{"title":"High-resolution X-ray computed tomography for identifying herbal medicines was as effective as microscopic examination","authors":"Hiroko Tokumoto, Nahoko Uchiyama, Michiho Ito","doi":"10.1007/s11418-024-01840-z","DOIUrl":"10.1007/s11418-024-01840-z","url":null,"abstract":"<div><p>Microscopic examination is one of the important identification methods for crude drug test described in the 18th Japanese Pharmacopoeia. This method is useful for identification because it can be used for small amounts of samples regardless of their storage conditions; however, this method requires a lot of technical skill in sectioning intricate and/or small samples and is time-consuming. High-resolution X-ray computed tomography (HRXCT) is a novel method for observing the internal morphology of materials. Previously, we used HRXCT to visualize the internal morphology of the Ephedra Herb, obtaining observations that closely match those obtained via microscopic examination. HRXCT employs a low-energy X-ray source and the permeation distance of the X-rays is very short. Therefore, HRXCT can be used for elucidating the morphology of small herbal medicines. In this study, Artemisia Capillaris Flower (capitulum with a diameter of approximately 2 mm) and Plantago Seed (seeds with a length of approximately 2 mm) were examined. The results showed that HRXCT examination was sufficient to illustrate the internal independent organs of Artemisia Capillaris Flower and that their inflorescences remained intact. When observing Plantago Seed, the internal morphology of more than one seed can be depicted simultaneously. Therefore, observation using HRXCT was easy, simple, and effective to illustrate the internal morphology of herbal medicines, which is typically time-consuming and requires advanced microscopy skills.</p><h3>Graphical Abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":654,"journal":{"name":"Journal of Natural Medicines","volume":"79 1","pages":"278 - 287"},"PeriodicalIF":2.5,"publicationDate":"2024-08-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142103216","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Yuta Koseki, Hiroaki Nishimura, Ryuji Asano, Katsuyuki Aoki, Li Shiyu, Ryosuke Sugiyama, Mami Yamazaki
{"title":"Isolation of new indole alkaloid triglucoside from the aqueous extract of Uncaria rhynchophylla","authors":"Yuta Koseki, Hiroaki Nishimura, Ryuji Asano, Katsuyuki Aoki, Li Shiyu, Ryosuke Sugiyama, Mami Yamazaki","doi":"10.1007/s11418-024-01836-9","DOIUrl":"10.1007/s11418-024-01836-9","url":null,"abstract":"<div><p><i>Uncaria rhynchophylla</i> (Miq.) Miq. (Rubiaceae) is widely used as a botanical raw material for traditional Japanese and Chinese medicines. However, not all of its potentially bioactive constituents have been isolated and characterized. Herein, one new indole alkaloid triglucoside (<b>1</b>), nine known alkaloids (<b>2</b>–<b>10</b>) and thirteen known non-alkaloids (<b>11</b>–<b>23</b>) were isolated from the aqueous extract of <i>Uncaria rhynchophylla</i> hook and structurally characterized <sup>1</sup>H and <sup>13</sup>C NMR and high-resolution electrospray ionization mass spectrometry. The absolute configurations of isolated compounds (<b>1</b>, <b>2</b> and <b>3</b>) were determined by the X-ray diffraction analysis of their single crystals obtained using a micro-drop crystallization technique. This technique allows single crystals to be obtained from samples as small as 50 µg, thus providing detailed structural information even on minor constituents and enabling the accurate quality monitoring of botanical raw materials more accurately.</p><h3>Graphical abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":654,"journal":{"name":"Journal of Natural Medicines","volume":"79 1","pages":"28 - 35"},"PeriodicalIF":2.5,"publicationDate":"2024-08-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1007/s11418-024-01836-9.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142034863","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Eleven new glycosidic acid methyl esters from the crude resin glycoside fraction of Ipomoea alba seeds","authors":"Nodoka Misuda, Hirotaka Nishikawa, Shin Yasuda, Hiroyuki Miyashita, Hitoshi Yoshimitsu, Ryota Tsuchihashi, Masafumi Okawa, Junei Kinjo, Masateru Ono","doi":"10.1007/s11418-024-01838-7","DOIUrl":"10.1007/s11418-024-01838-7","url":null,"abstract":"<div><p>Resin glycosides are characteristic of plants of the Convolvulaceae family and are well-known purgative ingredients in crude drugs, such as Rhizoma Jalapae, Orizaba Jalapa Tuber, and Pharbitidis Semen, which are used in traditional medicine and derived from plants belonging to this family. Isolated resin glycosides have demonstrated diverse biological activities, including antibacterial, ionophoric, anti-inflammatory, antiviral, and multidrug-resistance-modulating properties, as well as cytotoxicity against cancer cells. These compounds consist of hydroxyl fatty acid oligoglycosides (glycosidic acids), with portions of the saccharide moieties acylated with some organic acids to form the core structure. This study investigated the glycosidic acid components of a crude resin glycoside fraction obtained from a methanolic extract of <i>Ipomoea alba</i> L. seeds (Convolvulaceae). Eleven new glycosidic acid methyl esters and one known methyl ester were isolated from a glycosidic acid fraction treated with trimethylsilyldiazomethane in hexane. Their structures were determined using acidic hydrolysis and electrospray ionization-time of fight mass spectrometry and NMR spectral analyses. These compounds are penta-, tetra-, or triglycosides, with methyl 11<i>S</i>-hydroxytetradecanoate or methyl 11<i>S</i>-hydroxyhexadecanoate as the aglycone. Although <span>d</span>-quinovose and <span>l</span>-rhamnose are common monosaccharide components, the remaining monosaccharides are <span>d</span>-glucose, <span>d</span>-xylose, or <span>d</span>-fucose. The crude resin glycoside fraction showed non-negligible cytotoxicity against HL-60 human promyelocytic leukemia cells.</p><h3>Graphical abstract</h3><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":654,"journal":{"name":"Journal of Natural Medicines","volume":"78 4","pages":"1057 - 1070"},"PeriodicalIF":2.5,"publicationDate":"2024-08-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1007/s11418-024-01838-7.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141999210","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Isolation of C-29 oxygenated oleanane triterpenoids and a (+)-muurolene type sesquiterpenoid from the fruiting bodies of Fuscoporia torulosa and their bioactivities","authors":"Tatsuro Yoneyama, Chian Chen, Yoshihiro Ichimura, Katsuyuki Nakashima, Hiromichi Kenmoku, Hiroshi Imagawa, Akemi Umeyama, Masaaki Noji","doi":"10.1007/s11418-024-01832-z","DOIUrl":"10.1007/s11418-024-01832-z","url":null,"abstract":"<div><p>Basidiomycetes with a wide variety of skeletons of secondary metabolites can be expected to be the source of new interesting biological compounds. During our research on basidiomycetes, two new C-29 oxygenated oleanane-type triterpenes (<b>1</b> and <b>2</b>) and torulosacid (<b>3</b>), a muurolene type sesquiterpenoid with a five-membered ether ring along with nine known compounds (<b>4</b>–<b>12</b>), were isolated from the MeOH extract of the fruiting bodies of <i>Fuscoporia torulosa</i>. The structures of <b>1</b>–<b>3</b> were determined by NMR and HREIMS analysis. Further studies on the stereochemistry of <b>3</b> were conducted using X-ray crystallographic analysis and comparison of experimental and calculated ECD spectra. In the antimicrobial assay of isolates, <b>1</b>,<b> 7</b>, and <b>9</b> showed growth inhibitory activity against methicillin-resistant <i>Staphylococcus aureus</i> and other gram-positive strains. Isolation of oleanane type triterpenes from fungi including basidiomycetes, is a unique report that could lead to further isolation of new compounds and the discovery of unique biosynthetic enzymes.</p><h3>Graphical abstract</h3><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":654,"journal":{"name":"Journal of Natural Medicines","volume":"78 4","pages":"919 - 928"},"PeriodicalIF":2.5,"publicationDate":"2024-08-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141911310","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Formohyperins G–L, polycyclic prenylated benzoylphloroglucinols from the flowers of Hypericum formosanum","authors":"Rena Takizawa, Yusei Shimomoto, Daisuke Tsuji, Kiyoshi Imabayashi, Kohji Itoh, Reiko Akagi, Yoshiki Kashiwada, Naonobu Tanaka","doi":"10.1007/s11418-024-01839-6","DOIUrl":"10.1007/s11418-024-01839-6","url":null,"abstract":"<div><p>Phytochemical study on the flowers of <i>Hypericum formosanum</i> Maxim. (Hypericaceae) led to the isolation of formohyperins G–L (<b>1–6</b>), whose structures were assigned by detailed spectroscopic analysis. Formohyperins G–L (<b>1–6</b>) are new benzoylphloroglucinols substituted by a C<sub>10</sub> unit, a prenyl group, and a methyl group. Formohyperins G–J (<b>1–4</b>) possess a 6/6/6-tricyclic structure, while formohyperins K (<b>5</b>) and L (<b>6</b>) have a unique 6/6/5/4-tetracyclic structure consisting of cyclohexadienone, dihydropyrane, cyclopentane, and cyclobutane rings. The absolute configurations of <b>1–6</b> were deduced by analysis of the ECD spectra. Formohyperins G–J (<b>1–4</b>) and L (<b>6</b>) were found to show potent inhibitory activities against IL-1β release from LPS-treated murine microglial cells with EC<sub>50</sub> values of 5.0, 10.9, 6.3, 10.8, and 13.7 µM, respectively, without cytotoxicity. 6-<i>O</i>-Methylformohyperins G (<b>1a</b>) and I (<b>3a</b>) also exhibited the inhibitory activities with EC<sub>50</sub> values of 4.7 and 2.7 µM, respectively, although they were cytotoxic against microglial cells.</p><h3>Graphical abstract</h3><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":654,"journal":{"name":"Journal of Natural Medicines","volume":"78 4","pages":"970 - 977"},"PeriodicalIF":2.5,"publicationDate":"2024-08-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141911281","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Guantong Yu, Ruirui Wang, Xiaomei Liu, Yuhong Li, Lin Li, Xiaoming Wang, Yuhong Huang, Guixiang Pan
{"title":"Screening and identification of reactive metabolic compounds of Cortex Periplocae based on glutathione capture-mass spectrometry","authors":"Guantong Yu, Ruirui Wang, Xiaomei Liu, Yuhong Li, Lin Li, Xiaoming Wang, Yuhong Huang, Guixiang Pan","doi":"10.1007/s11418-024-01835-w","DOIUrl":"10.1007/s11418-024-01835-w","url":null,"abstract":"<div><p>As a traditional Chinese medicine (TCM), Cortex Periplocae (CP) has a wide range of pharmacological effects, as well as toxic side effects. The main toxic components of it are cardiac glycosides, which tend to cause cardiotoxicity. Currently, it has also been reported in studies to cause hepatotoxicity, but it is not clear whether the hepatotoxicity is related to the toxicity caused by the reactive metabolites. This study aims to investigate the target components of CP that generate reactive metabolic toxicity. The fluorescent probe method was used to detect glutathione (GSH)-trapped reactive metabolites in a co-incubation system of CP extract with rat liver microsomes. Identification of GSH conjugates was performed by LC–MS/MS and that of the possible precursor components that produce reactive metabolites was conducted by UPLC–Q-TOF/MS. Cell viability assays were performed on HepG2 and L02 cells to determine the cytotoxicity of the target components. The findings of our study demonstrate that the extract derived from CP has the ability to generate metabolites that exhaust the intracellular GSH levels, resulting in the formation of GSH conjugates and subsequent cytotoxic effects. Through the utilization of the UPLC–Q-TOF/MS technique, we were able to accurately determine the molecular weight of the precursor compound in CP to be 355.1023. The primary evidence to determining the GSH conjugetes relies on the appearance of characteristic product ions resulting from central neutral loss (CNL) scanning of 129 Da and product scanning of <i>m</i>/<i>z</i> 660 in the positive MS/MS spectrum. Through analysis, it was ultimately ascertained that the presence of chlorogenic acid (CGA) and its isomers, namely neochlorogenic acid (NCGA) and cryptochlorogenic acid (CCGA), could lead to the production of GSH conjugates, resulting in cytotoxicity at elevated levels. Taking these findings into consideration, the underlying cause for the potential hepatotoxicity of CP was initially determined.</p><h3>Graphical abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":654,"journal":{"name":"Journal of Natural Medicines","volume":"78 4","pages":"1044 - 1056"},"PeriodicalIF":2.5,"publicationDate":"2024-08-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1007/s11418-024-01835-w.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141892538","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
He Sun, Dandan Xiao, Xue Li, Tong Sun, Fanying Meng, Xinting Shao, Yuling Ding, Yong Li
{"title":"Study on the chemical composition and anti-fungi activities of anthraquinones and its glycosides from Rumex japonicus Houtt.","authors":"He Sun, Dandan Xiao, Xue Li, Tong Sun, Fanying Meng, Xinting Shao, Yuling Ding, Yong Li","doi":"10.1007/s11418-024-01834-x","DOIUrl":"10.1007/s11418-024-01834-x","url":null,"abstract":"<div><p>Fungi, such as <i>Trichophyton rubrum</i> (<i>T. rubrum</i>) and <i>Microsporum canis Bodin Anamorph</i> (<i>M. canis Bodin Anamorph</i>) are the main pathogens of dermatophysis. According to ancient books records, <i>Rumex japonicus</i> Houtt. (RJH) has a miraculous effect on the treatment of dermatophysis. To reveal the anti-fungi (<i>T. rubrum</i> and <i>M. canis Bodin Anamorph</i>) components and its mechanism of the <i>Rumex japonicus</i> Houtt. The vinegar extraction and alcohol precipitation, HPLC and nuclear magnetic resonance spectroscopy (NMR) were employed for analyzing the chemical compositions of RJH; in vitro anti-fungal experiment was investigated including test the minimum inhibitory concentration (MIC) and the minimum fungicidal concentration (MFC), spore germination rate, nucleic acid, protein leakage rate, biofilm structure, and the mechanism of anti-fungal and anti-fungal biofilms in RJH. Seven anthraquinones and their glycoside compounds were obtained in this study respectively, such as chrysophanol, physcion, aloe-emodin, emodin, rhein, emodin-8-O-<i>β</i>-D-glucoside and chrysophanol-8-O-<i>β</i>-D-glucoside. In <i>vitro</i> anti-fungal experiment results showed that RJH extracts have good anti-fungal activity for dermatophytic fungi. Among them, the MIC of the rhein, emodin and aloe-emodin against <i>T. rubrum</i> are 1.9 µg/ml, 3.9 µg/ml and 15.6 µg/ml, respectively; the MIC of emodin and aloe-emodin against <i>M. canis Bodin Anamorph</i> are 7.8 µg/ml and 62.5 µg/ml, respectively. In addition, its active components can inhibit fungal spore germination and the formation of bud tube, change cell membrane permeability, prevent hyphal growth, destroy biofilm structure, and down-regulate the expression of agglutinin-like sequence family 1 of the adhesion phase of biofilm growth. The study shows that RJH play a fungicidal role.</p><h3>Graphic abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":654,"journal":{"name":"Journal of Natural Medicines","volume":"78 4","pages":"929 - 951"},"PeriodicalIF":2.5,"publicationDate":"2024-08-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141892539","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Development of a determination method for quality control markers utilizing metabolic profiling and its application on processed Zingiber officinale Roscoe rhizome","authors":"Tomohisa Kanai, Tatsuya Shirahata, Shunsuke Nakamori, Yota Koizumi, Eiichi Kodaira, Noriko Sato, Hiroyuki Fuchino, Noriaki Kawano, Nobuo Kawahara, Takayuki Hoshino, Kayo Yoshimatsu, Yoshinori Kobayashi","doi":"10.1007/s11418-024-01837-8","DOIUrl":"10.1007/s11418-024-01837-8","url":null,"abstract":"<div><p>This study established an Orthogonal Partial Least Squares (OPLS) model combining <sup>1</sup>H-NMR and GC-MS data to identify characteristic metabolites in complex extracts. Both in metabolomics studies, and natural product chemistry, the reliable identification of marker metabolites usually requires laborious isolation and purification steps, which remains a bottleneck in many studies. Both ginger (GR) and processed ginger (PGR) are listed in the Japanese pharmacopeia. The plant of origin, the rhizome of <i>Zingiber officinale</i> Roscoe, is differently processed for these crude drugs. Notably, the quality of crude drugs is affected by genetic and environmental factors, making it difficult to maintain a certain quality standard. Therefore, characteristic markers for the quality control of GR and PGR are required. Metabolomic analysis using <sup>1</sup>H-NMR was able to discriminate between GR and PGR, but there were unidentified signals that were difficult to distinguish based on NMR data alone. Therefore, we combined <sup>1</sup>H-NMR and GC-MS analytical data to identify them by OPLS. As a result, α<i>r</i>-curcumene was found to be a useful marker for these identifications. This new approach enabled rapid identification of characteristic marker compounds and reduced the labor involved in the isolation process.</p><h3>Graphical abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":654,"journal":{"name":"Journal of Natural Medicines","volume":"78 4","pages":"952 - 969"},"PeriodicalIF":2.5,"publicationDate":"2024-08-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1007/s11418-024-01837-8.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141886801","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Search for natural products from actinomycetes of the genus Nocardia","authors":"Yasumasa Hara","doi":"10.1007/s11418-024-01833-y","DOIUrl":"10.1007/s11418-024-01833-y","url":null,"abstract":"<div><p>The genus <i>Nocardia</i> are gram-positive bacteria, many of which possess pathogenicity and infect human lungs, skin, brain, and other organs. Since research on the genus <i>Nocardia</i> has not progressed as rapidly as that on the genus <i>Streptomyces</i>, the genus <i>Nocardia</i> is considered a useful undeveloped resource for exploring natural products. On the other hand, when the genus <i>Nocardia</i> infects the human body, the strains are attacked by immune cells such as macrophages. Therefore, we suggested a new method for screening natural products by culturing the genus <i>Nocardia</i> in the presence of animal cells. In this review, we describe our recent results in searching for natural products from the genus <i>Nocardia</i>.</p><h3>Graphical abstract</h3>\u0000<div><figure><div><div><picture><img></picture></div></div></figure></div></div>","PeriodicalId":654,"journal":{"name":"Journal of Natural Medicines","volume":"78 4","pages":"828 - 837"},"PeriodicalIF":2.5,"publicationDate":"2024-08-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11364655/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141873886","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Dragon’s blood attenuates LPS-induced intestinal epithelial barrier dysfunction via upregulation of FAK-DOCK180-Rac1-WAVE2-Arp3 and downregulation of TLR4/NF-κB signaling pathways","authors":"Huayan Liu, Ranran Yan, Yongzhi Li, Jiaping Wang, Yulin Deng, Yujuan Li","doi":"10.1007/s11418-024-01824-z","DOIUrl":"10.1007/s11418-024-01824-z","url":null,"abstract":"<div><p>Inflammation-induced intestinal epithelial barrier (IEB) dysfunction is one of the important reasons for the occurrence and development of intestinal inflammatory-related diseases, including ulcerative colitis (UC), Crohn’s disease and necrotizing enterocolitis (NEC). Dragon’s blood (DB) is a traditional Chinese medicine and has been clinically used to treat UC. However, the protective mechanism of DB on intestinal inflammatory-related diseases has still not been elucidated. The present study aimed to explore the protection mechanism of DB on IEB dysfunction in rat ileum and human colorectal adenocarcinoma cells (Caco-2)/human umbilical vein endothelial cells (HUVECs) coculture system induced by lipopolysaccharide (LPS). DB could ameliorate rat ileum mucosa morphological injury, reduce the accumulation of lipid-peroxidation products and increase the expression of junction proteins. DB also alleviated LPS-induced Caco-2 cells barrier integrity destruction in Caco-2/ HUVECs coculture system, leading to increased trans-endothelial electrical resistance (TEER), reduced cell permeability, and upregulation of expressions of F-actin and junction proteins. DB contributed to the assembly of actin cytoskeleton by upregulating the FAK-DOCK180-Rac1-WAVE2-Arp3 pathway and contributed to the formation of intercellular junctions by downregulating TLR4-MyD88-NF-κB pathway, thus reversing LPS-induced IEB dysfunction. These novel findings illustrated the potential protective mechanism of DB on intestinal inflammatory-related diseases and might be useful for further clinical application of DB.</p><h3>Graphical abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":654,"journal":{"name":"Journal of Natural Medicines","volume":"78 4","pages":"1013 - 1028"},"PeriodicalIF":2.5,"publicationDate":"2024-07-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1007/s11418-024-01824-z.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141625556","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}