Review
Biochemistry & Molecular Biology
Gabriela Nistor, Cristina Trandafirescu, Alexandra Prodea, Andreea Milan, Andreea Cristea, Roxana Ghiulai, Roxana Racoviceanu, Alexandra Mioc, Marius Mioc, Viviana Ivan, Codruta Soica
Summary: This review summarizes the literature published in the last 10 years regarding derivatives of pentacyclic triterpenes bearing heterocyclic moieties and focuses on their biological activities and structure-activity relationships. The studies suggest that triterpenoid conjugates with heterocyclic moieties may be promising candidates for future clinical trials.
Article
Biochemistry & Molecular Biology
Jae Sang Han, Jun Gu Kim, Thi Phuong Linh Le, Yong Beom Cho, Mi Kyeong Lee, Bang Yeon Hwang
Summary: Three new ursane-type triterpenes and twenty-one known triterpenoids were isolated from the methanolic extract of Potentilla chinensis. Some of these compounds showed inhibitory effects on nitric oxide production in LPS-induced RAW264.7 macrophages.
BIOORGANIC CHEMISTRY
(2021)
Review
Chemistry, Organic
Yingkai Liu, Yuqing Jian, Mengru Cao, Bin Wang, Yixing Qiu, Hanwen Yuan, Xudong Zhou, Bin Li, Wenbing Sheng, Caiyun Peng, Zaiqi Zhang, Wei Wang
Summary: This review provides a comprehensive overview of the phytochemical investigations and biological activities of seco-tetracyclic and seco-pentacyclic triterpenoids discovered from 2000-2019.
MINI-REVIEWS IN ORGANIC CHEMISTRY
(2022)
Article
Plant Sciences
Huiqiang Wei, Jianghong Guo, Xiao Sun, Wenfeng Gou, Hongxin Ning, Haihua Shang, Qiang Liu, Wenbin Hou, Yiliang Li
Summary: Pomolic acid and tormentic acid were identified as potent SENP1 inhibitors, showing potential for reversing platinum-resistant ovarian cancer.
JOURNAL OF NATURAL PRODUCTS
(2022)
Article
Microbiology
Anna Dalinova, Anatoly Fedorov, Vsevolod Dubovik, Olga Voitsekhovskaja, Elena Tyutereva, Sergey Smirnov, Dmitry Kochura, Leonid Chisty, Igor Senderskiy, Alexander Berestetskiy
Summary: Ten-membered lactones demonstrate phytotoxic, antimicrobial, and fungicidal activity, with Stagonospora cirsii fungus producing phytotoxic stagonolides with high yield. The study aimed to create structurally related nonenolides and identify the structural features that affect their biological activity. The oxidation of C-7 hydroxyl group was found to be a key structural feature affecting the phytotoxicity of nonenolides, with 7S compounds showing higher phytotoxicity compared to their 7R analogues.
Article
Biochemistry & Molecular Biology
Antonio J. Leon-Gonzalez, Prudencio Saez-Martinez, Juan M. Jimenez-Vacas, Vicente Herrero-Aguayo, Antonio J. Montero-Hidalgo, Enrique Gomez-Gomez, Andres Madrona, Justo P. Castano, Jose L. Espartero, Manuel D. Gahete, Raul M. Luque
Summary: The study suggests that hydroxytyrosol (HT) and its lipophilic derivatives could be potential therapeutic tools for prostate cancer (PCa) by demonstrating their anti-proliferative and migration inhibitory effects on PCa cell lines.
Review
Biochemistry & Molecular Biology
Madalina Nistor, Dumitrita Rugina, Zorita Diaconeasa, Carmen Socaciu, Mihai Adrian Socaciu
Summary: Pentacyclic triterpenoids (TTs) are a unique family of phytochemicals that exhibit interesting properties and pharmacological effects. Some of these compounds, such as betulinic acid (BA) and betulin (B), have been extensively investigated for their potential as anticancer molecules. This review focuses on the anticancer mechanisms, structure-activity relationship, and improved efficiency of TTs when delivered via nanolipid vehicles. The use of liposomes and nanolipid complexes, particularly in conjunction with microbubbles for targeted delivery via sonoporation, opens up new avenues for enhancing the effectiveness of TTs.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Environmental Sciences
Soohyun Um, Jaeyoun Lee, Yechan Lee, Wan Namkung, Seung Hyun Kim
Summary: Five previously undescribed pentacyclic triterpenoid saponins, named pannoside A-E (1-5), were discovered from the whole plant of seashore aster. These compounds were identified as pentacyclic triterpenoids with sugar moieties and 3-hydroxybutyrate (3-HB) based on NMR, IR spectroscopic and MS data. Pannoside E (5) exhibited inhibitory activities against various cancer cell lines. These findings suggest that undiscovered secondary metabolites from halophytes could be a valuable source of bioactive compounds.
FRONTIERS IN MARINE SCIENCE
(2023)
Article
Biochemistry & Molecular Biology
Na Li, Chaobo Li, Juan Zhang, Qian Jiang, Zhaoxue Wang, Shaozhen Nie, Zhenzhen Gao, Guangyao Li, Hao Fang, Shaoda Ren, Xiaojing Li
Summary: Ovarian cancer is characterized by its high mortality rate due to the presence of cancer stem cells, which lead to treatment recurrence and metastasis. A study found that the celastrol derivative 6c showed potential inhibition against ovarian cancer cells and exhibited anti-cancer stem cell effects by inhibiting sphere formation and regulating cell surface markers. Furthermore, compound 6c also attenuated the expression of the STAT3 pathway, suggesting its role in inhibiting ovarian cancer cells.
CHEMICO-BIOLOGICAL INTERACTIONS
(2022)
Article
Chemistry, Applied
Desire Soh, Nkwengoua Ernestine, Emmanuella Marthe Tchana Satchet, Ulrich Dzo Defokou, Bernd Schneider, Vidari Giovanni, Barthelemy Nyasse
Summary: Two diterpenoids were isolated from Xylopia aethiopica fruits, and their antiproliferative activities were tested on various human tumor cells, with compound 2 showing significant activity against breast cancer cells and pulmonary adenocarcinoma cells.
NATURAL PRODUCT RESEARCH
(2022)
Article
Biochemistry & Molecular Biology
Shi-Zhou Qi, Ting Liu, Miao Wang, Xin-Xin Zhang, Yi-Ren Yang, Wen-Hua Jing, Li-Ping Long, Kai-Ru Song, Yue Jin, Hui-Yuan Gao
Summary: Most Euphorbiaceae plants are used as folk medicinal plants, but the Leptopus genus plants have not been investigated. A study found nine new phenylpropanoid-conjugated pentacyclic triterpenoids in Leptopus lolonum, which showed significant cytotoxicity against cancer cells.
BIOORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Ling Zhang, Xiao Qin, Chenlei Lian, Jieqing Liu
Summary: This paper synthesized a series of Icariside II (ICS II) derivatives and studied their structure-activity relationships (SARs). The in vitro antitumor activities against human breast cancer cell lines (MCF-7) were evaluated using Cell Counting Kit-8 (CCK-8 kit). Preliminary results showed that most derivatives exhibited good micromole level activities compared to ICS II. Among the derivatives, S27, which completely acetylated the hydroxyl of ICS II, exhibited the highest cytotoxicity with IC50 values of 0.70 +/- 0.08 mu M. Furthermore, compound S27 showed better selectivity for cancer cells over normal cells compared to ICS II. Our findings suggest that compound S27 may be a promising lead candidate drug for anticancer treatment.
BIOORGANIC & MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Hai-Qiang Wang, Shuang-Gang Ma, Dan Zhang, Yu-Huan Li, Jing Qu, Yong Li, Yun-Bao Liu, Shi-Shan Yu
Summary: Thirty new pentacyclic triterpenoids were isolated from Enkianthus chinensis, along with fourteen known triterpenoids. Compound 25 exhibited latent activity against HSV-1, while several compounds showed potent hepatoprotective effects in vitro.
BIOORGANIC CHEMISTRY
(2021)
Article
Oncology
Lilya U. Dzhemileva, Regina A. Tuktarova, Usein M. Dzhemilev, Vladimir A. D'yakonov
Summary: The search for new, effective and low-toxicity anticancer drugs is of utmost importance in modern medicinal chemistry. Pentacyclic triterpenoids are a class of biologically active compounds with diverse biological and pharmacological activities, particularly in terms of their antitumor and antiviral properties. However, their low potential for biological action, low water solubility, and unfavorable absorption and metabolism parameters pose significant challenges in their clinical use. In this study, we synthesized a series of ionic compounds based on betulinic, ursolic, and oleanolic acids to enhance the solubility and permeability of these compounds through biological membranes.
Article
Chemistry, Applied
Vanessa Rocha Machado, Amanda Virtuoso Jacques, Natalia Stefanes Marceli, Maique Weber Biavatti, Maria Claudia Santos-Silva
Summary: The study found that lupeol and some of its derivatives have cytotoxic effects on acute myeloid leukemia cells and acute lymphoid leukemia cells, with strong selectivity for leukemia cells over healthy cells. These compounds showed high blood compatibility, making them potential candidates for the development of anti-leukemic drugs that can be administered intravenously.
NATURAL PRODUCT RESEARCH
(2021)
Review
Pharmacology & Pharmacy
Mariana Matias, Adriana O. O. Santos, Samuel Silvestre, Gilberto Alves
Summary: Epilepsy is a chronic and complex neurological disease affecting approximately 50 million people worldwide. Despite the introduction of numerous new antiseizure drugs, many patients still suffer from uncontrolled seizures, necessitating the development of more effective therapies. Nanomedicine offers a promising approach to deliver drugs to the brain, enhancing their therapeutic potential. This review addresses the general features and management of epilepsy, as well as the challenges in developing better antiseizure therapies. It also discusses the role of nanomedicines in selectively delivering drugs, overcoming physical-chemical limitations, improving brain penetration, reducing adverse effects, and circumventing drug resistance.
Article
Chemistry, Multidisciplinary
Rafael F. A. Gomes, Bruno M. F. Goncalves, Kessia H. S. Andrade, Barbara B. Sousa, Nuno Maulide, Goncalo J. L. Bernardes, Carlos A. M. Afonso
Summary: A new nitrogen-rich furan compound, 3-acetamido-5-acetyl furan (3A5AF), was discovered from chitin biomass. A reactive synthon, 3-acetamido-5-furfuryl aldehyde (3A5F), was developed and demonstrated to be a source of bio-derived nitrogen-rich heteroaromatics, carbocycles, and bioconjugation reagents.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2023)
Review
Pharmacology & Pharmacy
Judite R. M. Coimbra, Paula I. Moreira, Armanda E. Santos, Jorge A. R. Salvador
Summary: This review explores the biological functions and structures of QPCT/L enzymes, highlights their therapeutic relevance, and summarizes recent developments in the discovery of small-molecule inhibitors targeting these enzymes.
DRUG DISCOVERY TODAY
(2023)
Review
Chemistry, Multidisciplinary
Pedro J. M. Sobral, Andre T. S. Vicente, Jorge A. R. Salvador
Summary: Cancer is a major cause of death, with an estimated 10 million deaths worldwide in 2020. Efforts have been made to find novel anticancer drugs with fewer side effects and greater effectiveness. Oridonin, a diterpenoid derived from Rabdosia rubescens, has shown promising anticancer properties. This mini-review highlights recent advances in oridonin derivatives as potential anticancer drugs and explores their mechanisms of action.
FRONTIERS IN CHEMISTRY
(2023)
Review
Agriculture, Dairy & Animal Science
Jessica Ribeiro, Vanessa Silva, Andreia Monteiro, Madalena Vieira-Pinto, Gilberto Igrejas, Filipa S. Reis, Lillian Barros, Patricia Poeta
Summary: Chicken meat is widely consumed around the world, and antibiotics have been used in its production to ensure high levels of output. However, the use of antibiotics in animal production has led to the emergence of antibiotic-resistant bacteria, particularly in the gut microbiota. Studies have found resistant strains of Enterococcus spp. and Escherichia coli in the gastrointestinal tract of chickens, with Enterococcus spp. showing resistance to at least seven classes of antibiotics and E. coli showing resistance to at least four. Some clonal lineages have also been identified in both broilers and humans, suggesting the transmission of bacteria through contaminated food, direct contact with animals, or environmental exposure.
Article
Agriculture, Dairy & Animal Science
Sandra Cunha, Carla Miranda, Angela Martins, Ruben Soares, Manuel Maia, Filipe Silva, Gilberto Igrejas, Patricia Poeta
Summary: This study investigated whether bovine colostrum can serve as a reservoir and vehicle for the transmission of antibiotic-resistant Enterococcus spp. The results showed the presence of antibiotic-resistant species and genes in calf colostrum, with a high percentage of multidrug-resistant isolates. This highlights the importance of hygiene measures to reduce microbial contamination of colostrum.
Article
Agriculture, Dairy & Animal Science
Ruben Soares, Carla Miranda, Sandra Cunha, Luis Ferreira, Angela Martins, Gilberto Igrejas, Patricia Poeta
Summary: The aim of this study was to assess the presence of Enterococcus species in ornamental animal feed and characterize their antimicrobial resistance and virulence factors. A total of 103 Enterococcus isolates were recovered from 57 samples of ornamental animal feed, with Enterococcus faecalis and E. faecium being the most frequently identified species. The isolates exhibited high resistance to rifampicin and erythromycin, and many were classified as multidrug-resistant. These findings highlight the public health concern of antibiotic-resistant Enterococcus spp. in ornamental animal feed and the increasing interaction between these animals and humans.
Article
Microbiology
Telma de Sousa, Michel Hebraud, Olimpia Alves, Eliana Costa, Luis Maltez, Jose Eduardo Pereira, Angela Martins, Gilberto Igrejas, Patricia Poeta
Summary: A study conducted at the Medical Center of Tras-os-Montes and Alto Douro (CHTMAD) found that Pseudomonas aeruginosa strains causing urinary tract infections are resistant to multiple antibiotics and have high biofilm formation and motility capabilities, posing a serious public health problem.
Article
Infectious Diseases
Vanessa Silva, Adriana Silva, Jessica Ribeiro, Alfredo Aires, Rosa Carvalho, Joana S. Amaral, Lillian Barros, Gilberto Igrejas, Patricia Poeta
Summary: Antimicrobial resistance is a growing global public health problem, and there is a need for new antimicrobial agents. The food industry produces bioactive by-products rich in phenolic compounds, which have antioxidant and antimicrobial properties. This study aimed to characterize the phenolic compounds in pomegranate, quince, and persimmon by-products and assess their antioxidant and antimicrobial activities.
Review
Infectious Diseases
Adriana Silva, Vanessa Silva, Jose Eduardo Pereira, Luis Maltez, Gilberto Igrejas, Patricia Valentao, Virgilio Falco, Patricia Poeta
Summary: Escherichia coli (E. coli) is an important pathogenic bacteria commonly found in livestock, serving as a carrier of drug-resistant genes between humans, animals, and the environment. The use of antimicrobials in food-producing animals, especially in the food chain, is a significant contributor to antimicrobial resistance (AMR) development and spread. This review focuses on the clonal lineages and resistance profiles of E. coli, including extended spectrum beta-lactamases (ESBL) producing E. coli, in various food-producing animals such as pigs, poultry, cattle, fish farming, and rabbits. The presence of ESBL-producing E. coli was found to be prevalent among farm animals, with high resistance rates to tetracycline and ampicillin observed in farms worldwide. There is an urgent need for a better understanding of the epidemiology of E. coli and ESBL-producing E. coli in livestock, as animal production plays a major role in the global antibiotic resistance problem, necessitating a One Health approach.
Article
Biochemistry & Molecular Biology
Tiago O. Pereira, Maryam Abbasi, Rita I. Oliveira, Romina A. Guedes, Jorge A. R. Salvador, Joel P. Arrais
Summary: In this work, a method is developed using deep reinforcement learning and attention mechanisms to predict binding affinity against a biological target and generate targeted hit compounds with consideration of stereochemical information. The study shows the importance of attention mechanisms and stereochemical information in the prediction and generation processes. By applying this method to USP7, synthesizable molecules with high biological affinity for the target are discovered, and the important regions for interaction with the receptor's active site are identified.
JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN
(2023)
Article
Pharmacology & Pharmacy
Luis Filipe, Telma de Sousa, Dario Silva, Miguel M. Santos, Manuela Ribeiro Carrott, Patricia Poeta, Luis C. Branco, Sandra Gago
Summary: The combination of active pharmaceutical ingredients in the form of ionic liquids or organic salts (API-OSILs) with mesoporous silica nanoparticles (MSNs) as drug carriers can enhance the capabilities of current antibiotics, especially against resistant strains of bacteria. In this study, three nanomaterials based on the modification of MSN surface with different ionic liquids coupled with anionic ciprofloxacin were prepared. These materials showed no cytotoxicity and exhibited improved antibacterial activity against both resistant and sensitive strains of K. pneumoniae. One particular nanomaterial, [MSN-Chol][Cip], showed significant enhancement with a tenfold decrease in MIC against sensitive strains. The importance of this study is rated at 8 out of 10 for its potential application in combating antibiotic resistance.
Article
Infectious Diseases
Madalena Santos, Raquel Santos, Pedro Soeiro, Samuel Silvestre, Susana Ferreira
Summary: This study aimed to evaluate the ability of resveratrol to modulate norfloxacin resistance in Staphylococcus aureus. The results showed that resveratrol could modulate norfloxacin resistance by inhibiting the NorA efflux pump of S. aureus.
Article
Chemistry, Medicinal
Romina A. Guedes, Jorge H. Grilo, Andreia N. Carvalho, Pedro M. P. Fernandes, Ana S. Ressurreicao, Vanessa Brito, Adriana O. Santos, Samuel Silvestre, Eleonora Gallerani, Maria Joao Gama, Riccardo Gavioli, Jorge A. R. Salvador, Rita C. Guedes
Summary: The purpose of this study was to discover novel proteasome inhibitors with anticancer activity to overcome the limitations of existing inhibitors. A structure-based virtual screening protocol was developed using the human 20S proteasome structure, and 246 compounds were selected for in vitro evaluation. Compound 4 (JHG58) was shortlisted as the best hit compound based on its proteasome inhibitory activity and ability to induce cell death. Molecular docking studies revealed its interactions with key residues at the catalytic active site.
Article
Biochemistry & Molecular Biology
Bruno M. F. Goncalves, Vanessa I. S. Mendes, Samuel M. Silvestre, Jorge A. R. Salvador
Summary: Arjunolic acid (AA) is a pentacyclic triterpenoid with promising anticancer properties. Novel AA derivatives with modifications at C-28 were designed and evaluated for their biological activity on human cancer and non-tumor cell lines. The most active derivative, compound 26, showed selectivity between malignant cells and non-malignant fibroblasts. It induced cell-cycle arrest and inhibited wound closure in PANC-1 cancer cells, and synergistically increased the cytotoxicity of Gemcitabine.
RSC MEDICINAL CHEMISTRY
(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)
