Article
Chemistry, Medicinal
Mario Saletti, Samuele Maramai, Annalisa Reale, Marco Paolino, Simone Brogi, Angela Di Capua, Andrea Cappelli, Gianluca Giorgi, Danilo D'Avino, Antonietta Rossi, Carla Ghelardini, Lorenzo Di Cesare Mannelli, Roccaldo Sardella, Andrea Carotti, Gerald Woelkart, Burkhard Klosch, Chiara Bigogno, Giulio Dondio, Maurizio Anzini
Summary: The design of compounds that selectively inhibit COX-2 and release NO is a promising strategy for developing potent anti-inflammatory agents with reduced gastrointestinal and cardiovascular toxicity. The results showed that the isosteric substitution of the ethereal oxygen atom with sulfur led to the synthesis of new selective and highly potent COX-2 inhibitors, capable of inducing vasorelaxant responses. These compounds also demonstrated significant efficacy in mouse models of inflammation and pain.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Maurizio Anzini, Mario Saletti, Samuele Maramai, Annalisa Reale, Marco Paolino, Simone Brogi, Angela Di Capua, Andrea Cappelli, Gianluca Giorgi, Danilo D'Avino, Antonietta Rossi, Carla Ghelardini, Lorenzo Di Cesare Mannelli, Roccaldo Sardella, Andrea Carotti, Gerald Woelkart, Burkhard Klosch, Chiara Bigogno, Giulio Dondio
Summary: The design of compounds that selectively inhibit COX-2 and release NO is a promising strategy for developing potent anti-inflammatory drugs with reduced gastrointestinal and cardiovascular toxicity. By substituting the oxygen atom with a sulfur atom, new selective and highly potent COX-2 inhibitors can be synthesized, capable of inducing vasorelaxation in vivo.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Multidisciplinary Sciences
Dalia E. Ali, Rania A. El Gedaily, Shahira M. Ezzat, Maged A. El Sawy, Meselhy R. Meselhy, Essam Abdel-Sattar
Summary: Plant resins from Eucalyptus trees contain bioactive compounds with high medicinal values. This study investigated the chemistry and anti-inflammatory activity of these resins and found that 1,6-dicinnamoyl-O-alpha-D-glucopyranoside (C5) showed significant inhibition against COX-2, TNF-alpha, NF-kappa B, and NO.
SCIENTIFIC REPORTS
(2023)
Review
Chemistry, Multidisciplinary
Deivasigamani Priya, Papichettypalle Gopinath, Loganathan Sumathi Dhivya, Anandan Vijaybabu, Manoharan Haritha, Senthilkumar Palaniappan, Muthu K. Kathiravan
Summary: Pyrazole derivatives have significant therapeutic potential for treating inflammation and inflammation-associated cancers, and their medicinal chemistry aspects are key to their biological activity.
Article
Biochemistry & Molecular Biology
Jignasa Savjani, Bhavesh Variya, Snehal Patel, Suja Mulamkattil, Harsh Amin, Shital Butani, Ahmed Allam, Jamaan Ajarem, Harsh Shah
Summary: This study developed a novel series of indomethacin analogues with potential anti-inflammatory properties and fewer side effects. Through various scientific approaches, the binding interactions between these analogues and COX-2 protein were evaluated, and the top-scoring complex was selected. In vitro and in vivo evaluations demonstrated that certain compounds exhibited strong COX-2 inhibition and anti-inflammatory potential without ulcerogenic liability.
Review
Chemistry, Multidisciplinary
N. Jeelan Basha
Summary: Cancer and inflammation are closely related through various pathways. Both disorders have led to millions of deaths. Key pathways responsible for inflammation and cancer include STAT3, NF-kappa B, COX, and histone acetylation, which can be targeted by medicinally potent heterocycles. Many NSAIDs, natural or synthetic, have been reported in this context. This review summarizes the molecular mechanisms of inflammation, the use of NSAIDs derived from natural sources or synthetic methods, and recent studies on potent anti-inflammatory agents known as heterocycles and their significance in cancer treatment. Literature for the study covers the period from 2019 to 2022.
Review
Biochemistry & Molecular Biology
Jiahua Cui, Jinping Jia
Summary: COX-2 is a key enzyme in the inflammatory process, and natural COX-2 inhibitors have been reported to have anti-inflammatory effects and benefits against cell injury. Understanding the characteristics of natural COX-2 inhibitors paves the way for the development of more potent and selective inhibitors in the future.
CURRENT MEDICINAL CHEMISTRY
(2021)
Article
Plant Sciences
Nada Elhefni, Sherif S. S. Ebada, Marwa M. M. Abdel-Aziz, El-Sayed M. Marwan, Saleh El-Sharkawy, Mona El-Neketi
Summary: Date palm waste from Egypt can be used to produce compounds with anti-Helicobacter pylori and anti-inflammatory activities, including a new sesquiterpene lactone derivative (phodactolide A) and other known compounds.
PHARMACEUTICAL BIOLOGY
(2023)
Article
Medicine, General & Internal
Foong Way David Tai, Mark E. McAlindon
Summary: NSAIDs are commonly used for treatment, but can cause a variety of gastrointestinal symptoms, which can be reduced by limiting their use or co-administering with proton pump inhibitors (PPIs) to reduce associated complications.
Review
Pharmacology & Pharmacy
Zhiran Ju, Menglan Li, Junde Xu, Daniel C. Howell, Zhiyun Li, Fen-Er Chen
Summary: Cyclooxygenases play a vital role in inflammation, but currently used anti-inflammatory drugs have associated adverse effects. Researchers are searching for novel selective COX-2 inhibitors.
ACTA PHARMACEUTICA SINICA B
(2022)
Article
Biochemistry & Molecular Biology
Fedora Grande, Francesca Giordano, Maria Antonietta Occhiuzzi, Carmine Rocca, Giuseppina Ioele, Michele De Luca, Gaetano Ragno, Maria Luisa Panno, Bruno Rizzuti, Antonio Garofalo
Summary: This study compared the interaction of two prodrugs and their active metabolite with the COX binding site, and assessed their potential as antiproliferative agents through cytotoxicity, cytofluorimetry, and protein expression assays. Encouraging results suggest that the compounds could act not only as precursors of the anti-inflammatory metabolite, but also as direct antiproliferative agents.
Article
Biochemistry & Molecular Biology
Sulaksha R. Desai, Vidya G. Desai, Raghuvir R. Pissurlenkar
Summary: In this study, a series of azomethine derivatives were synthesized and their anti-inflammatory potency was investigated. Computational docking studies showed better affinity of the compounds towards COX-2 compared to COX-1, with compounds 4a, 4d, and 4k exhibiting the best binding. In vitro inhibition assays confirmed that the synthesized compounds had less inhibition on COX-1 enzyme than COX-2 enzyme. Compound 4d showed the highest inhibition of inflammation in in-vivo screening. The compounds also demonstrated good antioxidant properties but minimal cytotoxicity on cancer cells.
BIOORGANIC CHEMISTRY
(2022)
Article
Biology
Lin Ding, Sisi Wu, Yaqi Shen, Xuemei Hu, Daoyu Hu, Ihab Kamel, Zhen Li
Summary: CT texture analysis can provide valuable information for the differential diagnosis of primary gastrointestinal lymphoma and gastrointestinal adenocarcinoma, serving as a potential adjunct tool in clinical practice.
Article
Biochemistry & Molecular Biology
Mohamed M. S. Hamoud, Nermine A. Osman, Samar Rezq, Hend A. A. Abd El-wahab, Abdalla E. A. Hassan, Hanan A. Abdel-Fattah, Damian G. Romero, Amany M. Ghanim
Summary: By synthesizing and evaluating two series of 1,3,4-oxadiazole and 1,2,4-triazole derivatives, this study discovered their potential anti-inflammatory and antioxidant activity, highlighting them as potential novel therapeutic agents for inflammation and oxidative stress-related diseases.
BIOORGANIC CHEMISTRY
(2022)
Article
Medicine, General & Internal
Dong Jun Oh, Hyuk Yoon, Hyun Soo Kim, Yoon Jin Choi, Cheol Min Shin, Young Soo Park, Nayoung Kim, Dong Ho Lee, You-Jung Ha, Eun Ha Kang, Yun Jong Lee, Nayoung Kim, Ki-Jeoung Kim, Fei Liu
Summary: This study found that in patients requiring long-term NSAID use, rebamipide appeared to be more effective than proton pump inhibitors in preventing small intestine damage and had fewer side effects.
KOREAN JOURNAL OF INTERNAL MEDICINE
(2022)
Article
Pharmacology & Pharmacy
Harilal Patel, Prakash Patel, Nirav Modi, Shaival Shah, Ashok Ghoghari, Bhavesh Variya, Ritu Laddha, Dipesh Baradia, Nitin Dobaria, Pavak Mehta, Nuggehally R. Srinivas
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2017)
Article
Pharmacology & Pharmacy
Anita K. Bakrania, Bhavesh C. Variya, Lalaji V. Rathod, Snehal S. Patel
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
(2018)
Article
Pharmacology & Pharmacy
Anita K. Bakrania, Bhavesh C. Variya, Snehal S. Patel
PHARMACOLOGICAL REPORTS
(2018)
Article
Medicine, Research & Experimental
Bhavesh C. Variya, Anita K. Bakrania, Yuanli Chen, Jihong Han, Snehal S. Patel
BIOMEDICINE & PHARMACOTHERAPY
(2018)
Review
Biochemistry & Molecular Biology
Volatiana Rakotoarivelo, Bhavesh Variya, Subburaj Ilangumaran, Marie-France Langlois, Sheela Ramanathan
CYTOKINE & GROWTH FACTOR REVIEWS
(2018)
Article
Medicine, Legal
Bhavesh C. Variya, Anita K. Bakrania, Prem Madan, Snehal S. Patel
REGULATORY TOXICOLOGY AND PHARMACOLOGY
(2019)
Article
Plant Sciences
Bhavesh C. Variya, Anita K. Bakrania, Snehal S. Patel
Article
Biochemistry & Molecular Biology
Md Gulam Musawwir Khan, Amit Ghosh, Bhavesh Variya, Madanraj Appiya Santharam, Rajani Kandhi, Sheela Ramanathan, Subburaj Ilangumaran
Article
Oncology
Md Gulam Musawwir Khan, Amit Ghosh, Bhavesh Variya, Madanraj Appiya Santharam, Awais Ullah Ihsan, Sheela Ramanathan, Subburaj Ilangumaran
Article
Biochemistry & Molecular Biology
Udit J. Chaube, Rakesh Rawal, Abhishek B. Jha, Bhavesh Variya, Hardik G. Bhatt
Summary: Lung cancer is a prevalent cancer worldwide, with issues of drug potency and resistance being major concerns. Research has identified mTOR as an important alternative target for treatment, with compounds like HB-UC-1 and HB-UC-5 showing promising inhibitory effects on mTOR activity in both cell-based and in vivo studies.
BIOORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Jignasa Savjani, Bhavesh Variya, Snehal Patel, Suja Mulamkattil, Harsh Amin, Shital Butani, Ahmed Allam, Jamaan Ajarem, Harsh Shah
Summary: This study developed a novel series of indomethacin analogues with potential anti-inflammatory properties and fewer side effects. Through various scientific approaches, the binding interactions between these analogues and COX-2 protein were evaluated, and the top-scoring complex was selected. In vitro and in vivo evaluations demonstrated that certain compounds exhibited strong COX-2 inhibition and anti-inflammatory potential without ulcerogenic liability.
Article
Anatomy & Morphology
Rajani Kandhi, Bhavesh Variya, Sheela Ramanathan, Subburaj Ilangumaran
Summary: This article describes an efficient method for isolating intrahepatic leukocytes from mice fed with high fat diet and proposes a strategy to alleviate autofluorescence during phenotyping by multicolor flow cytometry. The article also introduces a gating strategy for robust identification of different immune cell subsets. These procedures allow simultaneous processing of multiple samples and ensure reliable cell isolation and noise reduction for reliable characterization of intrahepatic leukocytes from fatty liver tissues.
ANATOMICAL RECORD-ADVANCES IN INTEGRATIVE ANATOMY AND EVOLUTIONARY BIOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Nikum D. Sitwala, Vivek K. Vyas, Bhavesh C. Variya, Snehal S. Patel, Chirag C. Mehta, Dharmraj N. Rana, Manjunath D. Ghate
BIOORGANIC CHEMISTRY
(2017)
Article
Biology
Anita K. Bakrania, Surender Nakka, Bhavesh C. Variya, Prabodh V. Shah, Snehal S. Patel
INDIAN JOURNAL OF EXPERIMENTAL BIOLOGY
(2017)