Article
Microbiology
Daisuke Oka, Naomitsu Yamaya, Takuya Kuno, Yuta Asakawa, Toshiyuki Shiragiku, Liang Chen, Jingbo Xue, Abudusaimi Mamuti, Fangguo Ye, Jiangqin Sun, Kinue Ohguro, Hisashi Miyamoto, Yukitaka Uematsu, Katsuya Inagaki, Jie-Fei Cheng, Makoto Matsumoto
Summary: OPS-2071 is a novel quinolone antibacterial agent with potent activity against Clostridioides difficile, exhibiting low systemic exposure and in vivo efficacy, making it a potential new therapeutic option for treating C. difficile infections.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2021)
Article
Biochemistry & Molecular Biology
Ekaterina Blinova, Egor Turovsky, Elena Eliseikina, Alexandra Igrunkova, Elena Semeleva, Grigorii Golodnev, Rita Termulaeva, Olga Vasilkina, Sofia Skachilova, Yan Mazov, Kirill Zhandarov, Ekaterina Simakina, Konstantin Belanov, Saveliy Zalogin, Dmitrii Blinov
Summary: A non-surgical pharmacological approach to control cellular vitality and functionality during ischemic and/or reperfusion-induced phases of strokes is important. The compound 3-EA has shown cell-protective effects by inhibiting cell death and calcium concentration increase. It intervenes in cell apoptosis through changes in gene expression, suggesting its potential as a neuroprotective molecule.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Microbiology
Aiko Masuko, Iichiro Takata, Kiyoko Fujita, Hirotoshi Okumura, Fumihito Ushiyama, Hideaki Amada, Hiroyuki Sugiyama
Summary: The novel DNA gyrase/topoisomerase IV inhibitor TP0480066 showed potent in vitro and in vivo activities against multidrug-resistant Neisseria gonorrhoeae strains, with no cross-resistance observed with ciprofloxacin. It also demonstrated low frequencies of spontaneous resistance and strong bactericidal activity, suggesting it may be a candidate antimicrobial agent for gonococcal infections.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2021)
Article
Biochemistry & Molecular Biology
Hui Shi, Jianhuan Li, Fei Liu, Sixue Bi, Weijuan Huang, Yuanyuan Luo, Man Zhang, Liyan Song, Rongmin Yu, Jianhua Zhu
Summary: A novel water-soluble alpha-d-glucan (ASPG-1) with immunoregulatory activity was purified and characterized from Arca subcrenata. ASPG-1 promoted lymphocyte viability, enhanced pinocytic capacity, and stimulated the secretion of NO and cytokines. It inhibited tumor growth in breast cancer mice and showed improved antitumor efficacy when combined with doxorubicin. Therefore, ASPG-1 has the potential to be developed as an adjuvant in tumor immunotherapy.
Article
Biochemistry & Molecular Biology
Zhiwei Zheng, Zhichao Chen, Ying Zhou, Yu Zou, Xiaojian Shi, Xiaobo Li, Jing Liao, Jun Yang, Xiang Li, Jintian Dai, Yuye Xu, Nipon Chattipakorn, Won-Jea Cho, Qidong Tang, Guang Liang, Wenqi Wu
Summary: In this study, a series of new compounds with diimide skeleton were successfully synthesized using CDI and NaH as condensation agents. The anti-inflammatory activity and cytotoxicity of the compound in RAW264.7 macrophages were evaluated. The results showed that these compounds exhibited good anti-inflammatory activity, with compound 4d showing an IC50 of 1.59 μM and 15.30 μM against IL-6 and TNF-α, respectively. Furthermore, compound 4d was able to alleviate acute lung injury (ALI) induced by LPS and improve the survival rate of LPS-induced sepsis in mice. Overall, the design and synthesis of the diimide skeleton provide a potential lead compound for the treatment of inflammatory diseases and offer a new approach for the design of amide compounds.
BIOORGANIC & MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Katarzyna Choroba, Beatriz Filipe, Anna Switlicka, Mateusz Penkala, Barbara Machura, Alina Bienko, Sandra Cordeiro, Pedro V. Baptista, Alexandra R. Fernandes
Summary: The study focused on the anticancer properties of dipicolinate-basedvanadium(IV) complexes with different diimines. These complexes showed high cytotoxic effect against HCT116-DoxR cells and induced cell death through apoptosis and autophagy pathways. They also interacted with BSA protein and did not promote tumor cell migration or angiogenesis.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Zixue Zhang, Qingwei Zhang, Hao Zhang, Minru Jiao, Zheng Guo, Xinyan Peng, Lei Fu, Jianqi Li
Summary: A series of novel compounds were designed, synthesized and evaluated for their anti-proliferative activity against cancer cells by demonstrating strong HDAC1 inhibitory activity with no adverse effects on normal cells.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Zhihao Chen, Karthik Rajan Rajamanickam, Mina Ding, Sang Kyoon Kim, Sang-wook Park, Eunae Kim, Sunwoo Lee, Tae-Hoon Lee
Summary: In this study, we discovered a potent candidate, PMSA derivative 11, for suppressing mature osteoclasts formation in vitro through a TRAP staining assay. The bioactivity of PMSA derivatives was evaluated and 11 showed the most promising bioactivity, with an IC50 value of 322.9 nM, which was 15-fold better than PMSA-3-Ac. Mechanistically, 11 decreased the expression of genes required for osteoclastogenesis by blocking NFATc1 translocation. In vivo investigation demonstrated that 11 prevented excessive osteoclastogenesis-mediated bone loss in ovariectomized osteoporosis mimic mice. These findings highlight the therapeutic potential of 11 as a lead compound for anti-osteoporosis by targeting NFATc1 translocation.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Mohammad Shafiei, Hossein Toreyhi, Loghman Firoozpour, Tahmineh Akbarzadeh, Mohsen Amini, Elaheh Hosseinzadeh, Mehrnoosh Hashemzadeh, Lee Peyton, Ensieh Lotfali, Alireza Foroumadi
Summary: Demand for new azole antifungal agents has increased due to the rising resistance of infective fungal species. The synthesis of novel fluconazole analogues with urea functionality led to the discovery of compounds 8b and 8c, which showed promising antifungal activities against Candida albicans. These compounds also demonstrated potent antibiofilm properties and low toxicity, making them potential leads for candidiasis drug discovery.
Article
Microbiology
Nathan P. Wiederhold, Thomas F. Patterson, Sandra Rebholz, Connell W. C. Boal, Monika Ehrensberger, Ryan Boyle, Melanie T. Cushion
Summary: A3IS is a synthetic product that releases hydrogen peroxide at therapeutic levels. It has broad-spectrum antimicrobial effects and has shown significant efficacy against various human pathogens, including fungi. It also exhibits good inhibitory effects on Pneumocystis. These findings suggest that A3IS is a novel antifungal agent.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2022)
Article
Biochemistry & Molecular Biology
Hui Shi, Santosh Panjikar, Chunlei Li, Xiaozheng Ou, Yun Zhou, Kunhao Zhang, Liyan Song, Rongmin Yu, Lianli Sun, Jianhua Zhu
Summary: Previous studies have shown that ASP-3 is a calcium-binding protein from Arca subcrenata that effectively inhibits the proliferation of HepG2 cells. Further research reveals that recombinant ASP-3 inhibits HepG2 cell proliferation by competitively binding to the EGF binding pocket of EGFR and inhibiting multiple signaling pathways. ASP-3 also demonstrates a significant antitumor effect in a HepG2 cell xenograft model, indicating its potential for liver cancer therapy.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2023)
Article
Biochemistry & Molecular Biology
I-Fan Lin, Chung-Hsu Lai, Shang-Yi Lin, Ching-Chi Lee, Nan-Yao Lee, Po-Yu Liu, Chih-Hui Yang, Yi-Han Huang, Jiun-Nong Lin
Summary: This study found that vancomycin is effective in treating E. anophelis infections, and the combination of vancomycin and rifampin can enhance their antimicrobial effect.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Environmental Sciences
Marwa E. Atya, Amr El-Hawiet, Mohamed A. Alyeldeen, Doaa A. Ghareeb, Mohamed M. Abdel-Daim, Mohamed M. El-Sadek
Summary: The study found that brown seaweed polysaccharides, particularly FUC, exhibit various benefits such as antioxidant, anti-inflammatory, anticancer, and hepatoprotective properties. Additionally, FCS showed stronger antioxidant and cytotoxic effects on hepatic cancer cells compared to FSP, and in vivo data demonstrated significant improvements in liver functions with FCS administration.
ENVIRONMENTAL SCIENCE AND POLLUTION RESEARCH
(2021)
Article
Agriculture, Multidisciplinary
Shuyi Song, Yanan Li, Xin Liu, Jiayi Yu, Zhe Li, Kexin Liang, Shaoping Wang, Jiayu Zhang
Summary: This study comprehensively screened and quantified the metabolites of astragalosides in Astragali Radix using techniques such as high-performance liquid chromatography and mass spectrometry. The study revealed the metabolic process of astragalosides in the intestine and found that the metabolites were associated with anti-inflammatory and antioxidant activities.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2023)
Article
Environmental Sciences
Jun Bai, Hailan Wang, Chenwen Li, Li Liu, Jianv Wang, Changzhen Sun, Qingbi Zhang
Summary: Melanoma is a highly invasive skin cancer, and current therapeutic drugs have limitations. This study developed a novel compound, SCZ0148, that targets mitochondria in melanoma cells. The results showed that SCZ0148 effectively inhibited melanoma cell proliferation, induced apoptosis and autophagy, and suppressed cell migration. This study suggests that SCZ0148 has great potential as a mitochondria-targeting anti-melanoma compound.
ENVIRONMENTAL TOXICOLOGY
(2023)