Article
Biochemistry & Molecular Biology
Olga Michalak, Marcin Cybulski, Wojciech Szymanowski, Agnieszka Gornowicz, Marek Kubiszewski, Kinga Ostrowska, Piotr Krzeczynski, Krzysztof Bielawski, Bartosz Trzaskowski, Anna Bielawska
Summary: A series of new derivatives of ursolic acid (UA) were designed and synthesized by substituting various amino acids (AAs) or dipeptides (DP) at the C-3 position of the steroid skeleton. These conjugates exhibited cytotoxic activity against hormone-dependent and triple-negative breast cancer cells. Mechanistic studies revealed the activation of apoptotic pathways for some compounds and the induction of autophagy for others. Additionally, the synthesized compounds showed potential as anticancer agents based on their ADME properties and molecular docking to the estrogen receptor.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Medicinal
Baoen He, Zuchang Zhu, Fenglian Chen, Rong Zhang, Weiqiang Chen, Te Zhang, Tao Wang, Jiamei Lei
Summary: The newly synthesized NO-releasing ursolic acid-arylidene derivative compound 5c showed potent broad-spectrum antitumor activity in various tumor cell lines, especially exhibiting the strongest apoptosis-inducing effect in MCF-7 cells. Compound 5c affected cell cycle, activated caspase, decreased the Bcl-2/Bax ratio, led to changes in mitochondrial membrane potential, and accumulation of reactive oxygen species in the cells. Additionally, a docking study revealed a potential interaction between the nitroxyethyl moiety of compound 5c and caspase-8 amino acid residues.
ARCHIV DER PHARMAZIE
(2021)
Article
Chemistry, Medicinal
Liwei Ma, Jinling Zhang, Xuemei Wang, Jifang Yang, Lina Guo, Xiaoli Wang, Bo Song, Wei Dong, Wenbao Wang
Summary: DSG-amino acid ester derivatives showed cytotoxic activities against various human cancer cell lines, with compound 7g exhibiting the most significant cytotoxicity against the K562 cell line. Mechanistic studies revealed that compound 7g induced mitochondrial-related apoptosis in K562 cells, highlighting its potential as a promising scaffold for the development of more potent anticancer agents.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Wen-Yan Wang, Wen-Yi Wu, A-Liang Li, Qing-Song Liu, Yue Sun, Wen Gu
Summary: Novel indolequinone derivatives of ursolic acid bearing ester, hydrazide, or amide moieties were designed, synthesized, and screened for their in vitro antiproliferative activities. Among them, compound 6t exhibited potent activity against three cancer cell lines with low cytotoxicity to normal cells. The compound induced apoptosis in cancer cells and may target the PI3K/AKT/mTOR signaling pathway, suggesting it as a promising lead for novel anticancer agents.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Manuela-Maria Iftime, Gabriela Liliana Ailiesei, Sergiu Shova, Camelia Miron, Hiromasa Tanaka, Masaru Hori, Luminita Marin
Summary: This paper reports the synthesis, structural characterization, and investigation of the antioxidant and anticancer activities of novel betulin-imine derivatives. The compounds were characterized using various methods and their chemical structures were confirmed. The results showed that the betulin-imine derivatives exhibited improved antioxidant and anticancer activities compared to betulin.
NEW JOURNAL OF CHEMISTRY
(2023)
Article
Engineering, Chemical
Yihong Yang, Siyue Ma, Ting Li, Jingjing He, Shitao Liu, Hongwu Liu, Jiaojiao Zhang, Xiang Zhou, Liwei Liu, Song Yang
Summary: In this study, ursolic acid derivatives were synthesized and assessed for their antibacterial ability. The results showed that one compound exhibited outstanding antibacterial activity, inducing bacterial death through excessive accumulation of reactive oxygen species and damage to the cell membrane. Moreover, the addition of hydrogen peroxide enhanced the antibacterial efficacy of this compound.
FRONTIERS OF CHEMICAL SCIENCE AND ENGINEERING
(2023)
Article
Chemistry, Physical
Jie-Ping Fan, Xiao-Hui Lai, Xue-Hong Zhang, Lu Yang, Tian-Tao Yuan, Hui-Ping Chen, Xianrui Liang
Summary: The formation of ionic derivatives from oleanolic acid (OA) and ursolic acid (UA) through a non-covalent synthetic approach improved their solubility and biological activity, showing potential for clinical applications. The UA-based ionic derivatives exhibited stronger inhibitory effects on the growth of human hepatoma cell lines compared to OA-based derivatives.
JOURNAL OF MOLECULAR LIQUIDS
(2021)
Article
Pharmacology & Pharmacy
Han Li, You Yu, Yi Liu, Zhihong Luo, Betty Yuen Kwan Law, Yi Zheng, Xing Huang, Wenhua Li
Summary: The combination of sorafenib and ursolic acid has shown significant synergistic antitumor activity in both in vitro and in vivo tumor xenograft models. The treatment induces selective apoptotic death and ferroptosis in cancer cells through the accumulation of intracellular reactive oxygen species. These findings suggest a novel effective therapeutic strategy for tumor treatment.
PHARMACOLOGICAL RESEARCH
(2022)
Article
Chemistry, Medicinal
Laura Grau, Richard Soucek, M. Dolors Pujol
Summary: Resveratrol, a natural compound with antioxidant properties, has potential as both a chemopreventive and cancer chemotherapeutic agent. Due to its poor bioavailability, the study of new derivatives is important. In this study, (E)-stilbenes derived from resveratrol and cyclic analogues with benzofuran or indole nucleus were synthesized and evaluated for their impact on tumor growth. Some compounds showed higher cytotoxicity than (E)-resveratrol, with one derivative demonstrating eight times greater cytotoxic activity against colon cancer cells. Certain cyclic derivatives also exhibited strong inhibition of cell growth.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Review
Medicine, Research & Experimental
Shumaila Ijaz, Javed Iqbal, Banzeer Ahsan Abbasi, Zakir Ullah, Tabassum Yaseen, Sobia Kanwal, Tariq Mahmood, Sandugash Sydykbayeva, Alibek Ydyrys, Zainab M. Almarhoon, Javad Sharifi-Rad, Christophe Hano, Daniela Calina, William C. Cho
Summary: Cancer remains a major cause of death globally, and rosmarinic acid (RA) is a bioactive compound found in plants. This review highlights the chemopreventive and chemotherapeutic effects of RA and its derivatives, providing clues for the development of complementary drugs for cancer treatment.
BIOMEDICINE & PHARMACOTHERAPY
(2023)
Article
Chemistry, Medicinal
Guolong Li, Zhichao Du, Pingping Shen, Jian Zhang
Summary: MeON-UA, especially compound 2a, showed significant antitumor activity against HepG2 cells by inducing apoptosis and targeting the PI3K/AKT/mTOR signaling pathway.
Article
Biochemistry & Molecular Biology
Ju Chen, Yunran Xu, Yan Yang, Xin Yao, Yuan Fu, Yi Wang, Yunjun Liu, Xiuzhen Wang
Summary: In this study, a series of glycyrrhetic acid derivatives were synthesized and their cytotoxicity against tumor cells was investigated. Compound 3a showed high antiproliferative activity against HeLa cells and its mechanism of action was explored through various assays. The results demonstrated that compound 3a could block the cell cycle, inhibit cell migration, induce apoptosis, and affect the expression of mitochondria-related proteins. This work provides valuable insights for the development of glycyrrhetinic acid compounds as potential anticancer molecules.
Article
Biochemistry & Molecular Biology
Natalia Wronska, Michal Szlaur, Katarzyna Zawadzka, Katarzyna Lisowska
Summary: Currently, there is a need for new antimicrobial drugs due to the excessive use of antibiotics and emerging resistance amongst bacteria. This study found that two triterpenoids and one flavonoid displayed antimicrobial activity and showed potential synergistic effects, enhancing the antimicrobial potential.
Review
Biochemistry & Molecular Biology
Siva S. Panda, Muthusamy Thangaraju, Bal L. Lokeshwar
Summary: Ursolic acid (UA) is a pentacyclic triterpene with diverse pharmacological properties, including anti-inflammatory, antimicrobial, antiviral, antioxidant, and anti-proliferative activities. It holds promise as a cancer preventive and therapeutic agent due to its relatively non-toxic properties against normal cells but its activities against cancer cells. However, its low bioavailability limits its clinical applications. Researchers have been designing and developing synthetic analogs of UA to overcome this limitation and utilize its importance.
Article
Chemistry, Medicinal
Linling Gan, Zongjie Gan, Yanrong Dan, Yaowei Li, Peiming Zhang, Shanwen Chen, Zaijun Ye, Tao Pan, Chunmei Wan, Xuelian Hu, Yu Yu
Summary: A series of novel TNBG analogues were developed, among which compound 14g exhibited strong inhibitory effects on HepG2 and A549 cells, possibly through the activation of PPARγ expression. In an in vivo xenograft model, 14g effectively reduced tumor growth and demonstrated excellent water solubility.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Engineering, Environmental
Hongmei Xiang, Jiao Meng, Wubin Shao, Dan Zeng, Jin Ji, Peiyi Wang, Xiang Zhou, Puying Qi, Liwei Liu, Song Yang
Summary: The excessive use and eco-unfriendly behavior of traditional pesticide formulations have serious drawbacks. In this study, a scalable and sustainable biopolymer-based core-shell nanocarrier loaded with an anti-viral candidate agent was developed for plant disease management. The nanocarrier exhibited enhanced UV resistance, improved foliar surface wettability, and activated host plant defense responses.
CHEMICAL ENGINEERING JOURNAL
(2023)
Article
Engineering, Environmental
Xiang Tan, Hongguo Wu, Heng Zhang, Hu Li, Song Yang
Summary: A renewed heterogeneous catalyst, PtSA/NC-AMP, consisting of both Pt single atoms and nanoclusters supported by Al(PO3)3, was developed for efficient hydrogenative scission of alkyl/aryl C-O bonds in lignin derivatives and oxygenated aryl/alkyl compounds, resulting in the formation of arenes and alkanes, respectively. The relay catalytic process based on the finite size effect, where Pt single atoms and nanoclusters play different roles, contributes to the excellent reactivity of PtSA/NC-AMP. Furthermore, the size-dependent strong metal-support interaction of Pt-Al(PO3)3 enhances the reactivity and stability of PtSA/NC-AMP. This study provides a reference for the multi-step upgrading of biomass involving targeted alkyl/aryl C-O bond cleavage.
CHEMICAL ENGINEERING JOURNAL
(2023)
Article
Biochemistry & Molecular Biology
Puying Qi, Na Wang, Taihong Zhang, Yumei Feng, Xiang Zhou, Dan Zeng, Jiao Meng, Liwei Liu, Linhong Jin, Song Yang
Summary: Anti-virulence strategies are effective for controlling bacterial diseases by targeting virulence factors. In this study, a series of dehydroabietic acid derivatives were synthesized and evaluated for their antibacterial activity. Compound 2b showed promising antibacterial activity against Xanthomonas oryzae pv. oryzae and effective control of bacterial leaf blight in rice. It also suppressed various virulence factors. These compounds can serve as lead compounds for developing novel bactericides.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Agriculture, Multidisciplinary
Dan Zeng, Shuai-Shuai Liu, Wu-Bin Shao, Tai-Hong Zhang, Pu-Ying Qi, Hong-Wu Liu, Xiang Zhou, Li-Wei Liu, Heng Zhang, Song Yang
Summary: This study synthesized 35 new 1,3,4-oxadiazole derivatives and evaluated their anti-phytopathogenic activities. Compound C-7 showed excellent antibacterial activity in vitro and acceptable activity in vivo against rice bacterial leaf blight. Moreover, C-7 could indirectly reduce the inducible expression of host SWEET genes, alleviating nutrient supply in the infection process of phytopathogenic bacteria. The study highlights the potential of 1,3,4-oxadiazole-based agrochemicals in controlling plant bacterial diseases.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2023)
Article
Agriculture, Multidisciplinary
Lihui Shao, Su Zhao, Song Yang, Xiang Zhou, Yan Li, Chengpeng Li, Danping Chen, Zhuirui Li, Guiping Ouyang, Zhenchao Wang
Summary: To discover novel antibacterial agents, two series of quinazolinone derivatives with novel structures were synthesized and their bioactivity against plant bacteria was tested. Compound D32 was identified as a potent antibacterial inhibitor against Xanthomonas oryzae pv. Oryzae (Xoo), with better inhibitory capacity compared to the commercial drugs. Further investigation revealed the mechanism of action of D32, which provides clues for the development of new therapeutic strategies.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2023)
Article
Agronomy
Wu-Bin Shao, Yan-Mei Liao, Rong-Shuang Luo, Jin Ji, Wan-Lin Xiao, Xiang Zhou, Li-Wei Liu, Song Yang
Summary: In this study, new phenothiazine derivatives were synthesized and evaluated for their inhibitory activity against tobacco mosaic virus (TMV). Compound A(8) exhibited the highest protective activity against TMV, with an EC50 of 115.67 μg/mL, which was significantly superior to the positive controls ningnanmycin and ribavirin. Biochemical assays demonstrated that compound A(8) could inhibit TMV replication by disrupting its self-assembly and also enhance the defense responses of tobacco plants. This research provides valuable insights for the discovery of new agrochemicals to control plant viral diseases.
PEST MANAGEMENT SCIENCE
(2023)
Article
Agronomy
Jiao-Jiao Zhang, Yu-Mei Feng, Jun-Rong Zhang, Wan-Lin Xiao, Shuai-Shuai Liu, Xiang Zhou, Heng Zhang, Pei-Yi Wang, Li-Wei Liu, Song Yang
Summary: A series of simple triclosan derivatives containing isopropanolamine moiety were designed and assessed for their antibacterial behavior. Some compounds showed excellent bioactivity against three destructive bacteria. Compound C-8 displayed high bioactivities towards Xoo and Xac.
PEST MANAGEMENT SCIENCE
(2023)
Article
Agronomy
Zhenxing Li, Binxin Yang, Yue Ding, Xiang Zhou, Zimian Fang, ShuaiShuai Liu, Jie Yang, Song Yang
Summary: A series of phosphonate derivatives containing a 1,2,3-triazole motif were developed and evaluated for their antiviral activity against tobacco mosaic virus (TMV) helicase. The optimized B-17 showed stronger curative activity against TMV compared to the commercial drug Ribavirin. Additionally, B-17 exhibited potential antiviral activity against other viruses and pathogens.
PEST MANAGEMENT SCIENCE
(2023)
Article
Energy & Fuels
Jinyu Tan, Dayong Yu, Junfa Yuan, Hongguo Wu, Hangyu Luo, Heng Zhang, Xiaobing Li, Hu Li, Song Yang
Summary: A novel ternary deep eutectic solvent (DES) was designed for wheat straw pretreatment, which achieved non-condensed lignin and high-yield fermentable sugars. The introduction of ethylene glycol into the DES protected lignin structure and improved enzymatic digestibility of cellulose. Trichosporon cutaneum cultivated in the waste liquid and residue hydrolysate produced 8.7 g microbial lipid per 100 g wheat straw, surpassing previous reports.
Article
Biochemistry & Molecular Biology
Zhenxing Li, Binxin Yang, Yue Ding, Jiao Meng, Jinhong Hu, Xiang Zhou, Liwei Liu, Zhibing Wu, Song Yang
Summary: Plant diseases caused by malignant and refractory phytopathogenic viruses have been effectively inhibited by novel eugenol derivatives targeting the tobacco mosaic virus helicase. Compound 2 t showed superior binding capability and impressive anti-viral activity, outperforming commercial drugs.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2023)
Article
Agriculture, Multidisciplinary
Wu-Bin Shao, Rong-Shuang Luo, Jiao Meng, Xiao-Kang Lv, Hong-Mei Xiang, Wan-Lin Xiao, Xiang Zhou, Li-Wei Liu, Zhi-Bing Wu, Song Yang
Summary: Phenothiazine derivatives showed excellent bioactivity against different bacteria and demonstrated potential as pesticide candidates for plant diseases. Compound C-2 had high effectiveness against rice leaf blight, outperforming commonly used pesticides.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2023)
Review
Chemistry, Physical
Wenfeng Zhao, Hu Li, Heng Zhang, Song Yang, Anders Riisager
Summary: Ammonia borane (AB) is a promising material for hydrogen storage and has attracted much attention in reductive organic transformations. This review summarizes the recent progress of AB-mediated transfer hydrogenation reactions of various substrates and discusses the synthesis protocols, reaction parameters, product distribution, and reactivity. The mechanism involving the action mode of AB and structure-activity relationships are also discussed, and the challenges and opportunities for AB-enabled transfer hydrogenation reactions are highlighted.
GREEN ENERGY & ENVIRONMENT
(2023)
Article
Chemistry, Multidisciplinary
Ye Meng, Jinshu Huang, Jie Li, Yumei Jian, Song Yang, Hu Li
Summary: By mimicking the key active species of hemoglobin p450 heme monooxygenase, a Fe-N-4 single atom-doped sulfur-containing carbon nitride photocatalyst was prepared and demonstrated to efficiently convert bio-based alcohols and NH2OH dot HCl to nitriles. The Fe-N-4 sites in the catalyst directly capture photogenerated electrons and molecular oxygen to generate superoxide radicals, while the surrounding S atoms confine photogenerated holes. This strategy of constructing atomic sites enhances the photocatalytic activity and selectivity for biomass valorization.
Article
Chemistry, Multidisciplinary
Feng Xu, Zao Li, Li-Long Zhang, Shengqi Liu, Hu Li, Yuhe Liao, Song Yang
Summary: Upgrading biomass-derived platforms to functionalized aromatics by a tandem Diels-Alder (DA) cycloaddition-aromatization strategy has attracted attention. Three challenges exist: improving the equilibrium of DA cycloaddition, controlling the regioselectivity of DA adducts, and increasing the stability of the cycloadduct. In this study, an intramolecular cycloaromatization strategy was developed using a defective Zn-BTC-SA catalyst and an acidic ionic liquid to achieve efficient and selective conversion of bio-furfurals to isoindolinones under liquid phase conditions. The protocol showed high yields and scalability.
Article
Chemistry, Multidisciplinary
Long Chen, Yixuan Liu, Heng Zhang, Yuncong Li, Songdang Zhang, Yulin Hu, Hu Li, Song Yang
Summary: Utilization of renewable biomass resources to produce value-added platform molecules, such as anethole, has attracted significant attention. In this study, a green and effective method for the stereoselective conversion of biomass-derived 4'-methoxyphenylacetone into trans-anethole was developed using a bifunctional acid catalyst. The catalyst exhibited a favorable structure with specific surface area, abundant mesopores, acidic sites, hydrophobicity, and stability. The optimized reaction conditions resulted in a high yield and excellent reusability. This catalytic strategy shows promise for the synthesis of anethole and other high-value molecules.
REACTION CHEMISTRY & ENGINEERING
(2023)
Article
Chemistry, Medicinal
Shuang Mei, Su Jiang, Yuting Wang, Han Jing, Peng Yang, Miao-Miao Niu, Jindong Li, Kai Yuan, Yan Zhang
Summary: This study identifies a dual-targeting peptide, AP-1, that effectively inhibits variants of concern (VOCs) of SARS-CoV-2 without impairing host cell viability. The findings suggest that AP-1 could be a promising broad-spectrum agent for treating emerging VOCs of SARS-CoV-2.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Hyeonjun Lee, Ju Yeon Lee, Hyunsoo Jang, Hye Young Cho, Minhee Kang, Sang Hyun Bae, Suin Kim, Eunji Kim, Jaebong Jang, Jin Young Kim, Young Ho Jeon
Summary: By using liquid chromatography-tandem mass spectrometry and nuclear magnetic resonance experiments, we identified new chemical moieties that bind to the target sites of the protein of interest, allowing for reversible binding and protein degradation. This method has the potential to expand the application of PROTAC technology.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Yingying Li, Xiyou Du, Xinru Kong, Yuelin Fang, Zhijing He, Dongzhu Liu, Hang Wu, Jianbo Ji, Xiaoye Yang, Lei Ye, Guangxi Zhai
Summary: This study proposes a novel nanoplatform based on the autophagy cascade to overcome the obstacles in chemo-immunotherapy. The platform combines chemotherapy and starvation therapy to initiate pro-death autophagy and enhance antigen presentation, while also remodeling the immunosuppressive tumor microenvironment. Furthermore, the study discovers a new therapeutic direction for the respiration inhibitor 3-bromopyruvic acid (3BP) in cancer treatment. Overall, this study offers an opportunity to improve antitumor efficacy and boost immune responses.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Bingsi Wang, Mingxu Ma, Yusen Dai, Pengfei Yu, Liang Ye, Wenyan Wang, Chunjie Sha, Huijie Yang, Yingjie Yang, Yunjing Zhu, Lin Dong, Shujuan Wei, Linlin Wang, Jingwei Tian, Hongbo Wang
Summary: Breast cancer is a common malignant tumor in women, and drug resistance remains a clinical challenge. In this study, a novel compound, G-5b, was developed with potent antagonistic and degradation activities comparable to the current drug fulvestrant. G-5b also showed improved stability and solubility. Mechanistically, G-5b engages the proteasome pathway to degrade ER, inhibiting the ER signaling pathway and inducing apoptosis and cell cycle arrest. In animal models, G-5b exhibited superior pharmacokinetics and pharmacodynamics properties. Overall, G-5b is a promising long-acting SERD worthy of further investigation and optimization.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Karoline B. Waitman, Larissa C. de Almeida, Marina C. Primi, Jorge A. E. G. Carlos, Claudia Ruiz, Thales Kronenberger, Stefan Laufer, Marcia Ines Goettert, Antti Poso, Sandra V. Vassiliades, Vinicius A. M. de Souza, Monica F. Z. J. Toledo, Neuza M. A. Hassimotto, Michael D. Cameron, Thomas D. Bannister, Leticia Costa-Lotufo, Joa o A. Machado-Neto, Mauricio T. Tavares, Roberto Parise-Filho
Summary: A series of hybrid inhibitors combining pharmacophores of known kinase inhibitors and benzohydroxamate HDAC inhibitors were synthesized and evaluated for their anticancer activity and pharmacokinetic properties. Compounds 4d-f exhibited promising cytotoxicity against hematological cells and moderate activity against solid tumor models. Compound 4d showed potent inhibition of multiple kinase targets and had stable interactions with HDAC and members of the JAK family. These compounds showed selective cytotoxicity with minimal effects on non-tumorigenic cells and favorable pharmacokinetic profiles.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Michal Sulik, Diana Fontinha, Dietmar Steverding, Szymon Sobczak, Michal Antoszczak, Miguel Prudencio, Adam Huczynski
Summary: This study describes the synthesis of the first-in-class ivermectin derivatives obtained through derivatization of the C13 position, along with the unexpected rearrangement of the macrolide ring. These derivatives show potential for antiparasitic activity and are important for the development of new antiparasitic agents.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Jun Liu, Qiu-Xian Chen, Wen-Fu Wu, Dong Wang, Si -Yu Zhao, Jia-Hao Li, Yi-Qun Chang, Shao-Gao Zeng, Jia-Yi Hu, Yu-Jie Li, Jia-Xin Du, Shu-Meng Jiao, Hai-Chuan Xiao, Qiang Zhang, Jun Xu, Jian-Fu Zhao, Hai -Bo Zhou, Yong-Heng Wang, Jian Zou, Ping-Hua Sun
Summary: A new anti-infective drug strategy has been discovered to attenuate virulence and modulate inflammation caused by drug-resistant Pseudomonas aeruginosa infections. Compound 5f inhibits biofilm formation, macrophage migration, and inflammatory response induced by P. aeruginosa, showing potential as a novel candidate against drug-resistant infections.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Liuzeng Chen, Ke Wang, Lingyun Wang, Wei Wang, Lifan Wang, Jia Li, Xiaohan Liu, Mengya Wang, Banfeng Ruan
Summary: In this study, a series of novel anti-inflammatory compounds were designed and synthesized based on the natural product pterostilbene skeleton. Among them, compound 8 showed the highest activity and exhibited its effects through inhibition of pro-inflammatory cytokines by blocking the NF-KB/MAPK signaling pathway. Compound 8 also demonstrated a good relieving effect on acute colitis in mice and showed good safety in acute toxicity experiments.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Si-Min Liang, Gui-Bin Liang, Hui-Ling Wang, Hong Jiang, Xian-Li Ma, Jian-Hua Wei, Ri-Zhen Huang, Ye Zhang
Summary: A series of novel multi-target antitumor agents were designed, synthesized, and evaluated. Some compounds exhibited significant antitumor activity and one compound showed excellent efficacy, limited toxicity, and low resistance. Further mechanism studies revealed that the compound exerted antitumor effects through multiple pathways.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
