Article
Environmental Sciences
Mohamed Hussain Syed, Ananthan Gnanakkan, Sivaperumal Pitchiah
Summary: This study investigated the analgesic, anti-inflammatory, and anti-pyretic activities ofPhallusia nigra. Results showed potential biomedical applications of the extracts, with acetonitrile fraction II showing higher analgesic response. The extracts also demonstrated potential to reduce edema induced by carrageenan in a time-dependent manner.
ENVIRONMENTAL SCIENCE AND POLLUTION RESEARCH
(2021)
Article
Biochemistry & Molecular Biology
Bilal Aslam, Asif Hussain, Muhammad Usman Bari, Muhammad Naeem Faisal, Zia ud Din Sindhu, Rasha Alonaizan, Rasha K. Al-Akeel, Shabana Naz, Rifat Ullah Khan
Summary: This study evaluated the in vivo effects of meloxicam and curcumin co-encapsulated PLGA nanoparticles in acute models of pyrexia, nociception, and inflammation. The results showed that PLGA encapsulation significantly improved the in vivo activities of both compounds, and co-encapsulation of meloxicam and curcumin enhanced their anti-pyretic, anti-nociceptive, and anti-inflammatory effects in a dose-dependent manner. Therefore, the combination of meloxicam and curcumin in a biodegradable nanocarrier system could provide a promising therapeutic approach for acute conditions.
Article
Chemistry, Applied
Marwa Zekrallah, Mahmoud M. Mashaly, Mona Saif, Rania Fouad
Summary: This study fabricates and analyzes the newly synthesized Cu(AHC)(2) complex to investigate its biological functionalities including cytotoxicity, DNA binding, and DNA cleavage. The results show that the Cu(AHC)(2) complex exhibits excellent cytotoxicity against HepG-2 cell line and strongly binds to DNA through intercalative mode, with the ability to destroy DNA.
APPLIED ORGANOMETALLIC CHEMISTRY
(2023)
Article
Pharmacology & Pharmacy
Shahbaz Irshad, Irfan Anjum, Muhammad Naveed Mushtaq, Kalim Ullah, Kashif Barkat, Muhammad Nasir Hayat Malik, Muhammad Ahmer Raza, Muhammad Zubair
Summary: This study confirmed the anti-inflammatory, analgesic, and antipyretic properties of Fagonia bruguieri, which may be attributed to the presence of various phyto-constituents.
PAKISTAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2022)
Article
Biochemistry & Molecular Biology
Arun Kumar Subramani, Amuthalakshmi Sivaperuman, Ramalakshmi Natarajan, Richie R. Bhandare, Afzal B. Shaik
Summary: This study utilized computational methods to analyze, design, and test compounds with potential anticancer activity, aiming to accelerate the development of new anti-breast cancer drugs.
Article
Biochemistry & Molecular Biology
Sulaiman Sulaiman, Shabir Ahmad, Syeda Sohaila Naz, Sara Qaisar, Sayyar Muhammad, Amal Alotaibi, Riaz Ullah
Summary: In this study, copper oxide nanoparticles were successfully synthesized and used as nanocarriers for etoricoxib and montelukast in combination therapy. The nanoparticles were characterized using various techniques and the nanoformulations showed high activity in vitro and in vivo. The results suggest that the nanoformulations have potential clinical applications in inhibiting inflammation, pain, and fever.
Article
Plant Sciences
Fiaz Alam, Muhammad Hanif, Asad ur Rahman, Sayyad Ali, Saeed Jan
Summary: The study evaluated the analgesic, antipyretic, and anti-inflammatory properties of Gaultheria trichophylla extract and salicylate-rich fraction in vivo, in vitro, and in silico. The results showed significant effects, supporting the traditional medicinal use of these components.
JOURNAL OF ETHNOPHARMACOLOGY
(2023)
Article
Multidisciplinary Sciences
Sulaiman Sulaiman, Shabir Ahmad, Syeda Sohaila Naz, Sara Qaisar, Sayyar Muhammad, Riaz Ullah, Mohammad Khalid Al-Sadoon, Aneela Gulnaz
Summary: The study describes the synthesis of a novel low dose PVA capped ET and MT conjugated ZnO nanomaterials with potential anti-inflammatory, analgesic and antipyretic properties. The nanomaterials showed higher anti-inflammatory and analgesic activity compared to the drugs (ET and MT), and similar antipyretic activity but more potent on a weight basis. The acute toxicity study demonstrated a wide therapeutic window. The findings suggest that the novel nanomaterials could be promising agents for pain relief, reducing inflammation, and treating fever.
JOURNAL OF KING SAUD UNIVERSITY SCIENCE
(2022)
Article
Integrative & Complementary Medicine
Tabinda Azim, Muhammad Wasim, Muhammad Shoaib Akhtar, Irfan Akram
Summary: The study showed that triazole derivatives exhibited promising anti-inflammatory, analgesic, and antipyretic effects with no signs of toxicity in mice. Further research is needed to explore their potential molecular mechanisms of action and for structural modifications.
BMC COMPLEMENTARY MEDICINE AND THERAPIES
(2021)
Article
Plant Sciences
Rahma Hamayun, Muhammad Shahid Iqbal, Muhammad Imran Qadir
Summary: The study evaluated the analgesic, anti-inflammatory, and antipyretic activities of Malva neglecta extracts in Swiss albino mice, demonstrating significant effects in reducing pain, inflammation, and fever in the experimental models.
BANGLADESH JOURNAL OF BOTANY
(2021)
Article
Chemistry, Inorganic & Nuclear
P. Jyothi, V. Sumalatha, D. Rajitha
Summary: Three Co(II) complexes were synthesized and characterized, showing good DNA binding, antimicrobial, and anticancer activities.
INORGANIC CHEMISTRY COMMUNICATIONS
(2022)
Article
Pharmacology & Pharmacy
Yongsheng Liu, Shan Su, Moxi Yu, Dongshen Zhai, Yachen Hou, Hui Zhao, Xue Ma, Min Jia, Xiaoyan Xue, Mingkai Li
Summary: The study reveals that the pyrancoumarin derivative LP4C inhibits MRSA biofilm formation by targeting the de novo pyrimidine synthesis pathway and attenuating the virulence of MRSA through inhibiting the expression of enzymes involved in the pathway.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Yanhong Liu, Linsheng Zhang, Maochao Guo, Liu Chen, Baixing Wu, Hongda Huang
Summary: The study reveals that phages have evolved Aca1 and Aca2 proteins to inhibit host CRISPR-Cas systems by binding to acr-aca promoters. The structural basis for the repression roles of Aca proteins is elucidated, shedding light on the repression roles of other Aca family proteins and the autoregulation roles of acr-aca operons.
JOURNAL OF BIOLOGICAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Abdallah M. Alfayomy, Salah A. Abdel-Aziz, Adel A. Marzouk, Montaser Sh. A. Shaykoon, Atsushi Narumi, Hiroyuki Konno, Sahar M. Abou-Seri, Fatma A. F. Ragab
Summary: Two new series of 1,3,4-oxadiazole and coumarin derivatives based on pyrimidine-5-carbonitrile scaffold were synthesized and evaluated for their COX-1/COX-2 inhibitory activity. Some compounds showed potent COX-2 inhibition and in vivo anti-inflammatory activity, with certain derivatives displaying superior efficacy and safety profile compared to the reference drug celecoxib. Molecular docking studies indicated similar binding interactions of select compounds 10c, 10j, and 14e as selective COX-2 inhibitors, with a higher potential for accessing the selectivity side pocket.
BIOORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Eman A. Fayed, Eman S. Nosseir, Ahmed Atef, Samar A. El-Kalyoubi
Summary: This study synthesized several novel coumarin derivatives with antimicrobial activity and tested them against various bacteria and fungi. The results showed that most of the newly synthesized compounds exhibited moderate to high activity, with the top four compounds inhibiting DNA gyrase and topoisomerase IV, interfering with cell division. In silico studies were also performed on the most active compounds, showing promising results.
MOLECULAR DIVERSITY
(2022)
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)