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Composition and bioactivity of propolis derived from New Zealand native forest
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2025-02-03 DOI: 10.1016/j.fitote.2025.106412
M. Manley-Harris, M.N.C. Grainger, L.M. Peters, S.T. Te Rire-McNeil
New Zealand's unique indigenous flora has evolved due to its geographical isolation in the Southern Hemisphere. In the 250 years, since European colonisation commenced, much indigenous flora has been replaced by plants largely of Northern Hemisphere origin including poplar species and pine. There are however still a few large areas of principally native flora. The honeybee (Apis mellifera) was introduced to New Zealand in 1839, so has no evolutionary link to the New Zealand indigenous flora. New Zealand propolis from areas in which honeybees have access to poplar and other Northern Hemisphere species is similar in chemical profile to Northern Hemisphere propolis. However, when honeybees were placed in an extensive area of native flora, Te Urewera in the North Island,the chemical profile of propolis produced was vastly different. This “endemic” propolis was characterised by the presence of diterpenoids in contrast to the flavonoids found in poplar-type propolis. These diterpenoids, isocupressic acid, acetyl isocupressic acid, manool, torulosal, communic acid and ferruginol, were characterised by GC–MS and by NMR spectroscopy of the isolated compounds. The “endemic” propolis has commonality with propolis of the Mediterranean-type as well as some Brazilian propolis. Investigation of the bioactivity of a sample of the “endemic” propolis revealed good antioxidant behaviour with a TEAC of 1481 mgtrolox g−1, dose-dependent inhibition of mitochondrial dehydrogenase activity, inhibition of superoxide production with an IC50 of 262 μg mL−1 and inhibition of methicillin resistant and methicillin sensitive S. aureus. Much of this bioactivity can be attributed to the presence of the diterpenoids.
{"title":"Composition and bioactivity of propolis derived from New Zealand native forest","authors":"M. Manley-Harris,&nbsp;M.N.C. Grainger,&nbsp;L.M. Peters,&nbsp;S.T. Te Rire-McNeil","doi":"10.1016/j.fitote.2025.106412","DOIUrl":"10.1016/j.fitote.2025.106412","url":null,"abstract":"<div><div>New Zealand's unique indigenous flora has evolved due to its geographical isolation in the Southern Hemisphere. In the 250 years, since European colonisation commenced, much indigenous flora has been replaced by plants largely of Northern Hemisphere origin including poplar species and pine. There are however still a few large areas of principally native flora. The honeybee (<em>Apis mellifera</em>) was introduced to New Zealand in 1839, so has no evolutionary link to the New Zealand indigenous flora. New Zealand propolis from areas in which honeybees have access to poplar and other Northern Hemisphere species is similar in chemical profile to Northern Hemisphere propolis. However, when honeybees were placed in an extensive area of native flora, Te Urewera in the North Island,the chemical profile of propolis produced was vastly different. This “endemic” propolis was characterised by the presence of diterpenoids in contrast to the flavonoids found in poplar-type propolis. These diterpenoids, isocupressic acid, acetyl isocupressic acid, manool, torulosal, communic acid and ferruginol, were characterised by GC–MS and by NMR spectroscopy of the isolated compounds. The “endemic” propolis has commonality with propolis of the Mediterranean-type as well as some Brazilian propolis. Investigation of the bioactivity of a sample of the “endemic” propolis revealed good antioxidant behaviour with a TEAC of 1481 mg<sub>trolox</sub> g<sup>−1</sup>, dose-dependent inhibition of mitochondrial dehydrogenase activity, inhibition of superoxide production with an IC<sub>50</sub> of 262 μg mL<sup>−1</sup> and inhibition of methicillin resistant and methicillin sensitive <em>S. aureus</em>. Much of this bioactivity can be attributed to the presence of the diterpenoids.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"181 ","pages":"Article 106412"},"PeriodicalIF":2.5,"publicationDate":"2025-02-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143255305","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}
引用次数: 0
Concoctive principles of detoxification and retention of the main toxicity of Tripterygium wilfordii and its anti-inflammatory efficacy by concocting with the medicinal excipient Spatholobi Caulis juice 通过与药用赋形剂 Spatholobi Caulis 果汁调制,研究威灵仙主要毒性肝毒的解毒和保留及其抗炎功效的调制原理。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2025-01-23 DOI: 10.1016/j.fitote.2025.106400
Lijie Ji , Yueyue Zhang , Yamin Li , Lingling Song , Tianzhu Zhang , Chenjie Du , Wanying Li , Xiaohui Wu , Qingwen He , Yanmei Wang , Qian Wang , Junming Wang
Tripterygium wilfordii (TW), which has severe hepatotoxicity, is commonly used as anti-rheumatism. Using the juice of auxiliary herbs in concocting poisonous herbs is a conventional method for toxicity reduction or efficacy enhancement. Traditional Chinese Pharmacy textbooks record that Spatholobi Caulis (SC) can alleviate the side effects caused by TW and also possesses excellent hepatoprotective effect. However, it is still unclear how the concoctive principles of hepatotoxicity reduction and anti-inflammatory efficacy retention of TW after being concocted with the medicinal excipient SC juice. Therefore, this study aimed to evaluate the hepatotoxicity and anti-inflammatory efficacy of concoction with SC juice on TW and preliminarily explored its detoxification mechanism. The attenuation effect of TW concocted with SC juice was determined by triptolide (TP) content, hepatic histological and serum biochemical indexes. The detoxification mechanism was predicted by network pharmacology and molecular docking, and confirmed by quantitative real-time PCR (qRT-PCR) and Western blot. Moreover, the anti-inflammatory efficacy was evaluated by paw edema test, and the major active ingredients in the SC juice introduced to TW concoction were detected. Concoction with SC juice significantly reduced TP content and serum biochemical indicator levels, alleviated liver pathological damage, introduced the main active ingredients, and inhibited the expression of hypoxia inducible factor-1α (HIF-1α) and vascular endothelial growth factor A (VEGFA). Furthermore, the anti-inflammatory efficacy was retained. In summary, this study elucidated that concoction with SC juice alleviated the hepatotoxicity of TW by inhibiting HIF-1α/VEGFA signaling, decreasing TP content, and introducing the main active components. Moreover, the anti-inflammatory efficacy was retained.
{"title":"Concoctive principles of detoxification and retention of the main toxicity of Tripterygium wilfordii and its anti-inflammatory efficacy by concocting with the medicinal excipient Spatholobi Caulis juice","authors":"Lijie Ji ,&nbsp;Yueyue Zhang ,&nbsp;Yamin Li ,&nbsp;Lingling Song ,&nbsp;Tianzhu Zhang ,&nbsp;Chenjie Du ,&nbsp;Wanying Li ,&nbsp;Xiaohui Wu ,&nbsp;Qingwen He ,&nbsp;Yanmei Wang ,&nbsp;Qian Wang ,&nbsp;Junming Wang","doi":"10.1016/j.fitote.2025.106400","DOIUrl":"10.1016/j.fitote.2025.106400","url":null,"abstract":"<div><div>Tripterygium wilfordii (TW), which has severe hepatotoxicity, is commonly used as anti-rheumatism. Using the juice of auxiliary herbs in concocting poisonous herbs is a conventional method for toxicity reduction or efficacy enhancement. Traditional Chinese Pharmacy textbooks record that Spatholobi Caulis (SC) can alleviate the side effects caused by TW and also possesses excellent hepatoprotective effect. However, it is still unclear how the concoctive principles of hepatotoxicity reduction and anti-inflammatory efficacy retention of TW after being concocted with the medicinal excipient SC juice. Therefore, this study aimed to evaluate the hepatotoxicity and anti-inflammatory efficacy of concoction with SC juice on TW and preliminarily explored its detoxification mechanism. The attenuation effect of TW concocted with SC juice was determined by triptolide (TP) content, hepatic histological and serum biochemical indexes. The detoxification mechanism was predicted by network pharmacology and molecular docking, and confirmed by quantitative real-time PCR (qRT-PCR) and Western blot. Moreover, the anti-inflammatory efficacy was evaluated by paw edema test, and the major active ingredients in the SC juice introduced to TW concoction were detected. Concoction with SC juice significantly reduced TP content and serum biochemical indicator levels, alleviated liver pathological damage, introduced the main active ingredients, and inhibited the expression of hypoxia inducible factor-1α (HIF-1α) and vascular endothelial growth factor A (VEGFA). Furthermore, the anti-inflammatory efficacy was retained. In summary, this study elucidated that concoction with SC juice alleviated the hepatotoxicity of TW by inhibiting HIF-1α/VEGFA signaling, decreasing TP content, and introducing the main active components. Moreover, the anti-inflammatory efficacy was retained.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"181 ","pages":"Article 106400"},"PeriodicalIF":2.5,"publicationDate":"2025-01-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143037709","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Bletilla ochracea Schltr. protects against ethanol-induced acute gastric ulcers by alleviating oxidative stress and inflammation and modulating gut microbiota
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2025-01-21 DOI: 10.1016/j.fitote.2025.106397
Xiaofen Li , Sili Liu , Yongmei Zhang , Chunhua Huang , Didong Lou
Gastric ulcers (GUs) are superficial diffuse lesions of the gastric mucosa that are characterised by being vulnerable to infection, difficult to cure and liable to recur. Bletilla ochracea Schltr. (BO) has the effects of astringent hemostasis, muscle growth and pain relief. We examined the effects of BO on acute GUs and their potential mechanisms from the perspectives of inflammation, oxidative stress and gut microbiota. Results indicated that BO alleviated pathological injury to the gastric mucosa and markedly alleviated oxidative stress and inflammation. In addition, BO significantly upregulated the levels of Nrf2, HO-1, NQO1 protein, and downregulated the levels of NF-κB p65, TLR4 protein. Moreover, BO significantly increased promoting the nuclear transfer of Nrf2 and markedly reduced the nuclear translocation of NF-κB p65. Furthermore, BO effectively modulated gut microbiota by increasing the diversity of species and relative abundance. Our study provided evidence that BO alleviated ethanol-induced acute GUs by activating the Nrf2/HO-1 and inhibiting the NF-κB p65/TLR4 signalling pathway, regulating dysbiosis of gut microbiota.
{"title":"Bletilla ochracea Schltr. protects against ethanol-induced acute gastric ulcers by alleviating oxidative stress and inflammation and modulating gut microbiota","authors":"Xiaofen Li ,&nbsp;Sili Liu ,&nbsp;Yongmei Zhang ,&nbsp;Chunhua Huang ,&nbsp;Didong Lou","doi":"10.1016/j.fitote.2025.106397","DOIUrl":"10.1016/j.fitote.2025.106397","url":null,"abstract":"<div><div>Gastric ulcers (GUs) are superficial diffuse lesions of the gastric mucosa that are characterised by being vulnerable to infection, difficult to cure and liable to recur. <em>Bletilla ochracea</em> Schltr. (BO) has the effects of astringent hemostasis, muscle growth and pain relief. We examined the effects of BO on acute GUs and their potential mechanisms from the perspectives of inflammation, oxidative stress and gut microbiota. Results indicated that BO alleviated pathological injury to the gastric mucosa and markedly alleviated oxidative stress and inflammation. In addition, BO significantly upregulated the levels of Nrf2, HO-1, NQO1 protein, and downregulated the levels of NF-κB p65, TLR4 protein. Moreover, BO significantly increased promoting the nuclear transfer of Nrf2 and markedly reduced the nuclear translocation of NF-κB p65. Furthermore, BO effectively modulated gut microbiota by increasing the diversity of species and relative abundance. Our study provided evidence that BO alleviated ethanol-induced acute GUs by activating the Nrf2/HO-1 and inhibiting the NF-κB p65/TLR4 signalling pathway, regulating dysbiosis of gut microbiota.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"181 ","pages":"Article 106397"},"PeriodicalIF":2.5,"publicationDate":"2025-01-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143028309","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Five new triterpenoids isolated from mastic: Structural identification and their anti-inflammatory activity
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2025-01-20 DOI: 10.1016/j.fitote.2025.106395
Wentian Xiang , Yangkai Luo , Xuerui An , Ting He , Ping Cai , Minawar Kurban , Wei Liu , Tao Yuan
Five new oleanane-type triterpenoids were isolated from mastic. Their structures including absolute configurations were determined by extensive spectroscopic methods and single-crystal X-ray crystallographic experiments. Compound 1 is distinguished by its rare furan ring. Compounds 35 are formed by the oxidative ring-opening reaction of the A ring in oleanane-type triterpenes, while compounds 3 and 4 are nor-triterpenes with a carbon atom missing at the C-28 position. The anti-inflammatory potential of the compounds was anticipated through network pharmacology, followed by a detailed molecular docking analysis. Finally, the anti-inflammatory effects were verified through the establishment of an in vitro model. Notably, compounds 3 and 4 exhibited significant inhibitory effects on NO production in RAW264.7 cells induced by lipopolysaccharide, with IC50 values of 8.68 ± 2.58 and 5.00 ± 3.06 μM, respectively. These values are lower than that of the positive control drug, dexamethasone, which has an IC50 of 9.93 ± 1.17 μM. The significant anti-inflammatory activity of these compounds suggests their potential as treatment candidates for inflammatory diseases.
{"title":"Five new triterpenoids isolated from mastic: Structural identification and their anti-inflammatory activity","authors":"Wentian Xiang ,&nbsp;Yangkai Luo ,&nbsp;Xuerui An ,&nbsp;Ting He ,&nbsp;Ping Cai ,&nbsp;Minawar Kurban ,&nbsp;Wei Liu ,&nbsp;Tao Yuan","doi":"10.1016/j.fitote.2025.106395","DOIUrl":"10.1016/j.fitote.2025.106395","url":null,"abstract":"<div><div>Five new oleanane-type triterpenoids were isolated from mastic. Their structures including absolute configurations were determined by extensive spectroscopic methods and single-crystal X-ray crystallographic experiments. Compound <strong>1</strong> is distinguished by its rare furan ring. Compounds <strong>3</strong>–<strong>5</strong> are formed by the oxidative ring-opening reaction of the A ring in oleanane-type triterpenes, while compounds <strong>3</strong> and <strong>4</strong> are nor-triterpenes with a carbon atom missing at the C-28 position. The anti-inflammatory potential of the compounds was anticipated through network pharmacology, followed by a detailed molecular docking analysis. Finally, the anti-inflammatory effects were verified through the establishment of an in vitro model. Notably, compounds <strong>3</strong> and <strong>4</strong> exhibited significant inhibitory effects on NO production in RAW264.7 cells induced by lipopolysaccharide, with IC<sub>50</sub> values of 8.68 ± 2.58 and 5.00 ± 3.06 μM, respectively. These values are lower than that of the positive control drug, dexamethasone, which has an IC<sub>50</sub> of 9.93 ± 1.17 μM. The significant anti-inflammatory activity of these compounds suggests their potential as treatment candidates for inflammatory diseases.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"181 ","pages":"Article 106395"},"PeriodicalIF":2.5,"publicationDate":"2025-01-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143022696","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Potential of Glycyrrhiza in the prevention of colitis-associated colon cancer
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2025-01-20 DOI: 10.1016/j.fitote.2025.106398
Fang Liu , Zhili Gu , Feiyang Yi , Xue Liu , Wenxuan Zou , Qingxia Xu , Yun Yuan , Nianzhi Chen , Jianyuan Tang

Ethnopharmacological relevance

Glycyrrhiza, a legume native to the Mediterranean region, has a long history of ethnomedicinal use in China. Due to its antiviral, antibacterial, anti-inflammatory, antioxidant, antitumor, anti-ulcer, and hepatoprotective properties, Glycyrrhiza is widely utilized in the treatment of gastrointestinal disorders.

The aim of the review

The specific mechanisms of the main active constituents of glycyrrhiza in the treatment of inflammatory bowel disease, precancerous lesions and colorectal cancer at all stages of the colitis-associated colon cancer “Inflammation-Dysplasia-Cancer” sequence, as well as its pharmacokinetics, toxicology, formulation improvements, and application studies, are reviewed to provide new insights and perspectives on glycyrrhiza as a dietary supplement to treat and prevent colitis-associated colon cancer.

Materials and methods

Information on Glycyrrhiza was retrieved from electronic databases, including PubMed and Web of Science.

Results

Glycyrrhiza is a well-established medicinal plant with significant potential for applications in both the food and pharmaceutical industries. Over 400 active constituents have been identified in Glycyrrhiza, including terpenoids, flavonoids, isoflavones, coumarins, and polyphenols. Numerous studies have demonstrated that Glycyrrhiza and its active compounds can inhibit the “Inflammation-Dysplasia-Cancer” progression of colitis-associated colon cancer by mitigating inflammatory bowel disease, reducing the number of intestinal precancerous lesions, and counteracting colorectal cancer. Furthermore, derivatives and nanocarriers are crucial for the effective treatment of colitis-associated colon cancer using Glycyrrhiza and its active constituents.

Conclusion

In conclusion, Glycyrrhiza is a plant with both medicinal and nutritional value, making it a potential food ingredient and dietary supplement for the treatment of colitis-associated colon cancer.
{"title":"Potential of Glycyrrhiza in the prevention of colitis-associated colon cancer","authors":"Fang Liu ,&nbsp;Zhili Gu ,&nbsp;Feiyang Yi ,&nbsp;Xue Liu ,&nbsp;Wenxuan Zou ,&nbsp;Qingxia Xu ,&nbsp;Yun Yuan ,&nbsp;Nianzhi Chen ,&nbsp;Jianyuan Tang","doi":"10.1016/j.fitote.2025.106398","DOIUrl":"10.1016/j.fitote.2025.106398","url":null,"abstract":"<div><h3>Ethnopharmacological relevance</h3><div>Glycyrrhiza, a legume native to the Mediterranean region, has a long history of ethnomedicinal use in China. Due to its antiviral, antibacterial, anti-inflammatory, antioxidant, antitumor, anti-ulcer, and hepatoprotective properties, Glycyrrhiza is widely utilized in the treatment of gastrointestinal disorders.</div></div><div><h3>The aim of the review</h3><div>The specific mechanisms of the main active constituents of glycyrrhiza in the treatment of inflammatory bowel disease, precancerous lesions and colorectal cancer at all stages of the colitis-associated colon cancer “Inflammation-Dysplasia-Cancer” sequence, as well as its pharmacokinetics, toxicology, formulation improvements, and application studies, are reviewed to provide new insights and perspectives on glycyrrhiza as a dietary supplement to treat and prevent colitis-associated colon cancer.</div></div><div><h3>Materials and methods</h3><div>Information on Glycyrrhiza was retrieved from electronic databases, including PubMed and Web of Science.</div></div><div><h3>Results</h3><div>Glycyrrhiza is a well-established medicinal plant with significant potential for applications in both the food and pharmaceutical industries. Over 400 active constituents have been identified in Glycyrrhiza, including terpenoids, flavonoids, isoflavones, coumarins, and polyphenols. Numerous studies have demonstrated that Glycyrrhiza and its active compounds can inhibit the “Inflammation-Dysplasia-Cancer” progression of colitis-associated colon cancer by mitigating inflammatory bowel disease, reducing the number of intestinal precancerous lesions, and counteracting colorectal cancer. Furthermore, derivatives and nanocarriers are crucial for the effective treatment of colitis-associated colon cancer using Glycyrrhiza and its active constituents.</div></div><div><h3>Conclusion</h3><div>In conclusion, Glycyrrhiza is a plant with both medicinal and nutritional value, making it a potential food ingredient and dietary supplement for the treatment of colitis-associated colon cancer.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"181 ","pages":"Article 106398"},"PeriodicalIF":2.5,"publicationDate":"2025-01-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143022697","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Antidiabetic effects of two naphthoquinones from the branches and leaves of Tectona grandis and possible mechanism 两种萘醌的抗糖尿病作用及其可能机制。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2025-01-17 DOI: 10.1016/j.fitote.2025.106396
Xuelin Chen , Jiyan Ni , Kun Zhang , Xia Zhao , Yumei Zhang
Tectona grandis is a Dai medicine that plays an important role in traditional medicine in India, Myanmar, West Africa, and Yunnan Province in China. T. grandis was recorded as an anti-diabetic herb in the Ayurvedic Pharmacopoeia; however, its potential antidiabetic components and possible mechanisms of action have almostly not been described to far. To completely comprehend the pharmacological components and therapeutic potential of T. grandis, we isolated chemical components from the plant's leaves and branches, evaluated their antidiabetic activities, and explored the possible mechanisms of active compounds using molecular docking and network pharmacology. In this study, two new quinones (12) and eighteen known compounds (320) were isolated and identified from T. grandis. Except for the new quinones 1 and 2, compounds 4, 1112, 1415, 1820 were separated from T. grandis for the first time. The naphthoquinones 1 and 3 showed significant antidiabetic activities in α-glucosidase inhibition assay (IC50: 92.52 ± 5.05 and 45.37 ± 1.50 μM, respectively), glucose uptake assay (Inhibition rate: 63.90 ± 1.04 % and 65.41 ± 1.96 %, respectively) and preadipocyte differentiation inhibition assay (Lipid droplet content decreased by 8.49 ± 0.71 % and 13.89 ± 0.29 %, respectively, compared to the model group). Our study also revealed that T. grandis might treat diabetes by targeting CASP3, ESR1, and PTGS2. This study provided important support for the traditional usage of T. grandis as an antidiabetic herb by identifying its antidiabetic components and possible mechanism.
大地黄是一种傣族药,在印度、缅甸、西非和中国云南省的传统医学中占有重要地位。在《阿育吠陀药典》中记载为抗糖尿病草药;然而,其潜在的抗糖尿病成分和可能的作用机制迄今几乎没有描述。为了全面了解大叶茅的药理成分和治疗潜力,我们从大叶茅的叶和枝中分离化学成分,评估其抗糖尿病活性,并利用分子对接和网络药理学方法探讨活性化合物的可能作用机制。本研究从大黄霉中分离鉴定了2个新醌类化合物(1-2)和18个已知化合物(3-20)。除新醌1和新醌2外,化合物4、11 ~ 12、14 ~ 15、18 ~ 20均为首次从该植物中分离得到。萘醌1和3显示显著的抗糖尿病的活动α葡糖苷酶抑制试验(IC50: 92.52 ±  5.05和45.37±1.50  μM,分别),葡萄糖吸收试验(抑制率:63.90 ±1.04   %和65.41±1.96  %,分别)和preadipocyte分化抑制试验(脂滴内容 下降了8.49±0.71   %和13.89±0.29  %,分别与模型组相比)。我们的研究还表明,大叶黄酮可能通过靶向CASP3、ESR1和PTGS2来治疗糖尿病。本研究确定了大叶参的抗糖尿病成分及其可能的机制,为大叶参作为抗糖尿病中药的传统应用提供了重要支持。
{"title":"Antidiabetic effects of two naphthoquinones from the branches and leaves of Tectona grandis and possible mechanism","authors":"Xuelin Chen ,&nbsp;Jiyan Ni ,&nbsp;Kun Zhang ,&nbsp;Xia Zhao ,&nbsp;Yumei Zhang","doi":"10.1016/j.fitote.2025.106396","DOIUrl":"10.1016/j.fitote.2025.106396","url":null,"abstract":"<div><div><em>Tectona grandis</em> is a Dai medicine that plays an important role in traditional medicine in India, Myanmar, West Africa, and Yunnan Province in China. <em>T. grandis</em> was recorded as an anti-diabetic herb in the Ayurvedic Pharmacopoeia; however, its potential antidiabetic components and possible mechanisms of action have almostly not been described to far. To completely comprehend the pharmacological components and therapeutic potential of <em>T. grandis</em>, we isolated chemical components from the plant's leaves and branches, evaluated their antidiabetic activities, and explored the possible mechanisms of active compounds using molecular docking and network pharmacology. In this study, two new quinones (<strong>1</strong>–<strong>2</strong>) and eighteen known compounds (<strong>3</strong>−<strong>20</strong>) were isolated and identified from <em>T. grandis</em>. Except for the new quinones <strong>1</strong> and <strong>2</strong>, compounds <strong>4</strong>, <strong>11</strong>–<strong>12</strong>, <strong>14</strong>–<strong>15</strong>, <strong>18</strong>–<strong>20</strong> were separated from <em>T. grandis</em> for the first time. The naphthoquinones <strong>1</strong> and <strong>3</strong> showed significant antidiabetic activities in <em>α</em>-glucosidase inhibition assay (IC<sub>50</sub>: 92.52 ± 5.05 and 45.37 ± 1.50 μM, respectively), glucose uptake assay (Inhibition rate: 63.90 ± 1.04 % and 65.41 ± 1.96 %, respectively) and preadipocyte differentiation inhibition assay (Lipid droplet content decreased by 8.49 ± 0.71 % and 13.89 ± 0.29 %, respectively, compared to the model group). Our study also revealed that <em>T. grandis</em> might treat diabetes by targeting CASP3, ESR1, and PTGS2. This study provided important support for the traditional usage of <em>T. grandis</em> as an antidiabetic herb by identifying its antidiabetic components and possible mechanism.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"181 ","pages":"Article 106396"},"PeriodicalIF":2.5,"publicationDate":"2025-01-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143002794","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Five new bisabolane-type sesquiterpenoids with oxygen-containing heterocyclic systems from Curcuma longa 姜黄含氧杂环体系中五个新的双abolane型倍半萜类化合物。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2025-01-17 DOI: 10.1016/j.fitote.2025.106399
Ou Dai , Guang-Xu Wu , Hong-Zhen Shu , Cheng Peng , Fei Liu , Liang Xiong
Five new bisabolane-type sesquiterpenoids (15) were isolated from the rhizomes of Curcuma longa, and all of them were oxygen-containing heterocyclic compounds. The structures of the compounds were elucidated using comprehensive spectroscopic techniques, and their absolute configurations were confirmed through electronic circular dichroism (ECD) calculations. All of the compounds were evaluated for their vasorelaxant and anti-inflammatory activities. The results showed that only compound 4 exhibited a vasorelaxant effect against KCl-induced contraction of rat aortic rings, and it achieved a diastolic ratio that exceeded 25 % at a concentration of 25 μM.
从姜黄根茎中分离到5个新的双abolane型倍半萜类化合物(1 ~ 5),均为含氧杂环化合物。利用综合光谱技术对化合物的结构进行了分析,并通过电子圆二色性(ECD)计算确定了化合物的绝对构型。所有化合物的血管松弛和抗炎活性进行了评估。结果表明,只有化合物4对kcl诱导的大鼠主动脉环收缩具有血管松弛作用,在浓度为25 μM时,其舒张比超过25 %。
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引用次数: 0
The protective effect and potential mechanism of Zanthoxylum bungeanum Maxim. on atherosclerosis 花椒的保护作用及其潜在机制。在动脉粥样硬化。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2025-01-16 DOI: 10.1016/j.fitote.2025.106394
Zongchao Li , Ruoxuan Xu , Can Li, Chenglin Chi, Xiaoli Yang, Shufang Yang, Rongxia Liu
The pericarp of Zanthoxylum bungeanum Maxim. (ZBM) is an edible spice with medicinal value, and it has anti-obesity, anti-inflammatory, and cardiovascular protective effects. This study investigated the therapeutic effect of ZBM on atherosclerosis (AS) and its potential mechanisms. An in vivo experimental model of AS was established on apolipoprotein-E deficient (ApoE−/−) mice to evaluate the efficacy of ZBM. Serum metabolomics combined with the vascular smooth muscle cell (VSMC) proliferation model were subsequently conducted to analyze the mechanisms. Results showed that ZBM effectively alleviated blood lipid disorders, aortic lipid accumulation, and intimal thickness in mice. Metabolomics indicated that ZBM mainly regulated 5 major metabolic pathways, including TCA cycle, steroid hormone biosynthesis, sphingolipid metabolism, glyoxylate and dicarboxylate metabolism, glycerophospholipid metabolism, which affected lipid metabolism and cell proliferation. Further experiments showed that ZBM inhibited VSMC proliferation likely because it blocked the signal transducer activator of transcription 3 (STAT3) phosphorylation and activated nuclear factor E2-related factor-2 (Nrf2)/heme oxygenase-1 (HO-1) pathway, resulting in G0/G1 phase arrest and reactive oxygen species (ROS) clearance.
花椒的果皮。(ZBM)是一种具有药用价值的食用香料,具有抗肥胖、抗炎和心血管保护作用。本研究探讨中药中药对动脉粥样硬化(AS)的治疗作用及其可能机制。以载脂蛋白e缺乏(ApoE-/-)小鼠为实验对象,建立AS的体内实验模型,评价ZBM的疗效。血清代谢组学结合血管平滑肌细胞(VSMC)增殖模型分析其作用机制。结果表明,中药能有效缓解小鼠血脂紊乱、主动脉脂质积累和内膜厚度。代谢组学表明,ZBM主要调控TCA循环、类固醇激素生物合成、鞘脂代谢、乙醛酸盐和二羧酸盐代谢、甘油磷脂代谢等5条主要代谢途径,影响脂质代谢和细胞增殖。进一步的实验表明,ZBM抑制VSMC增殖可能是由于其阻断了转录3信号转导激活因子(STAT3)磷酸化,激活了核因子e2相关因子-2 (Nrf2)/血红素加氧酶-1 (HO-1)通路,导致G0/G1期阻滞和活性氧(ROS)清除。
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引用次数: 0
Study on chemical composition, anti-inflammatory activity and quality control of the branch bark of Morus alba L. 桑树枝皮化学成分、抗炎活性及质量控制研究。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2025-01-16 DOI: 10.1016/j.fitote.2025.106383
Wenyuan Li , Lin Chen , Minpeng Li , Kaiye Peng , Xuemei Lin , Yifan Feng , Yun Zou , Xia Wu
In this study, the chemical constituents of branch bark and root bark of Morus alba L. were first qualitatively analyzed by UPLC-Q/TOF-MS. A total of 40 compounds were identified, including 20 flavonoids, 3 stilbenes, 1 phenolic acid, 1 alkaloid, 5 arylbenzofurans and 10 Diels-Alder adducts. Of these, 19 compounds were specific to the root bark, 10 to the branch bark, and 11 were common to both. Total phenolic and flavonoid contents were determined, and anti-inflammatory activities were evaluated. Ethyl acetate extracts of both significantly inhibited NO secretion, with the root bark showing a stronger effect than the branch bark. Chemical components of branch bark were further separated, and the anti-inflammatory activities of these isolated compounds were investigated. Eight compounds were isolated from the ethyl acetate extract of the branch bark of Morus alba L.. These compounds were able to inhibit the release of inflammatory factors, including NO, IL-6, and IL-1β, in a concentration-dependent manner. Among them, compounds SZP-1, SZP-6 and SZP-8 exhibited superior in vitro anti-inflammatory activity, comparable to the positive drug meloxicam at high concentrations. In addition, the quality standard of the branch bark of Morus alba L. was established for the first time according to the 2020 edition of the Chinese Pharmacopoeia. This study provides valuable insights into the medicinal value of the branch bark of Morus alba L. and promotes the comprehensive utilization of mulberry branch resources.
本研究首次采用UPLC-Q/TOF-MS对桑树枝皮和根皮的化学成分进行了定性分析。共鉴定出40个化合物,包括20个黄酮类化合物、3个二苯乙烯类化合物、1个酚酸类化合物、1个生物碱类化合物、5个芳基苯并呋喃类化合物和10个Diels-Alder加合物。其中19种化合物是根皮所特有的,10种是枝皮所特有的,11种是根皮和枝皮所共有的。测定总酚和类黄酮含量,并评价其抗炎活性。两种提取物的乙酸乙酯提取物均能显著抑制NO的分泌,且根皮对NO的抑制作用强于枝皮。进一步对树枝树皮的化学成分进行分离,并对分离得到的化合物进行抗炎活性研究。从桑树枝皮乙酸乙酯提取物中分离得到8个化合物。这些化合物能够以浓度依赖的方式抑制炎症因子的释放,包括NO, IL-6和IL-1β。其中,化合物SZP-1、SZP-6和SZP-8表现出较强的体外抗炎活性,在高浓度下与阳性药物美洛昔康相当。根据2020年版《中国药典》,首次建立了桑枝皮的质量标准。本研究为桑树枝皮药用价值的研究提供了有价值的见解,促进桑树枝资源的综合利用。
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引用次数: 0
Chemical profile, biological potential, molecular docking, molecular dynamics, and ADMET approaches of essential oils from extracted endemic Prangos aricakensis leaf and stem 猕桃叶茎挥发油的化学特征、生物学潜力、分子对接、分子动力学及ADMET方法。
IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Pub Date : 2025-01-16 DOI: 10.1016/j.fitote.2025.106391
Serbay Safak Gokcimen , Tevfik Ozen , Ibrahim Demirtas , Sarmad Marah , Fatih Gul , Lutfi Behcet
This paper investigated essential oils (EOs) of the endemic Prangos aricakensis (PA) used as spice and aroma by the Turkish people. Using a Clevenger-type device, EOs were obtained for the first time by hydro-distillation from dried parts of PA (L:leaf, S:stem). The EOs of the PALEO and PASEO were analyzed by GC–MS/MS. The main components of both parts were limonene, bornyl acetate, cinnamic acid ethyl ester, and methyl trans-cinnamate. In this work, enzyme inhibition, antioxidant, antimicrobial, antifungal, and DNA protection activities were applied for PASEO and PALEO. The PALEO in DPPH and PASEO in ABTS•+ scavenging activities were better than standard. In BChE inhibition activity, PALEO (6.69 ± 0.01 μg/mL) was more effective than galantamine (9.88 ± 2.42 μg/mL). It was active against pathogen bacteria and fungus, ranging between 32 and 128 μg/mL in terms of MIC, respectively. The results of molecular docking and ADMET of the four major components of EOs supported the effectiveness of the biological activity. Also, molecular dynamics (MD) simulations were performed for 100 ns, and MM-PBSA energies were calculated for the best-scored molecules in docking. In particular, radical scavenger, anti-BChE potential, and usability to develop different formulations against the disease were supported by in vitro, ADMET, and MD studies.
本文研究了土耳其特有植物Prangos aricakensis (PA)用作香料和香料的精油(EOs)。利用Clevenger-type装置,首次从PA (L:叶,S:茎)的干燥部分进行水蒸气蒸馏法获得了EOs。采用GC-MS/MS分析PALEO和PASEO的EOs。两组分的主要成分为柠檬烯、醋酸龙脑酯、肉桂酸乙酯和反式肉桂酸甲酯。在这项工作中,PASEO和PALEO具有酶抑制、抗氧化、抗菌、抗真菌和DNA保护活性。DPPH•的PALEO和ABTS•+的PASEO清除活性均优于标准。在BChE抑制活性方面,PALEO(6.69 ± 0.01 μg/mL)优于加兰他明(9.88 ± 2.42 μg/mL)。对病原菌和真菌的MIC值分别为32 ~ 128 μg/mL。四种主要成分的分子对接和ADMET结果支持了其生物活性的有效性。同时,进行了100 ns的分子动力学(MD)模拟,并计算了对接中得分最高的分子的MM-PBSA能量。特别是自由基清除剂、抗bche的潜力,以及开发不同配方对抗疾病的可用性,得到了体外、ADMET和MD研究的支持。
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Fitoterapia
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