Article
Multidisciplinary Sciences
Katherine Sattler, Ibrahim El-Battrawy, Lukas Cyganek, Siegfried Lang, Huan Lan, Xin Li, Zhihan Zhao, Jochen Utikal, Thomas Wieland, Martin Borggrefe, Xiaobo Zhou, Ibrahim Akin
Summary: Recent evidence shows the important role of the TRPV1 channel in the cardiovascular system and its association with inflammation. Experimental results demonstrate that TRPV1 mediates LPS-induced inflammation in cardiomyocytes, leading to changes in cellular electrophysiology. Further studies are needed to investigate the underlying pathways and clinical applications of these findings.
SCIENTIFIC REPORTS
(2021)
Article
Immunology
Murat Cakir, Furkan Yuksel, Mahmud Mustafa Ozkut, Merve Durhan, Emin Kaymak, Suat Tekin, Yilmaz Cigremis
Summary: This study investigated the effects of TRPV1 agonist capsaicin and antagonist capsazepine on an AD model induced by OKA. The results showed that capsaicin could reverse the pathological changes of neurodegeneration, neuroinflammation, and deterioration in spatial memory caused by ICV OKA administration.
INTERNATIONAL IMMUNOPHARMACOLOGY
(2023)
Article
Pharmacology & Pharmacy
Mircea Iftinca, Manon Defaye, Christophe Altier
Summary: TRPV1 is a significant channel in pain perception and its agonists are being studied for chronic pain management. While TRPV1 antagonists have limited clinical use due to side effects, capsaicin offers a potential avenue for long-lasting pain relief by defunctionalising nociceptors. The development of TRPV1-targeted drugs could provide a new generation of analgesics for various pain conditions.
Article
Biochemistry & Molecular Biology
Md. Mahbubur Rahman, Hyun Jung Jo, Chul-Kyu Park, Yong Ho Kim
Summary: The effects of Diosgenin, a botanical steroidal saponin, on nociception were investigated in this study. It was found that Diosgenin reduced capsaicin-induced pain behavior and thermal hyperalgesia in mice, possibly through antagonism of TRPV1 and suppression of inflammation in the DRG. The study also revealed that Diosgenin inhibited capsaicin-induced calcium currents in DRG and CHO cells.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Review
Biochemistry & Molecular Biology
Arpad Szallasi
Summary: Today's sedentary lifestyle and poor dietary habits contribute to the increasing prevalence of hypertension, a major risk factor for stroke. Recent research suggests that the activation of TRPV1 receptor by capsaicin, a compound found in chili peppers, can lower blood pressure and potentially be a therapeutic target for hypertensive patients. However, the mechanism of action of capsaicin on blood pressure regulation is more complex than previously understood. Further studies are needed to explore the potential benefits of TRPV1-targeting drugs in treating hypertension.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Suk-Yun Kang, Su Yeon Seo, Se Kyun Bang, Seong Jin Cho, Kwang-Ho Choi, Yeonhee Ryu
Summary: This study demonstrated that intrathecal administration of the TRPV1 antagonist capsazepine significantly reduced carrageenan-induced inflammatory pain in mice, potentially through the inhibition of NMDA receptor phosphorylation.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Chemistry, Medicinal
Jin Mi Kang, Sun Ok Kwon, Jihyae Ann, Sunho Lee, Changhoon Kim, Nayeon Do, Jin Ju Jeong, Peter M. Blumberg, Heejin Ha, Thi Ngoc Lan Vu, Sanghee Yoon, Sun Choi, Robert Frank-Foltyn, Bernhard Lesch, Gregor Bahrenberg, Hannelore Stockhausen, Thomas Christoph, Jeewoo Lee
Summary: The series of 117 2-(halogenated phenyl) acetamide and propanamide analogs were investigated as TRPV1 antagonists, with halogenated phenyl A-region analogs showing a broad functional profile. Antagonists 28 and 92 exhibited potent antagonism against capsaicin for hTRPV1, with antagonist 92 displaying promising analgesic activity in vivo. Molecular modeling of compound 92 suggested that the two fluoro groups in the A-region interacted hydrophobically with the receptor.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2021)
Review
Pharmacology & Pharmacy
Vipin Arora, James N. Campbell, Man-Kyo Chung
Summary: Capsaicin, the pungent ingredient in chili peppers, can cause intense burning pain in humans, but it has also been used as an analgesic for chronic pain conditions. The analgesic effects of capsaicin depend on concentration, with low concentrations inducing short-term defunctionalization and high concentrations leading to long-term defunctionalization.
PHARMACOLOGY & THERAPEUTICS
(2021)
Article
Chemistry, Medicinal
Qianqian Liang, Zhen Qiao, Qiqi Zhou, Dengqi Xue, KeWei Wang, Liming Shao
Summary: This study reports the synthesis of N-indazole-4-aryl piperazine carboxamide analogues as TRPV1 modulators. Compound 28 is identified as a potent and selective TRPV1 agonist, relieving inflammatory and thermal pain by desensitizing the native TRPV1 current in mice. The study also reveals an important hydrogen interaction between Arg557 and the indazole of compound 28.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Review
Physiology
Shtaywy S. S. Abdalla, Amani A. A. Harb, Ihab M. M. Almasri, Yasser K. K. Bustanji
Summary: Transient receptor potential vanilloid 1 (TRPV1) is a highly permeable ion channel that regulates lipid metabolism and is a potential therapeutic target for disorders such as hyperlipidemia. This review explores the role of TRPV1 in hyperlipidemia-associated metabolic syndrome and summarizes the molecular mechanisms underlying its regulatory effects on lipid metabolism. It also discusses the reciprocal modulation between TRPV1 and lipids, as well as the modulation of TRPV1 activity by different lipid classes.
FRONTIERS IN PHYSIOLOGY
(2022)
Article
Multidisciplinary Sciences
Tina Blazevic, Cosmin I. Ciotu, Markus Gold-Binder, Elke H. Heiss, Michael J. M. Fischer, Verena M. Dirsch
Summary: Capsaicin, an active compound of chili peppers, can inhibit platelet-derived growth factor-induced proliferation in primary rat vascular smooth muscle cells (VSMCs), possibly through a role of TRPV1. However, commercially available antibodies were ineffective in detecting TRPV1 expression. Moreover, TRPV1 agonists did not increase intracellular calcium levels in VSMCs. RT-qPCR results showed low TRPV1 expression in VSMCs, suggesting the absence of canonical TRPV1 channel activity.
Review
Biochemistry & Molecular Biology
Arpad Szallasi
Summary: Resiniferatoxin (RTX) is a potent analgesic with a wide range of pharmacological actions. Targeted RTX therapy shows promise in cancer pain management and treatment of knee pain in patients with osteoarthritis.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Multidisciplinary Sciences
Manae Tatsumi, Takayuki Kishi, Satoru Ishida, Hiroki Kawana, Akiharu Uwamizu, Yuki Ono, Kouki Kawakami, Junken Aoki, Asuka Inoue
Summary: A method previously used for detecting GPCR activation has been shown to also detect TRP channel activation. The method is simple, low-cost, and only requires an absorbance microplate reader. Using substrates of ADAM10, such as EGF and BTC, improves the specificity of the assay.
Article
Medicine, Research & Experimental
Ben Katz, Rachel Zaguri, Simon Edvardson, Channa Maayan, Orly Elpeleg, Shaya Lev, Elyad Davidson, Maximilian Peters, Shlomit Kfir-Erenfeld, Esther Berger, Shifa Ghazalin, Alexander M. Binshtok, Baruch Minke
Summary: This study provides direct evidence in humans for pain-related functional changes linked to TRPV1, a potential target in the development of pain relievers. Two individuals carrying a homozygous missense mutation in TRPV1 demonstrated insensitivity to heat stimulation, elevated pain thresholds, and abnormal responses to a TRPA1 channel activator. These findings highlight the importance of TRPV1 in pain modulation and may contribute to the development of novel pain therapies.
JOURNAL OF CLINICAL INVESTIGATION
(2023)
Article
Biochemistry & Molecular Biology
Ariana Hudita, Bianca Galateanu, Marieta Costache, Carolina Negrei, Rodica-Mariana Ion, Lorena Iancu, Octav Ginghina
Summary: This study investigated the therapeutic effects of alginate-microencapsulated capsaicin on neuropathic pain, revealing that this new formulation has lower cytotoxic effects, significant improvements in cell morphology and oxidative stress status, and can alter the expression profile of inflammatory cytokines compared to the control group.
Article
Environmental Sciences
Gopal Krishna, Rabi N. Sahoo, Prafull Singh, Himesh Patra, Vaishangi Bajpai, Bappa Das, Sudhir Kumar, Raju Dhandapani, Chandrapal Vishwakarma, Madan Pal, V. Chinnusamy
Summary: This study investigated the response of different rice genotypes to water deficit stress using thermal imaging, visible imaging, RWC, and CWSI, and identified drought-tolerant and drought-resistant genotypes. Effective relationships between RWC and CWSI, as well as canopy reflectance spectra and CWSI, were established, with 10 optimal wavebands related to water deficit stress identified. This research contributes to the quick detection of water deficit stress in crops and can aid in the development of drought-tolerant rice genotypes in the future.
GEOCARTO INTERNATIONAL
(2021)
Article
Multidisciplinary Sciences
Shovan Dogra, Madhumangal Pal
Summary: This paper introduces the concept of picture fuzzy subring of a crisp ring and studies some basic results. The properties of picture fuzzy subring under classical ring homomorphism are also investigated.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES INDIA SECTION A-PHYSICAL SCIENCES
(2021)
Article
Chemistry, Organic
G. Dhananjaya, Akula Raghunadh, P. Mahesh Kumar, S. Pulla Reddy, V. Narayana Murthy, Venkateswara Rao Anna, Manojit Pal
Summary: Polyhydroquinolines were synthesized via Hantzsch's multicomponent reaction using urea as an effective ammonia surrogate under green conditions. The reaction afforded a range of products depending on the nature of reaction conditions employed.
LETTERS IN ORGANIC CHEMISTRY
(2021)
Review
Biochemistry & Molecular Biology
Gangireddy Sujeevan Reddy, Manojit Pal
Summary: The indole framework is highly valued in medicinal chemistry for its ability to bind with receptors or proteins and its anti-tubercular properties. Recent studies have shown the inhibition of Mycobacterium tuberculosis by the gut microbiota metabolite indole propionic acid (IPA), highlighting the potential for new TB treatments.
CURRENT MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Mandava Venkata Basaveswara Rao, Bodapati Veera Durga Rao, Suryadevara Vijaya Vardhini, A. V. D. Nagendra Kumar, Dhilli Rao Gorja, Ravikumar Kapavarapu, Manojit Pal
Summary: This study focused on exploring N-(2-methoxyphenyl) substituted pyrazoles and related derivatives as potential cytotoxic agents, which were conveniently prepared via a sonochemical method. Compound 3c showed promising growth inhibition of MDAMB-231 and MCF-7 cell lines, and inhibition of SIRT1 in vitro, indicating its potential as a hit molecule for further research.
Review
Chemistry, Analytical
Sagnik Das, Subhajit Mojumder, Debdulal Saha, Mrinal Pal
Summary: In this review, the significant effects of various parameters on the sensing behavior of semiconductor metal oxide (SMO) based chemiresistive gas sensors have been discussed in detail. The study systematically reviewed the impact of different material and operating condition aspects on the gas sensing performance of SMO sensors. The importance of long-term stability and high-throughput synthesis techniques in practical applications was emphasized, and the future prospects of SMO-based sensors in personalized healthcare were briefly outlined.
SENSORS AND ACTUATORS B-CHEMICAL
(2022)
Article
Chemistry, Organic
Sailaja Garrepalli, Ramesh Gudipati, Kunta Ravindhranath, Manojit Pal
Summary: This article presents new synthetic methods for the enantiomer (4S, 12aR) and ethoxy acetamide, as well as an environmentally friendly alternative for the synthesis of impurity B. The synthesized impurities were characterized and analyzed, confirming the feasibility and suitability of the developed methods.
POLYCYCLIC AROMATIC COMPOUNDS
(2023)
Article
Chemistry, Physical
Tanushri Das, Subhajit Mojumder, Sonam Chakraborty, Debdulal Saha, Mrinal Pal
Summary: Pure and Sn-doped Bismuth Ferrite (BFO) nanoparticles were synthesized and their gas sensing properties towards formaldehyde were investigated. The Sn-doped BFO nanoparticles showed enhanced formaldehyde sensing performance, with high selectivity and fast response/recovery time. The detection limit of the prepared sensors was low, making them a potential candidate for monitoring formaldehyde in indoor and outdoor air quality.
APPLIED SURFACE SCIENCE
(2022)
Article
Materials Science, Ceramics
Sonam Chakraborty, Nirman Chakraborty, Swastik Mondal, Mrinal Pal
Summary: This study reports the efficient photocatalytic degradation of methyl blue dye using Sn-doped bismuth ferrite nanoparticles under visible light. The 1.5% Sn-doped BFO nanoparticles exhibited the highest photocatalytic activity, degrading 70% of the dye within 10 minutes of visible light irradiation. These nanoparticles also showed potential for degrading another important contaminant, RhB.
CERAMICS INTERNATIONAL
(2022)
Article
Chemistry, Analytical
Subhajit Mojumder, Tanushri Das, Sagnik Das, Nirman Chakraborty, Debdulal Saha, Mrinal Pal
Summary: This study presents a highly sensitive and selective Al and Y co-doped ZnO nanopowder sensor for detecting trace ethanol in exhaled breath. The sensor exhibits rapid response and recovery time, good repeatability, and long-term stability, as well as excellent selectivity towards ethanol. It has the potential to be used for detecting liver problems and for breathalyzer testing in cases of drunken driving.
SENSORS AND ACTUATORS B-CHEMICAL
(2022)
Article
Chemistry, Multidisciplinary
Snehasis Mishra, Kaustav Das, Sujan Chatterjee, Panchanan Sahoo, Sudip Kundu, Mrinal Pal, Asim Bhaumik, Chandan Kumar Ghosh
Summary: Carbon dots (CQDs) with tunable fluorescence emission and excitation, high water solubility, good photostability, and biocompatibility are considered promising for tumor theranostics. This study focused on the synthesis and characterization of highly fluorescent CQDs from orange juice. CQD/Ag heterostructures were also synthesized and their photostability and characterization were investigated. Cellular toxicity measurements were conducted to select the superior CQD/Ag heterostructure in the human colorectal carcinoma (HCT 116) cell line, along with the observation of cell death signaling through the ROS-dependent mitochondrial-mediated pathway.
Article
Chemistry, Multidisciplinary
Monalisa Adhikari, Sagnik Das, Dipankar Chattopadhyay, Debdulal Saha, Mrinal Pal
Summary: Recently, there has been significant interest in the precise detection of VOCs, especially acetone, ammonia, and alcohol, due to their importance in industrial safety, environmental monitoring, and human health. This article reports on a chemiresistive sensor based on polypyrrole nanotubes (PPNT) for the selective detection of trace acetone vapor at room temperature. The PPNT sensor demonstrated a high response to trace acetone vapor with a low detection limit and quick response and recovery times.
Article
Chemistry, Multidisciplinary
Narender Addu, Hinuja Miriyala, Ravikumar Kapavarapu, Sunder Kumar Kolli, Manojit Pal
Summary: The synthesis of spiroindoline-3,2'-quinazoline derivatives using Wang-OSO3H as a catalyst and their evaluation against MtbCM (Mycobacterium tuberculosis Chorismate Mutase) in silico and in vitro are reported. The docking studies revealed the binding of these compounds on the external surface pockets of the MtbCM active site cavity.
Article
Chemistry, Multidisciplinary
Gangireddy Sujeevan Reddy, Sharda Shukla, Harshavardhan Bhuktar, Kazi Amirul Hossain, Rebecca Kristina Edwin, Varadaraj Bhat Giliyaru, Parimal Misra, Manojit Pal
Summary: In this study, structurally similar benzofuran derivatives were designed and evaluated for their inhibitory activity against chorismate mutase. The molecules showed strong interactions with the target enzyme and were synthesized in high yields. Three compounds exhibited promising inhibition in vitro and could be of interest in the development of new anti-tubercular agents.
Article
Chemistry, Multidisciplinary
Sagnik Das, Uttam K. Ghorai, Rajib Dey, Chandan K. Ghosh, Mrinal Pal
Summary: This study reports the achievement of highly reproducible, stable, and intense white phosphorescence from phase-pure zinc oxide nanopowder synthesized by a simple, low temperature process. The white light emission has appreciable quantum yield and cool/near cool correlated color temperature, making it suitable for W-LED applications. The presence of zinc interstitial and oxygen interstitial defects responsible for the white phosphorescence was confirmed, and a defect chemistry-based thermodynamic interpretation was proposed to explain the white emission adequately.
NEW JOURNAL OF CHEMISTRY
(2022)