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Keywords = Cortex Mori Radicis

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15 pages, 2576 KiB  
Article
Benzofuran Derivatives from Cortex Mori Radicis and Their Cholinesterase-Inhibitory Activity
by Xiang Cui, Zehong Huang, Shanshan Deng, Yunxia Zhang, Guoyin Li, Lining Wang, Yanru Deng and Changjing Wu
Molecules 2024, 29(2), 315; https://doi.org/10.3390/molecules29020315 - 8 Jan 2024
Cited by 2 | Viewed by 2143
Abstract
The phytochemical investigation of Cortex Mori Radicis led to the isolation and identification of a new prenylated benzofuranone (1) and four ring-opening derivatives (25) named albaphenol A–E, as well as nigranol A (6), together with [...] Read more.
The phytochemical investigation of Cortex Mori Radicis led to the isolation and identification of a new prenylated benzofuranone (1) and four ring-opening derivatives (25) named albaphenol A–E, as well as nigranol A (6), together with ten 2-arylbenzofuran derivatives (716). The characterization of the structures of the new compounds and the structural revision of nigranol A (6) were conducted using the comprehensive analysis of spectroscopic data (1D/2D NMR, HRESIMS, CD, and XRD). Compounds 116 were tested for their inhibitory effects on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Compounds 1 and 4 showed weak BChE-inhibitory activity (IC50 45.5 and 61.0 μM); six 2-arylbenzofuran derivatives showed more-potent BChE-inhibitory activity (IC50 2.5–32.8 μM) than the positive control galantamine (IC50 35.3 μM), while being inactive or weakly inhibitory toward AChE. Cathafuran C (14) exhibited the most potent and selective inhibitory activity against BChE in a competitive manner, with a Ki value of 1.7 μM. The structure–activity relationships of the benzofuran-type stilbenes were discussed. Furthermore, molecular docking and dynamic simulations were performed to clarify the interactions of the inhibitor–enzyme complex. Full article
(This article belongs to the Special Issue Advances in Natural Products and Their Biological Activities)
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14 pages, 4518 KiB  
Article
Combined Treatment of Mori folium and Mori Cortex Radicis Ameliorate Obesity in Mice via UCP-1 in Brown Adipocytes
by Do-Sung Kim, Hwa-Young Lee, Hwa-Jin Kim, Geum-Hwa Lee, Young Jae Lim, Bo Mi Ko, Ji-Hyun Kim, Tae Won Kim, Hye Kyung Kim, Tae Young Kim, Dae Il Hwang, Ha Kyoung Choi, Seon Min Ju, Myung Ja Chung and Han-Jung Chae
Nutrients 2023, 15(17), 3713; https://doi.org/10.3390/nu15173713 - 24 Aug 2023
Cited by 3 | Viewed by 2460
Abstract
Mori Folium (Morus alba leaf, MF) and Mori Cortex Radicis (Morus alba root cortex, MR) have been studied for their anti-obesity effects by enhancing the browning process and inhibiting adipogenesis. However, important aspects of their protective mechanisms have not been thoroughly [...] Read more.
Mori Folium (Morus alba leaf, MF) and Mori Cortex Radicis (Morus alba root cortex, MR) have been studied for their anti-obesity effects by enhancing the browning process and inhibiting adipogenesis. However, important aspects of their protective mechanisms have not been thoroughly investigated, which could aid in developing functional food. Thus, this study aims to determine the synergistic effects of MF and MR against obesity and its associated mechanisms. In an in vitro cell culture model of brown adipocytes, a 1:1 mixture of MF and MR showed a synergistic effect on the expression of brown adipocyte-specific genes, including Ucp-1, Ppargc1a, Cbp/p300-interacting transactivator (Cited), Prdm16, Tbx1, and Fgf21 compared with either MF- or MR-treated conditions. Moreover, they demonstrated the involvement of cAMP and Ca2+ in induction of brown adipocyte-specific genes. In an in vivo model using HFD-fed mice, MF/MR significantly inhibited weight gain, plasma cholesterol, LDL, TG content, fat mass, and adipocyte size. Furthermore, MF/MR inhibited morphological alteration and the expressions of fatty acid synthesis genes such as Srebp1 and Fasn in the white adipose tissue. Thermogenesis genes were recovered in the brown adipose tissue with MF/MR supplementation, indicating that MF/MR regulated adipocytic dysmetabolism where AMPK signaling is involved. In conclusion, these results suggested that MF/MR regulates brown and beige adipocyte processes, providing one of the preventive functional food/herbal medicines against obesity and its associated metabolic diseases. Full article
(This article belongs to the Section Nutrition and Obesity)
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18 pages, 3947 KiB  
Article
Anti-Cancer Effects of a New Herbal Medicine PSY by Inhibiting the STAT3 Signaling Pathway in Colorectal Cancer Cells and Its Phytochemical Analysis
by Sanghee Han, Hail Kim, Min Young Lee, Junhee Lee, Kwang Seok Ahn, In Jin Ha and Seok-Geun Lee
Int. J. Mol. Sci. 2022, 23(23), 14826; https://doi.org/10.3390/ijms232314826 - 27 Nov 2022
Cited by 6 | Viewed by 2731
Abstract
Colorectal cancer (CRC) is an inflammation-associated common cancer worldwide. Paejang-san and Mori Cortex Radicis have been traditionally used for treating intestinal inflammatory diseases in Korea and China. In the present study, we developed a new herbal formula as an alternative to CRC treatments, [...] Read more.
Colorectal cancer (CRC) is an inflammation-associated common cancer worldwide. Paejang-san and Mori Cortex Radicis have been traditionally used for treating intestinal inflammatory diseases in Korea and China. In the present study, we developed a new herbal formula as an alternative to CRC treatments, which is composed of two main components of Paejangsan (Patriniae Radix (Paejang in Korean) and Coix Seed (Yiyiin in Korean)), and Mori Cortex Radicis (Sangbekpi in Korean) based on the addition and subtraction theory in traditional medicine, hence the name PSY, and explored the potential therapeutic effects of the new formula PSY in human CRC cells by analyzing viability, cell cycle and apoptosis. We found that PSY ethanol extract (EtOH-Ex), but not water extract, significantly suppressed the viability of human CRC cells, and synergistically decreased the cell proliferation compared to each treatment of Patriniae Radix and Coix Seed extract (PY) or Mori Cortex Radicis extract (S), suggesting the combination of PY and S in a 10-to-3 ratio for the formula PSY. PSY EtOH-Ex in the combination ratio reduced cell viability but induced cell cycle arrest at the G2/M and sub-G1 phases as well as apoptosis in CRC cells. In addition, the experimental results of Western blotting, immunofluorescence staining and reporter assays showed that PSY also inhibited STAT3 by reducing its phosphorylation and nuclear localization, which resulted in lowering STAT3-mediated transcriptional activation. In addition, PSY regulated upstream signaling molecules of STAT3 by inactivating JAK2 and Src and increasing SHP1. Moreover, the chemical profiles of PSY from UPLC-ESI-QTOF MS/MS analysis revealed 38 phytochemicals, including seven organic acids, eight iridoids, two lignans, twelve prenylflavonoids, eight fatty acids, and one carbohydrate. Furthermore, 21 potentially bioactive compounds were highly enriched in the PSY EtOH-Ex compared to the water extract. Together, these results indicate that PSY suppresses the proliferation of CRC cells by inhibiting the STAT3 signaling pathway, suggesting PSY as a potential therapeutic agent for treating CRC and 21 EtOH-Ex-enriched phytochemicals as anti-cancer drug candidates which may act by inhibiting STAT3. Full article
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15 pages, 2082 KiB  
Article
Mori Cortex Radicis Attenuates High Fat Diet-Induced Cognitive Impairment via an IRS/Akt Signaling Pathway
by SoHyeon You, Miran Jang and Gun-Hee Kim
Nutrients 2020, 12(6), 1851; https://doi.org/10.3390/nu12061851 - 21 Jun 2020
Cited by 27 | Viewed by 4430
Abstract
Present study was conducted to investigate ameliorating effects of Mori Cortex radicis on cognitive impair and neuronal defects in HFD-induced (High Fat Diet-Induced) obese mice. To induce obesity, C57BL/6 mice were fed an HFD for 8 weeks, and then mice were fed the [...] Read more.
Present study was conducted to investigate ameliorating effects of Mori Cortex radicis on cognitive impair and neuronal defects in HFD-induced (High Fat Diet-Induced) obese mice. To induce obesity, C57BL/6 mice were fed an HFD for 8 weeks, and then mice were fed the HFD plus Mori Cortex radicis extract (MCR) (100 or 200 mg/kg/day) for 6 weeks. Prior to sacrifice, body weights were measured, and Y-maze test and oral glucose tolerance test were performed. Serum lipid metabolic biomarkers (TG, LDL, and HDL/total cholesterol ratio) and antioxidant enzymes (glutathione, superoxide dismutase, and catalase), malondialdehyde (MDA), and acetylcholinesterase (AChE) levels were measured in brain tissues. The expressions of proteins related to insulin signaling (p-IRS, PI3K, p-Akt, and GLUT4) and neuronal protection (p-Tau, Bcl-2, and Bax) were examined. MCR suppressed weight gain, improved serum lipid metabolic biomarker and glucose tolerance, inhibited AChE levels and MDA production, and restored antioxidant enzyme levels in brain tissue. In addition, MCR induced neuronal protective effects by inhibiting p-Tau expression and increasing Bcl-2/Bax ratio, which was attributed to insulin-induced increases in the expressions p-IRS, PI3K, p-Akt, and GLUT4. These indicate MCR may reduce HFD-induced insulin dysfunction and neuronal damage and suggest MCR be considered a functional material for the prevention of T2DM-associated neuronal disease. Full article
(This article belongs to the Section Phytochemicals and Human Health)
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9 pages, 1178 KiB  
Article
A Tri-O-Bridged Diels-Alder Adduct from Cortex Mori Radicis
by An-Qi Lu, Ming-Hua Chen, Jie Gao, Lu Wang, Han-Yu Yang, Lan Li, Bo Zhang, Hao-Ke He and Su-Juan Wang
Molecules 2018, 23(1), 133; https://doi.org/10.3390/molecules23010133 - 9 Jan 2018
Cited by 9 | Viewed by 4582
Abstract
Sanggenon X, an unusual tri-O-bridged Diels-Alder adduct, was isolated from Cortex Mori Radicis. Its structure was established by spectroscopic analysis, including NMR and HR-MS (High Resolution Mass Spectrometry). Sanggenon X contained three O-bridged rings, where the oxygenated bridgeheads were all [...] Read more.
Sanggenon X, an unusual tri-O-bridged Diels-Alder adduct, was isolated from Cortex Mori Radicis. Its structure was established by spectroscopic analysis, including NMR and HR-MS (High Resolution Mass Spectrometry). Sanggenon X contained three O-bridged rings, where the oxygenated bridgeheads were all quaternary carbons. Chemical methylation was carried out to deduce the linkages of the three O-bridges. The absolute configuration was determined by calculating the ECD (Electronic Circular Dichroism) using the TDDFT (Time-Dependent Density Functional Theory) method. Sanggenon X showed significant antioxidant activity against Fe2+-Cys-induced lipid peroxidation in rat liver microsomes, and was as effective as the positive control, curcumin. Full article
(This article belongs to the Section Natural Products Chemistry)
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12 pages, 1233 KiB  
Article
Bioactive Benzofuran Derivatives from Cortex Mori Radicis, and Their Neuroprotective and Analgesic Activities Mediated by mGluR1
by Ya-Nan Wang, Mao-Feng Liu, Wei-Zhen Hou, Rui-Ming Xu, Jie Gao, An-Qi Lu, Mei-Ping Xie, Lan Li, Jian-Jun Zhang, Ying Peng, Li-Li Ma, Xiao-Liang Wang, Jian-Gong Shi and Su-Juan Wang
Molecules 2017, 22(2), 236; https://doi.org/10.3390/molecules22020236 - 8 Feb 2017
Cited by 37 | Viewed by 7343
Abstract
Four new benzofuran-type stilbene glycosides and 14 known compounds including 8 benzofuran-type stilbenes and 6 flavonoids were isolated from the traditional Chinese medicine, Cortex Mori Radicis. The new compounds were identified as (9R)-moracin P 3′-O-α-l-arabinopyranoside (1 [...] Read more.
Four new benzofuran-type stilbene glycosides and 14 known compounds including 8 benzofuran-type stilbenes and 6 flavonoids were isolated from the traditional Chinese medicine, Cortex Mori Radicis. The new compounds were identified as (9R)-moracin P 3′-O-α-l-arabinopyranoside (1), (9R)-moracin P 9-O-β-d-glucopyranoside (2), (9R)-moracin P 3′-O-β-d-glucopyranoside (3), and (9R)-moracin O 10-O-β-d-glucopyranoside (4) based on the spectroscopic interpretation and chemical analysis. Three benzofuran-type stilbenes, moracin O (5), R (7), and P (8) showed significant neuroprotective activity against glutamate-induced cell death in SK-N-SH cells. In addition, moracin O (5) and P (8) also demonstrated a remarkable inhibition of the acetic acid-induced pain. The molecular docking with metabotropic glutamate receptor 1 (mGluR1) results indicated that these neuroprotective benzofuran-type stilbenes might be the active analgesic components of the genus Morus, and acted by mediating the mGluR1 pathway. Full article
(This article belongs to the Collection Bioactive Compounds)
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