garnered attention as middle-molecular-weight drugs with the characteristics of small molecules and macromolecules. Lysine-specific demethylase 1 (LSD1) is a potential therapeutic target for lung cancer, neuroblastoma, and leukemia, and some peptide-based LSD1 inhibitors designed based on the N-terminus of SNAIL1, a member of the SNAIL/SCRATCH family of transcription factors, have been reported. The N-terminus of SNAIL1 peptide acts as a cap of the catalytic site of LSD1, inhibiting interactions with LSD1...
2024: Chemical & Pharmaceutical Bulletin
https://read.qxmd.com/read/38296556/rational-design-of-amphipathic-antimicrobial-peptides-with-alternating-l-d-amino-acids-that-form-helical-structures
#31
JOURNAL ARTICLE
Motoharu Hirano, Hidetomo Yokoo, Nobumichi Ohoka, Takahito Ito, Takashi Misawa, Makoto Oba, Takao Inoue, Yosuke Demizu
Antimicrobial peptides (AMPs) are promising therapeutic agents against bacteria. We have previously reported an amphipathic AMP Stripe composed of cationic L-Lys and hydrophobic L-Leu/L-Ala residues, and Stripe exhibited potent antimicrobial activity against Gram-positive and Gram-negative bacteria. Gramicidin A (GA), composed of repeating sequences of L- and D-amino acids, has a unique β6.3 -helix structure and exhibits broad antimicrobial activity. Inspired by the structural properties and antimicrobial activities of LD-alternating peptides such as GA, in this study, we designed Stripe derivatives with LD-alternating sequences...
2024: Chemical & Pharmaceutical Bulletin
https://read.qxmd.com/read/38296555/synthesis-of-coumarin-conjugated-oligonucleotides-via-knoevenagel-condensation-to-prepare-an-oligonucleotide-library
#32
JOURNAL ARTICLE
Takashi Osawa, Satoshi Obika
DNA-encoded libraries (DELs) are attracting attention as a screening tool in the early stages of drug discovery. In the development of DELs, drug candidate compounds are chemically synthesized on barcode DNA. Therefore, it is important to perform the synthesis under mild conditions so as to not damage the DNA. On the other hand, coumarins are gaining increasing research focus not only because they possess excellent fluorescence properties, but also because many medicines contain a coumarin skeleton. Among the various reactions developed for the synthesis of coumarins thus far, Knoevenagel condensation followed by intramolecular cyclization under mild conditions can yield coumarins...
2024: Chemical & Pharmaceutical Bulletin
https://read.qxmd.com/read/38296554/targeted-therapy-for-prostate-cancer-by-prostate-specific-membrane-antigen-targeted-small-molecule-drug-conjugates
#33
REVIEW
Ryo Nakajima
In the aging global population, prostate cancer is a worldwide health problem because the incidence rate of this disease increases at advanced ages. Although early-stage prostate cancer can be treated by total prostatectomy, the surgery causes side effects, such as incontinence and dysuria, that lower QOL. Once the disease progresses to metastatic castration-resistant prostate cancer (mCRPC), there are no effective chemotherapeutic agents without systematic side effects. Therefore, targeted therapies for mCPRC are urgently needed...
2024: Chemical & Pharmaceutical Bulletin
https://read.qxmd.com/read/38296553/foreword
#34
JOURNAL ARTICLE
Takayoshi Suzuki
No abstract text is available yet for this article.
2024: Chemical & Pharmaceutical Bulletin
https://read.qxmd.com/read/38296515/design-synthesis-and-biological-evaluation-of-water-soluble-prodrugs-of-c5-curcuminoid-go-y030-based-on-reversible-thia-michael-reaction
#35
JOURNAL ARTICLE
Hiroyuki Yamakoshi, Michihiro Fukuda, Hiro Ikeda, Shogo Fujiki, Aki Kohyama, Shota Nagasawa, Hanae Shinozaki, Hiroyuki Shibata, Yoshiharu Iwabuchi
Although curcumin and its analogs exhibit anticancer activity, they are still not used as anticancer drugs because of their water insolubility and extremely poor bioavailability. 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...
2024: Chemical & Pharmaceutical Bulletin
https://read.qxmd.com/read/38296514/near-infrared-fluorescent-silica-nanoparticles-based-on-gold-silver-alloy-nanoclusters-for-clinical-diagnosis
#36
JOURNAL ARTICLE
Hiroaki Ichimaru, Shigetoshi Kikuchi
In clinical diagnosis, fluorescent particles are applied to detect analytes in biofluids, such as blood and saliva. However, current fluorescence detection methods have not been optimized to account for the overlapping autofluorescence peaks of biological substances. Gold and silver nanoclusters are known to the novel fluorescent materials and their emission wavelengths depend on cluster size. 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...
2024: Chemical & Pharmaceutical Bulletin
https://read.qxmd.com/read/38267058/synthesis-and-biological-evaluation-of-2-azolylmethylene-3-2h-benzofuranone-derivatives-as-potent-monoamine-oxidases-inhibitors
#37
JOURNAL ARTICLE
Koichi Takao, Yuka Kubota, Kota Kurosaki, Hitoshi Kamauchi, Yoshihiro Uesawa, Yoshiaki Sugita
A series of 2-azolylmethylene-3-(2H)-benzofuranone derivatives, 2-indolylmethylene-3-(2H)-benzofuranone and 2-pyrrolylmethylene-3-(2H)-benzofuranone derivatives, were synthesized, and their monoamine oxidase (MAO) A and B inhibitory activities were evaluated. Compounds 1b, 3b, 6b, 7b, and 10b showed strong inhibitory activity against MAO-A, and compound 3b showed the highest potency and selectivity, with an IC50 value of 21 nM and a MAO-A selectivity index of 48. Compounds 3c, 4c, 9a, 9c, 10c, 11a, and 11c showed strong inhibitory activity against MAO-B, and compound 4c showed the highest potency and selectivity, with an IC50 value of 16 nM and a MAO-B selectivity index of >1100...
2024: Chemical & Pharmaceutical Bulletin
https://read.qxmd.com/read/38233138/a-tricyclic-aromatic-polyketide-isolated-from-the-marine-derived-fungus-curvularia-aeria
#38
JOURNAL ARTICLE
Hitoshi Kamauchi, Mayu Tanaka, Mitsuaki Suzuki, Miho Furukawa, Atsushi Ikeda, Chihiro Sasho, Yuka Kiba, Masashi Kitamura, Koichi Takao, Yoshiaki Sugita
A novel tricyclic polyketide, curvulanone (1), was isolated from the marine-derived fungus Curvularia aeria. The structure of 1 was determined by NMR and single-crystal X-ray crystallography. 1 had a cyclopentabenzopyranone with 3-acetic acid structure that is rarely found in natural compounds. Monoamine oxidase and sirtuin 1 inhibitory test was exhibited and 1 showed their inhibitory activity.
2024: Chemical & Pharmaceutical Bulletin
https://read.qxmd.com/read/38233137/chromatographic-evaluation-and-characterization-of-constituents-of-sunflower-seed-extract-used-as-food-additives
#39
JOURNAL ARTICLE
Yoshiaki Amakura, Takashi Uchikura, Morio Yoshimura, Naoko Masumoto, Yuzo Nishizaki, Naoki Sugimoto
Sunflower seed extract, an antioxidant agent registered on the List of Existing Food Additives in Japan, was evaluated using HPLC, and three common constituents were detected. These peaks were identified as monocaffeoylquinic acids (3-O-caffeoylquinic acid, 4-O-caffeoylquinic acid, and 5-O-caffeoylquinic acid [chlorogenic acid]). Upon scrutinizing other components, dicaffeoylquinic acids (isochlorogenic acids; 3,4-di-O-caffeoylquinic, 3,5-di-O-caffeoylquinic, and 4,5-di-O-caffeoylquinic acids) were also identified...
2024: Chemical & Pharmaceutical Bulletin
https://read.qxmd.com/read/38233136/derivation-of-the-extended-kawakita-equation-for-estimating-the-yield-state-of-powder-in-die
#40
JOURNAL ARTICLE
Tsubasa Sato, Naoto Morita, Etsuo Yonemochi, Kozo Takayama
For powder compaction, the Kawakita equation has been used to estimate the powder behavior inside the die. The compression pressure exerted on powders is not homogeneous because of the friction on the die wall. However, the yield pressure and porosity estimated using the Kawakita equation are defined based on the assumption that homogeneous voids and compression pressure are distributed throughout the powder bed. In this study, an extended Kawakita equation was derived by considering the variation in the compression pressure as it corresponds to the distance from the loading punch surface...
2024: Chemical & Pharmaceutical Bulletin
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