Pharmaceuticals最新文献

{"title":"Multifunctionality and Possible Medical Application of the BPC 157 Peptide-Literature and Patent Review.","authors":"Michalina Józwiak, Marta Bauer, Wojciech Kamysz, Patrycja Kleczkowska","doi":"10.3390/ph18020185","DOIUrl":"10.3390/ph18020185","url":null,"abstract":"<p><p>BPC 157, known as the \"Body Protection Compound\", is a pentadecapeptide isolated from human gastric juice that demonstrated its pleiotropic beneficial effects in various preclinical models mimicking medical conditions, such as tissue injury, inflammatory bowel disease, or even CNS disorders. Unlike many other drugs, BPC 157 has a desirable safety profile, since only a few side effects have been reported following its administration. Nevertheless, this compound was temporarily banned by the World Anti-Doping Agency (WADA) in 2022 (it is not currently listed as banned by the WADA). However, it has not been approved for use in standard medicine by the FDA and other global regulatory authorities due to the absence of sufficient and comprehensive clinical studies confirming its health benefits in humans. In this review, we summarize information on the biological activities of BPC 157, with particular reference to its mechanism of action and probable toxicity. This generated the attention of experts, as BPC 157 has been offered for sale on many websites. We also present recent interest in BPC 157 as reflected in a number of patent applications and granted patents.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 2","pages":""},"PeriodicalIF":4.3,"publicationDate":"2025-01-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11859134/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143503558","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Aging Reduces ATP-Binding Cassette Transporter Expression in Brain Microvessels of Mice.","authors":"Yukiyo Wada, Masaki Inoko, Kanako Ishihara, Karin Fukumoto, Yuya Tsurudome, Michiko Horiguchi, Akio Fujimura, Kentaro Ushijima","doi":"10.3390/ph18020191","DOIUrl":"10.3390/ph18020191","url":null,"abstract":"<p><p><b>Background:</b> ATP-binding cassette (ABC) transporters are expressed in the vascular walls of brain capillaries and remove toxic chemicals from the brain. The expression of ABC transporters in peripheral organs is transcriptionally regulated by clock genes and exhibits 24 h periodic fluctuations. In addition, clock gene outputs diminish with aging. In this study, we evaluated whether the expression of ABC transporters in the blood-brain barrier (BBB) of young mice had a 24 h cycle, and whether the expression of ABC transporters in the BBB decreased with age. <b>Methods:</b> Brain microvascular (BMV) fractions from the cerebral cortex of male C57BL/6J mice were prepared using dextran. BMV fractions from young mice (12 weeks old) were prepared every four hours to evaluate 24 h rhythmicity. BMV fractions from both young and aged mice (85 weeks old) were prepared when protein expression peaked (Zeitgeber Time 5). Protein and mRNA expression of ABC transporters in BMV fractions were measured. <b>Results:</b> In young mice, protein expression of P-glycoprotein, breast cancer resistance protein, and multidrug resistance protein 4 showed time-dependent variations with a peak in the light phase (Zeitgeber Time 5); mRNA expression showed no time-dependent variation. The protein expression of these transporters was lower in the BBB of aged mice than in that of young mice, although mRNA expression did not differ between young and aged mice. <b>Conclusions:</b> ABC transporter protein expression levels in BMV endothelial cells decreased with aging; however, mRNA levels did not change, which suggests changes in protein expression did not result from diminished clock gene output. Further studies are needed to elucidate the mechanisms by which ABC transporter expression in the BBB decreases with aging.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 2","pages":""},"PeriodicalIF":4.3,"publicationDate":"2025-01-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11859312/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143502841","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"<i>Alternaria alternata</i> (Fr) Keissl Crude Extract Inhibits HIV Subtypes and Integrase Drug-Resistant Strains at Different Stages of HIV Replication.","authors":"Darian Naidu, Ernest Oduro-Kwateng, Mahmoud E S Soliman, Sizwe I Ndlovu, Nompumelelo P Mkhwanazi","doi":"10.3390/ph18020189","DOIUrl":"10.3390/ph18020189","url":null,"abstract":"<p><p><b>Background/Objectives</b>: The development of HIV drug resistance to current antiretrovirals, and the antiretrovirals' inability to cure HIV, provides the need of developing novel drugs that inhibit HIV-1 subtypes and drug-resistance strains. Fungal endophytes, including <i>Alternaria alternata</i>, stand out for their potentially antiviral secondary metabolites. Hence, this study investigates the anti-HIV activities and mechanism of action of the <i>A. alternata</i> crude extract against different HIV-1 subtypes and integrase-resistant mutant strains. <b>Methods</b>: Cytotoxicity of the <i>A. alternata</i> crude extract on TZM-bl cells using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay was performed. The crude extract antiviral activity against subtypes A, B, C, and D and integrase drug-resistant strain T66K and S230R was determined using a luciferase-based antiviral assay. Luciferase and p24 ELISA-based time-of-addition assays were used to determine the mechanism of action of the crude extract. Docking scores and protein ligand interactions of integrase T66K and S230R strains against the identified bioactive compounds were determined. <b>Results</b>: The crude extract CC₅₀ was 300 μg/mL and not cytotoxic to the TZM-bl cell lines. In HIV-1 subtypes A, B, C, and D, the crude extract exhibited 100% inhibition and therapeutic potential. The <i>A. alternata</i> crude extract had strong anti-HIV-1 activity against integrase strand transfer drug-resistant strains T66K and S230R, with a 0.7265- and 0. 8751-fold increase in susceptibility. The crude extract had antiviral activity during attachment, reverse transcription, integration, and proteolysis. In silico calculations showed compounds 2,3-2H-Benzofuran-2-one, 3,3,4,6-tetramethyl-, 3-Methyl-1,4-diazabicyclo[4.3.0]nonan-2,5-dione, N-acetyl, Coumarin, 3,4-dihydro-4,5,7-trimethyl-, Cyclopropanecarboxamide, N-cycloheptyl, Pyrrolo[1,2-a]pyrazine-1,4-dione, and hexahydro-3-(2-methylpropyl)- crude extract bioactive compounds had strong docking scores and diverse binding mechanisms with integrase. <b>Conclusions</b>: The <i>A. alternata</i> crude extract demonstrates strong antiviral activity against different HIV-1 subtypes and integrase drug-resistance strains. The extract inhibited various stages of the HIV-1 life cycle. The bioactive compounds 2,3-2H-Benzofuran-2-one, 3,3,4,6-tetramethyl-, 3-Methyl-1,4-diazabicyclo[4.3.0]nonan-2,5-dione, N-acetyl, Coumarin, 3,4-dihydro-4,5,7-trimethyl-, Cyclopropanecarboxamide, N-cycloheptyl, Pyrrolo[1,2-a]pyrazine-1,4-dione, and hexahydro-3-(2-methylpropyl)- may be responsible for the antiviral activity of <i>A. alternata</i>.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 2","pages":""},"PeriodicalIF":4.3,"publicationDate":"2025-01-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11859181/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143503441","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Prevention and Treatment of Peritoneal Dialysis-Associated Fibrosis with Intraperitoneal Anti-Fibrotic Therapy in Experimental Peritoneal Fibrosis.","authors":"Chiao-Yin Sun, Yu-Ting Hsieh, Shang-Chieh Lu, Chi-Ying F Huang","doi":"10.3390/ph18020188","DOIUrl":"10.3390/ph18020188","url":null,"abstract":"<p><strong>Background/objectives: </strong>Long-term peritoneal dialysis (PD) often results in peritoneal damage and fibrosis, impairing peritoneal membrane function and leading to ultrafiltration failure. This study aimed to explore the therapeutic potential of nintedanib and pirfenidone in preventing and treating PD-associated peritoneal fibrosis using experimental models.</p><p><strong>Methods: </strong>An animal model of peritoneal fibrosis and cultured mesothelial cells were utilized to evaluate the effects of nintedanib and pirfenidone. Histological analysis, molecular techniques, and RNA sequencing were employed to assess the fibrosis, inflammation, and gene expression. The key outcomes included changes in the peritoneal structure, inflammatory markers, and transcriptional regulation.</p><p><strong>Results: </strong>Induced peritoneal fibrosis resulted in significant structural and histological changes. Treatment with nintedanib and pirfenidone effectively prevented peritoneal thickening and reduced excessive fibrosis deposition. Both agents ameliorated the inflammatory responses by lowering inflammatory marker expression, inhibiting cytokine activity, and decreasing macrophage infiltration. Molecular analyses revealed the suppression of inflammation-related transcription regulators and cytokine receptors. RNA sequencing identified glucose-induced gene expression changes and demonstrated significant modulation by the treatments. In animal studies with established fibrosis, these agents reduced peritoneal inflammation and slowed fibrosis progression.</p><p><strong>Conclusions: </strong>This study demonstrates that intraperitoneal administration of nintedanib and pirfenidone shows promise as an anti-fibrosis therapy for preventing and treating peritoneal fibrosis associated with PD. These findings highlight the potential of targeted interventions to improve the long-term outcomes for PD patients.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 2","pages":""},"PeriodicalIF":4.3,"publicationDate":"2025-01-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11859390/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143503582","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Fluoroquinolone-Mediated Tendinopathy and Tendon Rupture.","authors":"Ezgi Duman, Sigrid Müller-Deubert, Girish Pattappa, Ioannis Stratos, Stephan A Sieber, Hauke Clausen-Schaumann, Victoria Sarafian, Chisa Shukunami, Maximilian Rudert, Denitsa Docheva","doi":"10.3390/ph18020184","DOIUrl":"10.3390/ph18020184","url":null,"abstract":"<p><p>The fluoroquinolone (FQ) class of antibiotics includes the world's most prescribed antibiotics such as ciprofloxacin, levofloxacin, and ofloxacin that are known for their low bacterial resistance. This is despite their potential to trigger severe side effects, such as myopathy, hearing loss, tendinopathy, and tendon rupture. Thus, healthcare organizations around the world have recommended limiting the prescription of FQs. Tendinopathy is a common name for maladies that cause pain and degeneration in the tendon tissue, which can result in tendon rupture. Whilst there are several identified effects of FQ on tendons, the exact molecular mechanisms behind FQ-mediated tendon rupture are unclear. Previous research studies indicated that FQ-mediated tendinopathy and tendon rupture can be induced by changes in gene expression, metabolism, and function of tendon resident cells, thus leading to alterations in the extracellular matrix. Hence, this review begins with an update on FQs, their mode of action, and their known side effects, as well as summary information on tendon tissue structure and cellular content. Next, how FQs affect the tendon tissue and trigger tendinopathy and tendon rupture is explored in detail. Lastly, possible preventative measures and promising areas for future research are also discussed. Specifically, follow-up studies should focus on understanding the FQ-mediated tendon changes in a more complex manner and integrating in vitro with in vivo models. With respect to in vitro systems, the field should move towards three-dimensional models that reflect the cellular diversity found in the tissue.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 2","pages":""},"PeriodicalIF":4.3,"publicationDate":"2025-01-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11858458/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143503473","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Investigating Potential Anti-Bacterial Natural Products Based on Ayurvedic Formulae Using Supervised Network Analysis and Machine Learning Approaches.","authors":"Pei Gao, Ahmad Kamal Nasution, Naoaki Ono, Shigehiko Kanaya, Md Altaf-Ul-Amin","doi":"10.3390/ph18020192","DOIUrl":"10.3390/ph18020192","url":null,"abstract":"<p><p><b>Objectives</b>: This study implements a multi-dimensional methodology to systematically identify potential natural antibiotics derived from the medicinal plants utilized in Ayurvedic practices. <b>Methods</b>: Two primary analytical techniques are employed to explore the antibiotic potential of the medicinal plants. The initial approach utilizes a supervised network analysis, which involves the application of distance measurement algorithms to scrutinize the interconnectivity and relational patterns within the network derived from Ayurvedic formulae. <b>Results</b>: 39 candidate plants with potential natural antibiotic properties were identified. The second approach leverages advanced machine learning techniques, particularly focusing on feature extraction and pattern recognition. This approach yielded a list of 32 plants exhibiting characteristics indicative of natural antibiotics. A key finding of this research is the identification of 17 plants that were consistently recognized by both analytical methods. These plants are well-documented in existing literature for their antibacterial properties, either directly or through their bioactive compounds, which suggests a strong validation of the study's methodology. By synergizing network analysis with machine learning, this study provides a rigorous and multi-faceted examination of Ayurvedic medicinal plants, significantly contributing to the identification of natural antibiotic candidates. <b>Conclusions</b>: This research not only reinforces the potential of traditional medicine as a source for new therapeutics but also demonstrates the effectiveness of combining classical and contemporary analytical techniques to explore complex biological datasets.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 2","pages":""},"PeriodicalIF":4.3,"publicationDate":"2025-01-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11859686/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143503538","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"GABA_A Receptors Are Involved in the Seizure Blockage Prompted by a Polyphenol-Rich Extract of White Grape Juice in Rodents.","authors":"Alessandro Maugeri, Rita Citraro, Antonio Leo, Caterina Russo, Michele Navarra, Giovambattista De Sarro","doi":"10.3390/ph18020186","DOIUrl":"10.3390/ph18020186","url":null,"abstract":"<p><p><b>Background/Objectives:</b> Polyphenols have been suggested to possess anticonvulsant properties, which can be exploited as tools in novel strategies against epilepsy. Along that line, the aim of this study was to investigate the effects of a polyphenol-rich extract of white grape juice (WGJe) in different rodent models of epilepsy, exploring its putative mechanism of action. <b>Methods</b>: In this study, we employed pentylenetetrazole (PTZ)-injected ICR-CD1 mice, audiogenic seizure (AGS)-susceptible DBA/2 mice and WAG/Rij rats. Seizures were monitored and scored, while absence was assessed by electroencephalogram. The open-field test was employed to assess the anxiolytic effects of WGJe. In order to assess the involvement of the GABA_A receptor, we used the antagonist flumazenil in AGS-susceptible DBA/2 mice. Computational analyses were employed to evaluate the interaction of the main polyphenols of WGJe and GABA_A receptors. <b>Results</b>: Our results showed that the intraperitoneal injection of WGJe hindered tonic seizures in PTZ-injected ICR-CD1 mice. In WAG/Rij rats, WGJe did not elicit any significant effects on spike-wave discharges compared to untreated rats. In AGS-susceptible DBA/2 mice, WGJe significantly hampered both clonic and tonic seizures, as well as induced anxiolytic effects. Interestingly, when administering WGJe with flumazenil to DBA/2 mice, we noted that the observed effects were mediated by the GABA_A receptor. Moreover, docking simulations confirmed that the main polyphenols of WGJe are able to interact with the benzodiazepine sites located in both extracellular and transmembrane domains in the GABA_A receptor. <b>Conclusions:</b> This study outlines the mechanism underlying the anti-epileptic activity of WGJe, thus supporting its potential role in the management of epilepsy.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 2","pages":""},"PeriodicalIF":4.3,"publicationDate":"2025-01-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11859719/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143503475","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Diverse Roles of Antibodies in Antibody-Drug Conjugates.","authors":"Aiko Yamaguchi, H Charles Manning","doi":"10.3390/ph18020180","DOIUrl":"10.3390/ph18020180","url":null,"abstract":"<p><p>The emergence of antibody-drug conjugates (ADCs) has transformed the treatment landscape of a variety of cancers. ADCs typically consist of three main components: monoclonal antibody, chemical linker, and cytotoxic payload. These integrated therapeutic modalities harness the benefits of each component to provide a therapeutic response that cannot be achieved by conventional chemotherapy. Antibodies play roles in determining tumor specificity through target-mediated uptake, prolonging the circulation half-life of cytotoxic payloads, and providing additional mechanisms of action inherent to the original antibody, thus significantly contributing to the overall performance of ADCs. However, ADCs have unique safety concerns, such as drug-induced adverse events related to the target-mediated uptake of the ADC in normal tissues (so-called \"on-target, off-tumor toxicity\") and platform toxicity, which are partially derived from limited tumor uptake of antibodies. Identifying suitable target antigens thus impacts the clinical success of ADCs and requires careful consideration, given the multifaceted aspects of this unique treatment modality. This review briefly summarizes the representative roles that antibodies play in determining the efficacy and safety of ADCs. Key considerations for selecting suitable cell surface target antigens for ADC therapy are also highlighted.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 2","pages":""},"PeriodicalIF":4.3,"publicationDate":"2025-01-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11859538/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143503486","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"The Efficacy of Honey for the Treatment of Perineal Wounds Following Vaginal Birth: A Narrative Review.","authors":"Isa S Schaap, Céline M J G Lardenoije, Senna J J M van Riel, Niels A J Cremers","doi":"10.3390/ph18020182","DOIUrl":"10.3390/ph18020182","url":null,"abstract":"<p><p><b>Background/Objectives</b>: During vaginal delivery, the perineum can be damaged either by episiotomy or by a spontaneous perineal tear, leading to several complications. The wound healing process should proceed as quickly and properly as possible without an infection. Medical grade honey (MGH) may be a potent treatment option due to its antimicrobial and pro-healing activities. This literature study investigated the role of honey in the treatment of vaginal wounds after delivery. <b>Methods</b>: Studies published before 17 July 2024 in the PubMed, Web of Science, Embase, Scopus, EBSCO host/CINAHL, Cochrane Library, and Google Scholar databases about honey, episiotomy wounds, and perineal tears, as well as those investigating wound healing and/or pain, were assessed. <b>Results</b>: Ten studies were included (six RCTs, of which three were double-blind, one was quasi-experimental with a posttest only, and three were observational studies without a control group), with 723 participants in total. Six of the seven controlled studies showed honey significantly improved various outcome measures, such as improved wound healing, and reduced need for pain medication. The three non-controlled studies also had a positive outcome, improving wound healing and decreasing pain intensity and prickling sensation. However, the overall quality of available evidence is limited. Different types of honey concentrations, origins, and additives were used in the included studies. Using a standardized MGH formulation may help to maintain consistent and potent effects. Therefore, additional research is needed to determine the efficacy of MGH in perineal trauma and to establish guidelines for clinical use. <b>Conclusions</b>: Honey potentially has a great effect on wound healing of perineal trauma; however, more research is necessary to substantiate the findings in the current literature.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 2","pages":""},"PeriodicalIF":4.3,"publicationDate":"2025-01-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11858692/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143503528","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Andrographolide Sulfonates and Xiyanping: A Review of Chemical Composition, Pharmacological Activities, Clinical Applications, and Adverse Reactions.","authors":"Zihong Li, Lihao Yao, Zhenjie Liu, Liuping Wang, Huini Ruan, Yuanle Shen, Peng Zhang, Kaitong Li, Honglan Wang, Lili Fan, Liangxing Tu, Jianfang Feng","doi":"10.3390/ph18020183","DOIUrl":"10.3390/ph18020183","url":null,"abstract":"<p><p><i>Andrographis paniculata</i> is a plant of the Acanthaceae family and its primary bioactive constituent, andrographolide, exhibits a broad spectrum of pharmacological activities and notable clinical efficacy. However, its poor solubility and limited bioavailability pose significant challenges for therapeutic applications. To overcome these limitations, researchers have synthesized andrographolide sulfonates by reacting andrographolide with ethanol and sulfuric acid. This sulfonated derivative significantly enhances water solubility and bioavailability while retaining key pharmacological properties such as anti-inflammatory and antiviral activities. As a representative formulation, Xiyanping injection has been widely employed in the treatment of respiratory infections, pneumonia, and related conditions, playing a critical role during the COVID-19 pandemic. Despite its widespread application, there has yet to be a comprehensive review of its chemical composition and pharmacological mechanisms. Additionally, the safety of Xiyanping injection remains a topic of some debate. This review systematically examines the chemical composition, pharmacological activities, clinical applications, and adverse reactions of andrographolide sulfonates and their formulation in Xiyanping injection to provide a scientific basis for further research and applications, while also offering valuable insights for the development of similar sulfonated drugs.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 2","pages":""},"PeriodicalIF":4.3,"publicationDate":"2025-01-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11859262/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143502853","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}