Review
Biochemistry & Molecular Biology
Jia-Yi Dou, Yu-Chen Jiang, Zhen-Yu Cui, Li-Hua Lian, Ji-Xing Nan, Yan-Ling Wu
Summary: Acanthoic acid (AA), isolated from the root bark of Acanthopanax koreanum Nakai, exhibits a wide range of pharmacological activities and targets multiple signaling pathways. Studies have also focused on structural modifications of AA to enhance its pharmacological effects.
Article
Engineering, Chemical
Gabriela Nistor, Alexandra Mioc, Marius Mioc, Mihaela Balan-Porcarasu, Roxana Ghiulai, Roxana Racoviceanu, Stefana Avram, Alexandra Prodea, Alexandra Semenescu, Andreea Milan, Cristina Dehelean, Codruta Soica
Summary: This study investigated the antiproliferative activity of newly developed 1,2,4-triazole derivatives of betulinic acid (BA) in an in vitro environment. The results showed that BA-triazole derivatives 4a and 4b exhibited higher cytotoxicity against the RPMI-7951 cell line compared to their precursors. Further analysis revealed that these compounds induced apoptotic mechanism at the mitochondrial level, inhibited mitochondrial respiration, and affected the expression of apoptosis-related genes.
Article
Infectious Diseases
Andrey Moacir do Rosario Marinho, Claudia Maria S. C. de Oliveira, Joao Victor Silva-Silva, Samara C. Anchieta de Jesus, Jose Edson S. Siqueira, Luana C. de Oliveira, Jessica Fernandes Auzier, Liviane N. Soares, Maria Lucia Belem Pinheiro, Sebastiao C. Silva, Livia S. Medeiros, Emmanoel V. Costa, Patricia S. Barbosa Marinho
Summary: In this study, acanthoic acid (AA) was biotransformed using the fungus Xylaria sp., resulting in the synthesis of a novel compound 3 fi,7 fi-dihydroxyacanthoic acid (S1). The activity of S1 against Escherichia coli and its interactions with superoxide dismutase 1 (SOD1) were investigated using molecular docking. The results suggest that SOD1 enzyme could be a potential target for the antioxidant activity of S1.
Article
Chemistry, Multidisciplinary
Irum Shahzadi, Ameer Fawad Zahoor, Azhar Rasul, Asim Mansha, Sajjad Ahmad, Zohaib Raza
Summary: A series of novel theophylline-7-acetic acid (acefylline)-derived 1,2,4-triazole hybrids with N-phenyl acetamide moieties were synthesized and tested for inhibitory potential against lung and breast cancer cell lines. Compound 11g showed the strongest inhibition with the lowest IC50 value and low cytotoxicity, and in silico modeling was carried out to confirm its binding mode in relation to its anti-cancer activity.
Article
Oncology
Jian Lin, Yuting Dai, Chen Sang, Guohe Song, Bin Xiang, Mao Zhang, Liangqing Dong, Xiaoli Xia, Jiaqiang Ma, Xia Shen, Shuyi Ji, Shu Zhang, Mingjie Wang, Hai Fang, Xiaoming Zhang, Xiangdong Wang, Bing Zhang, Jian Zhou, Jia Fan, Hu Zhou, Daming Gao, Qiang Gao
Summary: This study reveals the heterogeneity of the immunogenomic traits in intrahepatic cholangiocarcinoma (iCCA) among patients, which poses challenges and opportunities for personalized immunotherapy.
JOURNAL FOR IMMUNOTHERAPY OF CANCER
(2022)
Article
Materials Science, Multidisciplinary
Yu Yang, Guoqing Wang, Longlin Lei, Yangkai Xiong, Zhiqiang Fang, Lei Huang, Jinbo Liu, Daxiong Hu, Jianhe Liao
Summary: This paper presents a new antibacterial nanofiller, triazole fluoroaromatic hydrocarbon-modified nano-zinc oxide, which can be mixed with zinc acrylate resin to produce a low surface energy antifouling coating. The coating exhibits a high bactericidal rate and is expected to be widely used in the field of marine antifouling.
Article
Chemistry, Medicinal
Warabhorn Rodphon, Pavitra Laohapaisan, Nantamon Supantanapong, Onrapak Reamtong, Lukana Ngiwsara, Kriengsak Lirdprapamongkol, Charnsak Thongsornkleeb, Nisachon Khunnawutmanotham, Jumreang Tummatorn, Jisnuson Svasti, Somsak Ruchirawat
Summary: Eighteen hybrid compounds between 8-bromo-2-fluoro-isocryptolepine and 1,2,3-triazole were synthesized and evaluated for cytotoxic activity against cancer cell lines. Some of these hybrids exhibited potent inhibitory effects on cancer cells with lower toxicity to normal cells. Further investigation revealed different mechanisms of action for the compounds in inhibiting cancer cell growth.
Article
Biochemistry & Molecular Biology
Xiaoping Zhao, Ziyang Chen, Ning Lin, Jingzhi Ma
Summary: In this study, a regio-selective and local modification strategy was performed on the reducing end of cellulose nanocrystals (CNC) with the grafting of long-chain poly(ethylene oxide) (PEO) to produce the end-grafted nanocrystals (CNC-eg-PEO). Through thiol-ene click reaction, the terminal allyl-PEO was covalently attached on the modified nanocrystal possessing the reactive thiol groups, maintaining surface chemistry and enhancing redisperstion stability. The CNC-eg-PEO showed low cytotoxicity to ATCC cell lines HFF and CAL-27, suggesting its potential for biomedical applications.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2021)
Article
Chemistry, Medicinal
Lan Luo, Jing Jing Jia, Qiu Zhong, Xue Zhong, Shilong Zheng, Guangdi Wang, Ling He
Summary: The newly synthesized compound 6a has shown promising anticancer activity by inhibiting cell growth and inducing apoptosis in vitro, as well as suppressing tumor growth in vivo, indicating its potential as a future anticancer agent.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Engineering, Environmental
Meijiao Zhou, Jinhua Li, Mine Du, Jun Wang, Han Yeong Kaw, Lizhong Zhu, Wei Wang
Summary: In this study, it was found that halobenzoquinones (HBQs) can be metabolized by reacting with glutathione (GSH) to form various glutathionylated conjugates (SG-HBQs), and SG-MeO-HBQs were identified as the primary metabolites significantly correlated with the unusual cytotoxicity variation of HBQs. This metabolic pathway can enhance toxicity and provide new insights into the toxicity and metabolic mechanism of HBQs.
ENVIRONMENTAL SCIENCE & TECHNOLOGY
(2023)
Article
Nanoscience & Nanotechnology
Olesya A. Laput, Irina V. Vasenina, Yelena G. Shapovalova, Andrey N. Ochered'ko, Aleksandr Chernyavskii, Sergey Kudryashov, Irina A. Kurzina
Summary: In this study, the effect of low-temperature barrier discharge plasma treatment on the modification of polylactic acid (PLA)-based scaffolds was explored. The immune response of macrophages to the modified PLA surface was also investigated. Results showed that argon plasma treatment can improve the wettability characteristics of PLA and increase the surface energy, but it has a certain effect on cell viability. Furthermore, the presence of PLA scaffolds does not cause excessive expression of proinflammatory cytokines.
ACS APPLIED MATERIALS & INTERFACES
(2022)
Article
Chemistry, Multidisciplinary
Gicheon Lee, Chanmin Lee, Hyungjin Kim, Yukwon Jeon, Yong-Gun Shul, Jinwon Park
Summary: A composite nanoparticle with an acid-base bifunctional structure has been developed for the transesterification of rapeseed oil, showing improved fatty acid methyl ester conversions compared to pure nanoparticles. The optimal catalyst with a triazole:PWA ratio of 6:1 exhibited the best performance due to its large surface area, balanced acidity, and strong basicity.
Article
Biochemistry & Molecular Biology
Willyenne M. Dantas, Valentina N. M. de Oliveira, Diogo A. L. Santos, Gustavo Seabra, Prem P. Sharma, Brijesh Rathi, Lindomar J. Pena, Ronaldo N. de Oliveira
Summary: Viruses like Zika virus (ZIKV) are responsible for certain diseases, but there is currently no specific treatment available. A study found that specific hybrid compounds have antiviral activity against ZIKV, showcasing potential for future applications.
Review
Gastroenterology & Hepatology
Chiara Raggi, Maria Letizia Taddei, Colin Rae, Chiara Braconi, Fabio Marra
Summary: Metabolic reprogramming is a characteristic of cancer, allowing tumor cells to survive and proliferate in resource-limited conditions. Cholangiocarcinoma, the second most common form of primary liver cancer, is associated with metabolic alterations such as increased aerobic glycolysis and glutamine anaplerosis. Therapeutic interventions targeting these metabolic changes may have potential benefits for treating cholangiocarcinoma.
JOURNAL OF HEPATOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Aida Buza, Cuneyt Turkes, Mustafa Arslan, Yeliz Demir, Busra Dincer, Arleta Rifati Nixha, Sukru Beydemir
Summary: Sulfonamides bearing 1,2,3-triazole moiety were designed as inhibitors of human alpha-carbonic anhydrases (hCAs). Some derivatives showed selectivity towards the hCA I and II isoforms. The synthesized compounds demonstrated significant antiproliferative activity and minimal cytotoxicity in various cell lines.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2023)
Article
Pharmacology & Pharmacy
Anisha Mazumder, Anupma Dwivedi, Wirat Assawapanumat, Rungnapha Saeeng, Witaya Sungkarat, Norased Nasongkla
Summary: In this study, galactose-targeted and non-targeted micelles were designed to enhance the anticancer activity and achieve targeted imaging using RSPP050 as an anticancer agent and superparamagnetic iron oxide (SPIO) as a contrast agent. The results showed that galactose micelles had higher drug loading content and cytotoxicity compared to non-targeted micelles. Moreover, targeted SPIO micelles decreased the magnetic resonance imaging (MRI) intensity, indicating their potential as a contrast agent for hepatocellular carcinoma.
PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY
(2022)
Article
Chemistry, Organic
Suttida Rinkam, Warapong Senapak, Sarayut Watchasit, Rungnapha Saeeng, Uthaiwan Sirion
Summary: A convenient and practical method for the synthesis of unsymmetrical triarylmethanes was demonstrated using a Bronsted acidic ionic liquid as the catalyst in a one-pot three-component double Friedel-Crafts reaction at 80 degrees C. The reaction was successful under metal- and solvent-free conditions, yielding moderate to high yields of the desired products from a wide range of substrates. The mechanism of the reaction was studied using quantitative NMR analysis.
Article
Biochemistry & Molecular Biology
Bodee Nutho, Patcharin Wilasluck, Peerapon Deetanya, Kittikhun Wangkanont, Patcharee Arsakhant, Rungnapha Saeeng, Thanyada Rungrotmongkol
Summary: This study investigates the potential of twenty-one 12-dithiocarbamate-14-deoxyandrographolide analogues as inhibitors of SARS-CoV-2 Mpro through in vitro and in silico studies. The findings suggest that four compounds show promising inhibitory activity against SARS-CoV-2 Mpro, highlighting their potential as antiviral agents.
COMPUTATIONAL AND STRUCTURAL BIOTECHNOLOGY JOURNAL
(2022)
Article
Pharmacology & Pharmacy
Supusson Pengnam, Purin Charoensuksai, Boon-ek Yingyongnarongkul, Rungnapha Saeeng, Hasan Uludag, Prasopchai Patrojanasophon, Praneet Opanasopit, Samarwadee Plianwong
Summary: Breast cancer is the second leading cause of cancer-related death in the US. This study developed a chitosan derivative-stabilized 3nAG nanosuspension and improved its efficacy in killing breast cancer cells by adding siRNA.
Article
Chemistry, Multidisciplinary
Patamawadee Silalai, Suwichada Jaipea, Jiraporn Tocharus, Anan Athipornchai, Apichart Suksamrarn, Rungnapha Saeeng
Summary: The designed and synthesized 1,2,3-triazole-genipin analogues showed neuroprotective activity and inhibition of butyrylcholinesterase. They have the potential to be promising lead compounds as anti-Alzheimer's agents.
Article
Multidisciplinary Sciences
Chihiro Motozono, Mako Toyoda, Toong Seng Tan, Hiroshi Hamana, Yoshihiko Goto, Yoshiki Aritsu, Yusuke Miyashita, Hiroyuki Oshiumi, Kimitoshi Nakamura, Seiji Okada, Keiko Udaka, Mizuki Kitamatsu, Hiroyuki Kishi, Takamasa Ueno
Summary: Mutations in the spike protein of SARS-CoV-2 can lead to escape from the neutralizing antibody response but still retain susceptibility to cellular immune response. A specific mutation, G446S, in the spike protein of the Omicron BA.1 variant affects antigen processing/presentation and enhances antiviral activity by vaccine-induced T cells.
NATURE COMMUNICATIONS
(2022)
Article
Multidisciplinary Sciences
Supawan Jamnongsong, Patipark Kueanjinda, Pongsakorn Buraphat, Phuwanat Sakornsakolpat, Kulthida Vaeteewoottacharn, Seiji Okada, Siwanon Jirawatnotai, Somponnat Sampattavanich
Summary: This study presents a comprehensive drug response profiling for cholangiocarcinoma (CCA) and identifies two major CCA subgroups with unique molecular pathways. MEK and Src inhibitors show specific cytotoxicity against one CCA subgroup without affecting normal cholangiocytes. The developed CCA45 signature accurately predicts prognosis for Asian CCA patients and provides a valuable resource for drug repurposing in CCA and rare cancers.
Article
Oncology
Ayumi Kanemaru, Satoru Shinriki, Mimi Kai, Kanae Tsurekawa, Kazuya Ozeki, Shota Uchino, Naoki Suenaga, Kou Yonemaru, Shunsuke Miyake, Takeshi Masuda, Ryusho Kariya, Seiji Okada, Hisashi Takeshita, Yuki Seki, Hiromu Yano, Yoshihiro Komohara, Ryoji Yoshida, Hideki Nakayama, Jian-Dong Li, Hideyuki Saito, Hirofumi Jono
Summary: EGFR-targeted molecular therapies, such as EGFR-TKIs, have potential as novel therapeutic agents for CYLD-negative oral squamous cell carcinoma (OSCC) patients with poor prognosis, according to this study.
CANCER CELL INTERNATIONAL
(2022)
Article
Plant Sciences
Suwichada Jaipea, Natthiya Saehlim, Waraporn Sutcharitruk, Anan Athipornchai, Kornkanok Ingkaninan, Rungnapha Saeeng
Summary: The alkaloid piperine 1 extracted from the black pepper plant (Piper nigrum L.) was converted to piperine amide derivatives (3a-3z) through condensation with various piperazine derivatives and secondary amines. These synthesized compounds were evaluated for their antioxidant and inhibition activities against AChE and BChE, which are important targets for Alzheimer’s disease therapy. Most of the compounds showed good antioxidant behavior and potent inhibition of AChE and BChE activities. In particular, compound 3c exhibited the highest AChE inhibition, while compounds 3v, 3x, and 3z showed better BChE inhibitory activities than galantamine. Docking studies confirmed their good binding energies to the target enzymes, suggesting their potential as anti-Alzheimer's drugs.
PHYTOCHEMISTRY LETTERS
(2023)
Article
Virology
Patta Phumesin, Jutatip Panaampon, Ryusho Kariya, Thawornchai Limjindaporn, Pa-thai Yenchitsomanus, Seiji Okada
Summary: Dengue virus (DENV) infection is a serious public health problem in tropical and subtropical regions, causing a range of clinical manifestations. Currently, there is no specific antiviral drug for DENV infection. In this study, cepharanthine (CEP) was found to have inhibitory effects on DENV infection at the initial viral replication states and proinflammatory cytokine secretion, making it a potential candidate for further development as an anti-DENV treatment.
Article
Multidisciplinary Sciences
Kamonnaree Chotinantakul, Pattranuch Chusri, Seiji Okada
Summary: This study investigated the prevalence and molecular genetic features of ESBL-producing and multidrug-resistant E. coli in river water in northern Thailand. The results showed that approximately 45.3% of E. coli were MDR, and 22% were ESBL producers. Among the ESBL-producing strains, CTX-M-15 was the predominant type. The study also revealed the presence of various plasmid replicons and mobile elements.
Article
Plant Sciences
Parichaya Aimvijarn, Witchuda Payuhakrit, Nisamanee Charoenchon, Seiji Okada, Prasit Suwannalert
Summary: Ultraviolet type B (UVB) radiation plays an important role in hyperpigmentation disorder by inducing cellular oxidative stress and abnormal melanin production. Phenolic compounds, which are secondary metabolites synthesized in stress conditions, have been found to have antioxidant and anti-melanogenesis properties. However, their effect on F-actin rearrangement-associated dendrite formation has not been studied. This study aimed to investigate the enhancement of phenolic compounds in riceberry rice germination under UVB radiation (RR-GR) and their potential in suppressing melanogenesis through F-actin rearrangement.
Article
Plant Sciences
Nittaya Boonmuen, Kanoknetr Suksen, Mintra Kaewkittikhun, Laongthip Ruknarong, Patamawadee Silalai, Rungnapha Saeeng, Arthit Chairoungdua, Sunhapas Soodvilai, Duangrat Tantikanlayaporn
Summary: While obesity is a global health threat, effective pharmacological interventions have been limited. This study explored the use of a genipin analogue, G300, derived from Gardenia jasminoides Ellis, as a potential therapeutic agent for obesity. G300 was found to suppress adipogenic differentiation and lipid accumulation in adipocytes, and improve adipocyte function. These findings suggest that G300 has the potential to be a novel treatment for obesity and related disorders.
JOURNAL OF NATURAL PRODUCTS
(2023)
Article
Chemistry, Organic
Patamawadee Silalai, Rungnapha Saeeng
Summary: This paper presents the acid-controlled divergent synthesis of 3-pyrrolidin-2-yl-1H-indoles and symmetric and unsymmetrical bis(indolyl)methanes (BIMs) through photocatalyzed decarboxylative coupling and Friedel-Crafts alkylation reactions. The method offers C-H functionalization, switchable formation of two products, room-temperature conditions, low photocatalyst loadings, absence of strong oxidant, and moderate to excellent yields. It has been successfully applied for the synthesis of natural product vibrindole A and 1,1-bis(1H-indol-3-yl)-2-phenylethane.
JOURNAL OF ORGANIC CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Piyanard Boonnate, Ryusho Kariya, Seiji Okada
Summary: Adult T cell leukemia/lymphoma (ATLL) is an aggressive T-cell malignancy that develops in some elderly human T-cell leukemia virus (HTVL-1) carriers. Despite conventional and targeted therapies, ATLL has a poor prognosis, and a new safe and efficient therapy is required. This study found that Shikonin (SHK) could induce apoptosis of ATLL cells through the generation of reactive oxygen species (ROS), loss of mitochondrial membrane potential, and induction of endoplasmic reticulum (ER) stress. These findings suggest that SHK could be a potent anti-ATLL agent.
