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Keywords = Rehmannia glutinosa Libosch

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19 pages, 4707 KiB  
Article
Secondary Metabolites from Rehmannia glutinosa Protect Mitochondrial Function in LPS-Injured Endothelial Cells
by Liwen Zhong, Mengkai Lu, Huiqi Fang, Chao Li, Hua Qu and Gang Ding
Pharmaceuticals 2025, 18(8), 1125; https://doi.org/10.3390/ph18081125 - 27 Jul 2025
Viewed by 235
Abstract
Background: Rehmannia glutinosa, a traditional Chinese herb, is commonly used to treat vascular-related disorders. Sepsis-associated vascular endothelial dysfunction is closely associated with mitochondrial damage. This study investigated the protective effects of secondary metabolites from R. glutinosa against LPS-induced mitochondrial dysfunction in [...] Read more.
Background: Rehmannia glutinosa, a traditional Chinese herb, is commonly used to treat vascular-related disorders. Sepsis-associated vascular endothelial dysfunction is closely associated with mitochondrial damage. This study investigated the protective effects of secondary metabolites from R. glutinosa against LPS-induced mitochondrial dysfunction in endothelial cells, providing potential therapeutic insights into sepsis-related vascular complications. Methods: Phytochemical profiling of fresh R. glutinosa roots was conducted, and the structures of new secondary metabolites (1 and 2) were elucidated through comprehensive spectroscopic analysis and ECD calculations. UPLC-Q-TOF-MS/MS characterized phenylethanoid glycosides. Mitochondrial function was assessed by measuring the membrane potential, ROS levels, and TOM20/DRP1 expression in LPS-injured HUVECs. Results: Two novel eremophilane-type sesquiterpenes, remophilanetriols J (1) and K (2), along with five known phenylethanoid glycosides (37), were isolated from the fresh roots of R. glutinosa. UPLC-Q-TOF-MS/MS analysis revealed unique fragmentation pathways for phenylethanoid glycosides (37). In LPS-injured HUVECs, all compounds collectively restored the mitochondrial membrane potential, attenuated ROS accumulation, and modulated TOM20/DRP1 expression. In particular, remophilanetriol K (2) exhibited potent protective effects at a low concentration (1.5625 μM). Conclusions: This study identifies R. glutinosa metabolites as potential therapeutics for sepsis-associated vascular dysfunction by preserving mitochondrial homeostasis. This study provides a mechanistic basis for the traditional use of R. glutinosa and offers valuable insights into the development of novel therapeutics targeting mitochondrial dysfunction in sepsis. Full article
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14 pages, 2614 KiB  
Article
Identification of Bioactive Compounds from the Roots of Rehmannia glutinosa and Their In Silico and In Vitro AMPK Activation Potential
by Hwaryeong Lee, Isoo Youn, Sang Gyun Noh, Hyun Woo Kim, Eunhye Song, Sang-Jip Nam, Hae Young Chung and Eun Kyoung Seo
Molecules 2024, 29(24), 6009; https://doi.org/10.3390/molecules29246009 - 20 Dec 2024
Viewed by 1471
Abstract
Rehmannia glutinosa Libosch., which belongs to the Orobanchaceae family, is a perennial herb found in China, Japan, and Korea. In traditional medicine, it is used to cool the body, improve water metabolism in the kidney, and provide protection from metabolic diseases such as [...] Read more.
Rehmannia glutinosa Libosch., which belongs to the Orobanchaceae family, is a perennial herb found in China, Japan, and Korea. In traditional medicine, it is used to cool the body, improve water metabolism in the kidney, and provide protection from metabolic diseases such as type 2 diabetes mellitus (T2DM) and obesity. In this study, three new compounds were isolated from the roots of R. glutinosa, along with eighteen known compounds. Structure elucidation was performed with spectroscopic analyses including nuclear magnetic resonance (NMR) and circular dichroism (CD) spectroscopy. As the AMP-activated protein kinase (AMPK) signaling pathway is reportedly related to metabolic diseases, AMPK activation studies were conducted using in silico simulations and in vitro assays. Among the isolated compounds, 1 showed a potential as an AMPK activator in both in silico simulations and in vitro experiments. Our findings expand the chemical profiles of the plant R. glutinosa and suggest that one newly found compound (1) activates AMPK. Full article
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16 pages, 2403 KiB  
Article
Green Synthesized Silver Nanoparticles Induced Accumulation of Biomass and Secondary Metabolites in Hairy Roots of Rehmannia glutinosa
by Yunhao Zhu, Xiangxiang Hu, Le Dong, Han Yang, Danning Zhou, Xiangnan Liu, Chengming Dong, Xiule Yue and Le Zhao
Int. J. Mol. Sci. 2024, 25(23), 13088; https://doi.org/10.3390/ijms252313088 - 5 Dec 2024
Viewed by 1131
Abstract
The hairy roots of Rehmannia glutinosa (Gaertn.) Libosch. ex Fisch. & C. A. Mey. are capable of producing active compounds such as iridoid glycoside, and phenylethanoid glycosides, which have potential applications in the pharmaceutical industry. Silver nanoparticles (AgNPs) have been used as novel [...] Read more.
The hairy roots of Rehmannia glutinosa (Gaertn.) Libosch. ex Fisch. & C. A. Mey. are capable of producing active compounds such as iridoid glycoside, and phenylethanoid glycosides, which have potential applications in the pharmaceutical industry. Silver nanoparticles (AgNPs) have been used as novel elicitors in the induced cultivation of hairy roots, but there is a lack of research regarding their effects on R. glutinosa hairy roots. In the present study, silver nanoparticles (Pp-AgNPs) synthesized by the endophytic fungus Penicillium polandii PG21 were adopted to elicit hairy roots of R. glutinosa, to investigate their influences on the biomass, color, secondary metabolites, antioxidant activity, sucrose metabolism, and phytohormone-related gene expression. The results revealed that the dry weight and fresh weight of R. glutinosa hairy roots were both higher in the treated group than in the control group after addition of 2 mg/L Pp-AgNPs for 20 d. The content of verbascoside, total phenylethanol glycosides and total cycloartenoid in the treatment group reached the highest level at 20 d, which were 1.75, 1.51, 1.44 times more than those in the control group, respectively. Pp-AgNPs significantly stimulated the enzyme activities of catalase (CAT), superoxide dismutase (SOD), and peroxidase (POD). The growth-promoting effect of Pp-AgNPs may be accomplished by increasing sucrose metabolism, and regulating the synthesis and signal transduction of gibberellin (GA) and indoleacetic acid (IAA). Moreover, expressed sequence tags-simple sequence repeat (EST-SSR)-based genetic diversity analyses indicated that there was little possibility of genetic variation among samples under different treatment conditions. In conclusion, the appropriate concentration of Pp-AgNPs can be used as an effective elicitor to improve the biomass and secondary metabolites content in R. glutinosa hairy roots. Full article
(This article belongs to the Special Issue Physiology and Molecular Biology of Plant Stress Tolerance)
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14 pages, 2968 KiB  
Article
Si-Wu Water Extracts Protect against Colonic Mucus Barrier Damage by Regulating Muc2 Mucin Expression in Mice Fed a High-Fat Diet
by Zheng Ruan, Yujuan Yu, Peiheng Han, Li Zhang and Zhongyi Hu
Foods 2022, 11(16), 2499; https://doi.org/10.3390/foods11162499 - 18 Aug 2022
Cited by 4 | Viewed by 3775
Abstract
A high-fat diet (HFD) could cause gut barrier damage. The herbs in si-wu (SW) include dang gui (Angelica sinensis (Oliv.) Diels), shu di huang (the processed root of Rehmannia glutinosa Libosch.), chuan xiong (rhizome of Ligusticum chuanxiong Hort.), and bai shao [...] Read more.
A high-fat diet (HFD) could cause gut barrier damage. The herbs in si-wu (SW) include dang gui (Angelica sinensis (Oliv.) Diels), shu di huang (the processed root of Rehmannia glutinosa Libosch.), chuan xiong (rhizome of Ligusticum chuanxiong Hort.), and bai shao (the root of Paeonia lactiflora f. pilosella (Nakai) Kitag.). Si-wu water extracts (SWE) have been used to treat blood deficiency. Components of one herb from SW have been reported to have anti-inflammatory and anti-obesity activities. However, there have been no reports about the effects of SWE on gut barrier damage. Therefore, the aim of the study was to explore the effect of SWE on gut barrier damage. In this study, we found that SWE effectively controlled body weight, liver weight, and feed efficiency, as well as decreased the serum TC level in HFD-fed mice. Moreover, SWE and rosiglitazone (Ros, positive control) increased the colonic alkaline phosphatase (ALP) level, down-regulated serum pro-inflammatory cytokine levels, and reduced intestinal permeability. In addition, SWE increased goblet cell numbers and mucus layer thickness to strengthen the mucus barrier. After supplementation with SWE and rosiglitazone, the protein expression of CHOP and GRP78 displayed a decrease, which improved the endoplasmic reticulum (ER) stress condition. Meanwhile, the increase in Cosmc and C1GALT1 improved the O-glycosylation process for correct protein folding. These results collectively demonstrated that SWE improved the mucus barrier, focusing on Muc2 mucin expression, in a prolonged high-fat diet, and provides evidence for the potential of SWE in the treatment of intestinal disease-associated mucus barrier damage. Full article
(This article belongs to the Section Plant Foods)
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21 pages, 5751 KiB  
Article
The Effects of NAA on the Tuberous Root Yield and Quality of Rehmannia glutinosa and Its Regulatory Mechanism by Transcriptome and Metabolome Profiling
by Jianjun Li, Jialin Zhu, Huimin Li, Jingxiao Ma, Peilei Chen and Yanqing Zhou
Curr. Issues Mol. Biol. 2022, 44(8), 3291-3311; https://doi.org/10.3390/cimb44080227 - 22 Jul 2022
Cited by 6 | Viewed by 2735
Abstract
Naphthylacetic acid (NAA) was used to increase the tuberous root yield of Rehmannia glutinosa, but the differences between its NAA-treated and control tuberous roots (NT and CG) and the regulatory mechanism of NAA effect remain unclear. In order to investigate them, [...] Read more.
Naphthylacetic acid (NAA) was used to increase the tuberous root yield of Rehmannia glutinosa, but the differences between its NAA-treated and control tuberous roots (NT and CG) and the regulatory mechanism of NAA effect remain unclear. In order to investigate them, NTs and CGs were used as materials, and both yield-related indices were measured; the metabolomics and transcriptomics were used to capture differentially accumulated metabolites (DAM) and to validate them via mining differentially expressed genes (DEGs), respectively. The effects of NAA treatment: increased NT mass per plant by 21.14%, through increasing the number of roots and increasing the mean root diameter; increased catalpol content by 1.2234% (p < 0.05); up-regulated 11DAMs and 596DEGs; and down-regulated 18 DAMs and 517DEGs. In particular, we discovered that NAA regulated its DAMs and biomass via 10 common metabolic pathways, and that the number of NAA-down-regulated DAMs was more than that of NAA-up-regulated DAMs in its tuberous root. Furthermore, HPLC validated the changes of several DAMs and 15 DEGs (4CL, ARF, CCoAOMT, ARGOS, etc.) associated with the yield increase and DAMs were verified by RT-qPCR. This study provided some valuable resources, such as tuberous root indices, key genes, and DAMs of Rehmannia glutinosa in response to NAA for distinguishing the CGs from NTs, and novel insights into the regulatory mechanism of NAA effects on both at the transcriptomic and metabolomic levels, so it will lay a theoretical foundation for NAA-regulated plant yield and quality, and provide references for prohibiting the uses of NAA as a swelling agent in medicinal tuber plants in China. Full article
(This article belongs to the Special Issue Advanced Research in Plant Metabolomics)
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13 pages, 4195 KiB  
Article
The Salutary Effects of Catalpol on Diesel Exhaust Particles-Induced Thrombogenic Changes and Cardiac Oxidative Stress, Inflammation and Apoptosis
by Abderrahim Nemmar, Sumaya Beegam, Nur Elena Zaaba, Salem Alblooshi, Saleh Alseiari and Badreldin H. Ali
Biomedicines 2022, 10(1), 99; https://doi.org/10.3390/biomedicines10010099 - 4 Jan 2022
Cited by 14 | Viewed by 2507
Abstract
Inhaled particulate air pollution exerts pulmonary inflammation and cardiovascular toxicity through secondary systemic effects due to oxidative stress and inflammation. Catalpol, an iridiod glucoside, extracted from the roots of Rehmannia glutinosa Libosch, has been reported to possess anti-inflammatory and antioxidant properties. Yet, the [...] Read more.
Inhaled particulate air pollution exerts pulmonary inflammation and cardiovascular toxicity through secondary systemic effects due to oxidative stress and inflammation. Catalpol, an iridiod glucoside, extracted from the roots of Rehmannia glutinosa Libosch, has been reported to possess anti-inflammatory and antioxidant properties. Yet, the potential ameliorative effects of catalpol on particulate air pollution—induced cardiovascular toxicity, has not been studied so far. Hence, we evaluated the possible mitigating mechanism of catalpol (5 mg/kg) which was administered to mice by intraperitoneal injection one hour before the intratracheal (i.t.) administration of a relevant type of pollutant particle, viz. diesel exhaust particles (DEPs, 30 µg/mouse). Twenty-four hours after the lung deposition of DEPs, several cardiovascular endpoints were evaluated. DEPs caused a significant shortening of the thrombotic occlusion time in pial microvessels in vivo, induced platelet aggregation in vitro, and reduced the prothrombin time and the activated partial thromboplastin time. All these actions were effectively mitigated by catalpol pretreatment. Likewise, catalpol inhibited the increase of the plasma concentration of C-reactive proteins, fibrinogen, plasminogen activator inhibitor-1 and P- and E-selectins, induced by DEPs. Moreover, in heart tissue, catalpol inhibited the increase of markers of oxidative (lipid peroxidation and superoxide dismutase) and nitrosative (nitric oxide) stress, and inflammation (tumor necrosis factor α, interleukin (IL)-6 and IL-1β) triggered by lung exposure to DEPs. Exposure to DEPs also caused heart DNA damage and increased the levels of cytochrome C and cleaved caspase, and these effects were significantly diminished by the catalpol pretreatment. Moreover, catalpol significantly reduced the DEPs-induced increase of the nuclear factor κB (NFκB) in the heart. In conclusion, catalpol significantly ameliorated DEPs–induced procoagulant events and heart oxidative and nitrosative stress, inflammation, DNA damage and apoptosis, at least partly, through the inhibition of NFκB activation. Full article
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35 pages, 1453 KiB  
Review
Multiple Biological Effects of an Iridoid Glucoside, Catalpol, and Its Underlying Molecular Mechanisms
by Subrat Kumar Bhattamisra, Kah Heng Yap, Vikram Rao and Hira Choudhury
Biomolecules 2020, 10(1), 32; https://doi.org/10.3390/biom10010032 - 24 Dec 2019
Cited by 86 | Viewed by 7964
Abstract
Catalpol, an iridoid glucoside, is widely distributed in many plant families and is primarily obtained from the root of Rehmannia glutinosa Libosch. Rehmannia glutinosa is a plant very commonly used in Chinese and Korean traditional medicine for various disorders, including diabetes mellitus, neuronal [...] Read more.
Catalpol, an iridoid glucoside, is widely distributed in many plant families and is primarily obtained from the root of Rehmannia glutinosa Libosch. Rehmannia glutinosa is a plant very commonly used in Chinese and Korean traditional medicine for various disorders, including diabetes mellitus, neuronal disorders, and inflammation. Catalpol has been studied extensively for its biological properties both in vitro and in vivo. This review aims to appraise the biological effects of catalpol and their underlying mechanisms. An extensive literature search was conducted using the keyword “Catalpol” in the public domains of Google scholar, PubMed, and Scifinder. Catalpol exhibits anti-diabetic, cardiovascular protective, neuroprotective, anticancer, hepatoprotective, anti-inflammatory, and anti-oxidant effects in experimental studies. Anti-inflammatory and antioxidant properties are mostly related for its biological effect. However, some specific mechanisms are also elucidated. Elevated serotonin and BDNF level by catalpol significantly protect against depression and neurodegeneration. Catalpol demonstrated an increased mitochondrial biogenesis and activation of PI3K/Akt pathway for insulin sensitizing effect. Further, its cardiovascular protective effect was linked to PI3K/Akt, apelin/APJ and Jak-Stat pathway. Catalpol produced a significant reduction in cell proliferation and an increase in apoptosis in different cancer conditions. Overall, catalpol demonstrated multiple biological effects due to its numerous mechanisms including anti-inflammatory and antioxidant effects. Full article
(This article belongs to the Section Natural and Bio-derived Molecules)
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18 pages, 5514 KiB  
Article
Rehmannia glutinosa Libosch Extracts Prevent Bone Loss and Architectural Deterioration and Enhance Osteoblastic Bone Formation by Regulating the IGF-1/PI3K/mTOR Pathway in Streptozotocin-Induced Diabetic Rats
by Wan Gong, Naidan Zhang, Gang Cheng, Quanlong Zhang, Yuqiong He, Yi Shen, Qi Zhang, Bo Zhu, Qiaoyan Zhang and Luping Qin
Int. J. Mol. Sci. 2019, 20(16), 3964; https://doi.org/10.3390/ijms20163964 - 15 Aug 2019
Cited by 119 | Viewed by 7594
Abstract
Rehmanniae Radix Praeparata (RR, named as Shudihuang in traditional Chinese medicine), the steamed roots of Rehmannia glutinosa Libosch (Scrophulariaceae), has been demonstrated to have anti-diabetic and anti-osteoporotic activities. This study aimed to explore the protective effect and underlying mechanism of RR on diabetes-induced [...] Read more.
Rehmanniae Radix Praeparata (RR, named as Shudihuang in traditional Chinese medicine), the steamed roots of Rehmannia glutinosa Libosch (Scrophulariaceae), has been demonstrated to have anti-diabetic and anti-osteoporotic activities. This study aimed to explore the protective effect and underlying mechanism of RR on diabetes-induced bone loss. It was found that RR regulated the alkaline phosphatase activity and osteocalcin level, enhanced bone mineral density, and improved the bone microarchitecture in diabetic rats. The catalpol (CAT), acteoside (ACT), and echinacoside (ECH) from RR increased the proliferation and differentiation of osteoblastic MC3T3-E1 cells injured by high glucose and promoted the production of IGF-1 and expression of related proteins in BMP and IGF-1/PI3K/mammalian target of rapamycin complex 1 (mTOR) signaling pathways. The verifying tests of inhibitors of BMP pathway (noggin) and IGF-1/PI3K/mTOR pathway (picropodophyllin) and molecular docking of IGF-1R further indicated that CAT, ACT, and ECH extracted from RR enhanced bone formation by regulating IGF-1/PI3K/mTOR signaling pathways. These findings suggest that RR may prove to be a promising candidate drug for the prevention and treatment of diabetes-induced osteoporosis. Full article
(This article belongs to the Section Molecular Pharmacology)
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16 pages, 2214 KiB  
Article
Metabolomics Profiling Reveals Rehmanniae Radix Preparata Extract Protects against Glucocorticoid-Induced Osteoporosis Mainly via Intervening Steroid Hormone Biosynthesis
by Tianshuang Xia, Xin Dong, Yiping Jiang, Liuyue Lin, Zhimin Dong, Yi Shen, Hailiang Xin, Qiaoyan Zhang and Luping Qin
Molecules 2019, 24(2), 253; https://doi.org/10.3390/molecules24020253 - 11 Jan 2019
Cited by 37 | Viewed by 6055
Abstract
Rehmanniae Radix Preparata (RR), the dry rhizome of Rehmannia glutinosa Libosch., is a traditional herbal medicine for improving the liver and kidney function. Ample clinical and pharmacological experiments show that RR can prevent post-menopausal osteoporosis and senile osteoporosis. In the present study, in [...] Read more.
Rehmanniae Radix Preparata (RR), the dry rhizome of Rehmannia glutinosa Libosch., is a traditional herbal medicine for improving the liver and kidney function. Ample clinical and pharmacological experiments show that RR can prevent post-menopausal osteoporosis and senile osteoporosis. In the present study, in vivo and in vitro experiments, as well as a UHPLC-Q/TOF-MS-based metabolomics study, were used to explore the preventing effect of RR on glucocorticoid-induced osteoporosis (GIOP) and its underlying mechanisms. As a result, RR significantly enhanced bone mineral density (BMD), improved the micro-architecture of trabecular bone, and intervened in biochemical markers of bone metabolism in dexamethasone (DEX)-treated rats. For the in vitro experiment, RR increased the cell proliferation and alkaline phosphatase (ALP) activity, enhanced the extracellular matrix mineralization level, and improved the expression of runt-related transcription factor 2 (RUNX2) and osteopontin (OPN) in DEX-injured osteoblasts. For the metabolomics study, a total of 27 differential metabolites were detected in the DEX group vs. the control group, of which 10 were significantly reversed after RR treatment. These metabolites were majorly involved in steroid hormone biosynthesis, sex steroids regulation, and amino acid metabolism. By metabolic pathway and Western blotting analysis, it was further ascertained that RR protected against DEX-induced bone loss, mainly via interfering steroid hormone biosynthesis, as evidenced by the up-regulation of cytochrome P450 17A1 (CYP17A1) and aromatase (CYP19A1), and the down-regulation of 11β-hydroxysteroid dehydrogenase (HSD11B1). Collectively, these results indicated that RR had a notable preventing effect on GIOP, and the action mechanism might be related to steroid hormone biosynthesis. Full article
(This article belongs to the Special Issue Plant Extracts: Biological and Pharmacological Activity)
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11 pages, 6998 KiB  
Article
Construction and Quality Analysis of Transgenic Rehmannia glutinosa Containing TMV and CMV Coat Protein
by Zhongqiu Teng, Ye Shen, Jing Li, Zhongping Lin, Min Chen, Min Wang, Man Li, Hongran Dong and Luqi Huang
Molecules 2016, 21(9), 1134; https://doi.org/10.3390/molecules21091134 - 27 Aug 2016
Cited by 7 | Viewed by 5947
Abstract
Plant viruses, especially tobacco mosaic virus (TMV) and cucumber mosaic virus (CMV) are serious threats to Rehmannia glutinosa which is a “top grade” herb in China. In the present study, TMV- and CMV-resistant Rehmannia glutinosa Libosch. plants were constructed by transforming the protein [...] Read more.
Plant viruses, especially tobacco mosaic virus (TMV) and cucumber mosaic virus (CMV) are serious threats to Rehmannia glutinosa which is a “top grade” herb in China. In the present study, TMV- and CMV-resistant Rehmannia glutinosa Libosch. plants were constructed by transforming the protein (CP) genes of TMV and CMV into Rehmannia glutinosa via a modified procedure of Agrobacterium tumefaciens-mediated transformation. Integration and expression of TMV CP and CMV CP transgenes in 2 lines, LBA-1 and LBA-2, were confirmed by PCR, Southern blot and RT-PCR. Both LBA-1 and LBA-2 were resistant to infection of homologous TMV and CMV strains. The quality of transgenic Rehmanniae Radix was evaluated based on fingerprint analysis and components quantitative analysis comparing with control root tubes. These results showed that chemical composition of transgenic Rehmanniae Radix were similar to non-transgenic ones, which demonstrated that the medical quality and biosafety of transgenic Rehmanniae Radix were equivalent to non-transgenic material when consumed as traditional Chinese medicinal (TCM). Full article
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