{"title":"锯棕榈提取物对香草素受体TRPV1的影响。","authors":"Shizuo Yamada, Yoshihisa Kato","doi":"10.1111/luts.12413","DOIUrl":null,"url":null,"abstract":"<p><strong>Objective: </strong>Transient receptor potential vanilloid subtype 1 (TRPV1) may play a significant role in the pathophysiology of the bladder. The present study investigated the effects of the herbal product, saw palmetto extract (SPE) on TRPV1-mediated Ca<sup>2+</sup> influx and specific [<sup>3</sup> H]resiniferatoxin ([<sup>3</sup> H]RTX) binding to TRPV1 in HEK293 cells expressing TRPV1 (HEK293VR11 cells).</p><p><strong>Methods: </strong>Ca<sup>2+</sup> influx induced by and the direct binding activity of TRPV1 were measured using a method with Fura 2-AM, a cytoplasmic calcium indicator, and a radioligand binding assay using a [<sup>3</sup> H]RTX, respectively.</p><p><strong>Results: </strong>SPE did not markedly affect Ca<sup>2+</sup> influx in HEK293VR11 cells; however, it significantly inhibited capsaicin-induced increases in Ca<sup>2+</sup> influx in these cells. The specific binding of [<sup>3</sup> H]RTX in HEK293VR11 cells was saturable with K<sub>d</sub> value of 120 ± 7 pM and B<sub>max</sub> of 1.07 ± 0.10 fmol/mg protein, and was inhibited by low concentrations of non-labeled RTX with K<sub>i</sub> of 60.1 ± 7.6 nM. These results confirmed the pharmacological specificity of specific binding sites of [<sup>3</sup> H]RTX to TRPV1 in HEK293VR11 cells. SPE inhibited the specific binding of [<sup>3</sup> H]RTX in a concentration-dependent manner, with K<sub>i</sub> of 24.2 ± 1.4 μg/mL.</p><p><strong>Conclusions: </strong>The present study demonstrated for the first time, that SPE inhibited capsaicin-induced Ca<sup>2+</sup> influx with binding to TRPV1 in HEL293VR11 cells. These results will contribute to a more detailed understanding of the pharmacological effects of SPE on urinary dysfunction.</p>","PeriodicalId":18028,"journal":{"name":"LUTS: Lower Urinary Tract Symptoms","volume":null,"pages":null},"PeriodicalIF":1.5000,"publicationDate":"2022-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"4","resultStr":"{\"title\":\"Effects of saw palmetto extract on the vanilloid receptor TRPV1.\",\"authors\":\"Shizuo Yamada, Yoshihisa Kato\",\"doi\":\"10.1111/luts.12413\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><strong>Objective: </strong>Transient receptor potential vanilloid subtype 1 (TRPV1) may play a significant role in the pathophysiology of the bladder. The present study investigated the effects of the herbal product, saw palmetto extract (SPE) on TRPV1-mediated Ca<sup>2+</sup> influx and specific [<sup>3</sup> H]resiniferatoxin ([<sup>3</sup> H]RTX) binding to TRPV1 in HEK293 cells expressing TRPV1 (HEK293VR11 cells).</p><p><strong>Methods: </strong>Ca<sup>2+</sup> influx induced by and the direct binding activity of TRPV1 were measured using a method with Fura 2-AM, a cytoplasmic calcium indicator, and a radioligand binding assay using a [<sup>3</sup> H]RTX, respectively.</p><p><strong>Results: </strong>SPE did not markedly affect Ca<sup>2+</sup> influx in HEK293VR11 cells; however, it significantly inhibited capsaicin-induced increases in Ca<sup>2+</sup> influx in these cells. The specific binding of [<sup>3</sup> H]RTX in HEK293VR11 cells was saturable with K<sub>d</sub> value of 120 ± 7 pM and B<sub>max</sub> of 1.07 ± 0.10 fmol/mg protein, and was inhibited by low concentrations of non-labeled RTX with K<sub>i</sub> of 60.1 ± 7.6 nM. These results confirmed the pharmacological specificity of specific binding sites of [<sup>3</sup> H]RTX to TRPV1 in HEK293VR11 cells. SPE inhibited the specific binding of [<sup>3</sup> H]RTX in a concentration-dependent manner, with K<sub>i</sub> of 24.2 ± 1.4 μg/mL.</p><p><strong>Conclusions: </strong>The present study demonstrated for the first time, that SPE inhibited capsaicin-induced Ca<sup>2+</sup> influx with binding to TRPV1 in HEL293VR11 cells. These results will contribute to a more detailed understanding of the pharmacological effects of SPE on urinary dysfunction.</p>\",\"PeriodicalId\":18028,\"journal\":{\"name\":\"LUTS: Lower Urinary Tract Symptoms\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":1.5000,\"publicationDate\":\"2022-03-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"4\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"LUTS: Lower Urinary Tract Symptoms\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1111/luts.12413\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2021/10/21 0:00:00\",\"PubModel\":\"Epub\",\"JCR\":\"Q3\",\"JCRName\":\"UROLOGY & NEPHROLOGY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"LUTS: Lower Urinary Tract Symptoms","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1111/luts.12413","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2021/10/21 0:00:00","PubModel":"Epub","JCR":"Q3","JCRName":"UROLOGY & NEPHROLOGY","Score":null,"Total":0}
Effects of saw palmetto extract on the vanilloid receptor TRPV1.
Objective: Transient receptor potential vanilloid subtype 1 (TRPV1) may play a significant role in the pathophysiology of the bladder. The present study investigated the effects of the herbal product, saw palmetto extract (SPE) on TRPV1-mediated Ca2+ influx and specific [3 H]resiniferatoxin ([3 H]RTX) binding to TRPV1 in HEK293 cells expressing TRPV1 (HEK293VR11 cells).
Methods: Ca2+ influx induced by and the direct binding activity of TRPV1 were measured using a method with Fura 2-AM, a cytoplasmic calcium indicator, and a radioligand binding assay using a [3 H]RTX, respectively.
Results: SPE did not markedly affect Ca2+ influx in HEK293VR11 cells; however, it significantly inhibited capsaicin-induced increases in Ca2+ influx in these cells. The specific binding of [3 H]RTX in HEK293VR11 cells was saturable with Kd value of 120 ± 7 pM and Bmax of 1.07 ± 0.10 fmol/mg protein, and was inhibited by low concentrations of non-labeled RTX with Ki of 60.1 ± 7.6 nM. These results confirmed the pharmacological specificity of specific binding sites of [3 H]RTX to TRPV1 in HEK293VR11 cells. SPE inhibited the specific binding of [3 H]RTX in a concentration-dependent manner, with Ki of 24.2 ± 1.4 μg/mL.
Conclusions: The present study demonstrated for the first time, that SPE inhibited capsaicin-induced Ca2+ influx with binding to TRPV1 in HEL293VR11 cells. These results will contribute to a more detailed understanding of the pharmacological effects of SPE on urinary dysfunction.
期刊介绍：
LUTS is designed for the timely communication of peer-reviewed studies which provides new clinical and basic science information to physicians and researchers in the field of neurourology, urodynamics and urogynecology. Contributions are reviewed and selected by a group of distinguished referees from around the world, some of whom constitute the journal''s Editorial Board. The journal covers both basic and clinical research on lower urinary tract dysfunctions (LUTD), such as overactive bladder (OAB), detrusor underactivity, benign prostatic hyperplasia (BPH), bladder outlet obstruction (BOO), urinary incontinence, pelvic organ prolapse (POP), painful bladder syndrome (PBS), as well as on other relevant conditions. Case reports are published only if new findings are provided.
LUTS is an official journal of the Japanese Continence Society, the Korean Continence Society, and the Taiwanese Continence Society. Submission of papers from all countries are welcome. LUTS has been accepted into Science Citation Index Expanded (SCIE) with a 2011 Impact Factor.
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