Background
Baicalein is the major bioactive flavonoid in some herb medicines and dietary plants; however, the detailed metabolism pathway of its major metabolite oroxylin A-7-O-β-d-glucuronide in human was not clear. It was important to illustrate the major metabolic enzymes that participate in its elimination for the clinic use of baicalein.
Two baicalein derivatives, baicalin and oroxylin A, were synthesized in this study. These derivatives exhibit diverse biological activities, such as anxiolytic and anticancer activities as well as memory enhancement. In order to synthesize baicalin from aglycon baicalein using Escherichia coli, we utilized a glycosyltransferase that regioselectively transfers glucuronic acid from UDP-glucuronic acid to the 7-hydroxy group of baicalein. To increase baicalin productivity, an araA deletion E. coli ...
#1Xiao Zhu(CUHK: The Chinese University of Hong Kong)H-Index: 8
#2Jianyuan Deng(CUHK: The Chinese University of Hong Kong)H-Index: 2
Last. Tai Ning Lam(CUHK: The Chinese University of Hong Kong)H-Index: 2
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Baicalein, a typical flavonoid presented in Scutellariae radix, exhibits a unique metabolic profile during first-pass metabolism: parallel glucuronidation and sulfation pathways, with possible substrate inhibition in both pathways. In this project, we aimed to construct an agent-based model to dynamically represent baicalein pharmacokinetics and to verify the substrate inhibition hypothesis. The model consisted of three 3D spaces and two membranes: apical space (S1), intracellular space (S2), ba...
ic inflammatory diseases, including OLP, involves in the activation of the nuclear factor-kappa B (NF-κB) signaling pathway. Baicalein (BAI) is an alcohol soluble flavonoid known for its anti-inflammatory effect. However, its effectiveness on keratinocytes in OLP remains unclear. In the present study, we examined inflammation in oral mucosa tissue from OLP patients. Hematoxylin and eosin staining showed denser subepithelial lymphocytes infiltration compared to the normal oral mucosa epithelium. ...
#1Fang Wang(Peking Union Medical College)H-Index: 4
#2Hou-Zao Chen(Peking Union Medical College)H-Index: 31
Last. De-Pei Liu(Peking Union Medical College)H-Index: 52
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An abdominal aortic aneurysm (AAA) is a permanent, localized dilatation of the abdominal aorta. In western countries, the morbidity of AAA is approximately 8%. Currently, pharmacotherapies for AAA are limited. Here, we demonstrate that baicalein (BAI), the main component of the Chinese traditional drug “Huang Qin”, attenuates the incidence and severity of AAA in Apoe -/- mice infused with angiotensin II (AngII). Mechanically, BAI treatment decreases AngII-induced reactive oxygen species (ROS) pr...
#1Yonglei Cui(Dalian Medical University)H-Index: 7
#2Xiangge Tian(Dalian Medical University)H-Index: 18
Last. Xiaochi Ma(Dalian Medical University)H-Index: 26
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3-Acetyl-11-keto-β-boswellic acid (AKBA) and 11-keto-β-boswellic acid (KBA) are widely used in the clinic as anti-inflammatory drugs. However, these drugs have the poor bioavailability, which may be caused by their extensive metabolism. In this study, we systemically characterized both phase I and II metabolism of AKBA and KBA in vitro. In total, four major metabolites were firstly biosynthesized and identified using 1D and 2D NMR spectroscopy. Among them, three metabolites were novel. The kinet...
#2Deepak Sharma(BARC: Bhabha Atomic Research Centre)H-Index: 27
Last. Santosh K. Sandur(BARC: Bhabha Atomic Research Centre)H-Index: 31
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Abstract NF-κB is a crucial mediator of inflammatory and immune responses and a number of phytochemicals that can suppress this immune-regulatory transcription factor are known to have promising anti-inflammatory potential. However, we report that inducer of pro-inflammatory transcription factor NF-κB functions as an anti-inflammatory agent. Our findings reveal that a plant derived flavonoid baicalein could suppress mitogen induced T cell activation, proliferation and cytokine secretion. Treatme...
Abstract Structural identification of natural products by tandem mass spectrometry requires laborious spectral analysis. Herein, we report a targeted post-acquisition data processing strategy, key ion filtering (KIF), to analyze untargeted mass spectral data. This strategy includes four steps: (1) untargeted data acquisition by ultra-high performance liquid chromatography coupled with hybrid quadrupole orbitrap mass spectrometry (UHPLC/orbitrap-MS); (2) construction of a key ion database accordi...
Background The prognosis of acute megakaryoblastic leukemia (AMKL) is really dismal, which urges for development of novel treatment. Baicalein is one type of flavonoids extracted from Scutellaria baicalensis Georgi (Huang Qin). It inhibited cell proliferation and subcutaneous tumor formation of many tumor cell lines. However, whether baicalein possesses anti-AMKL activities has not been tested.
#1Si-Cheng Liang(CAS: Chinese Academy of Sciences)H-Index: 13
#2Yang-Liu Xia(DICP: Dalian Institute of Chemical Physics)H-Index: 8
Last. Ling Yang(DICP: Dalian Institute of Chemical Physics)H-Index: 8
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Our previous study demonstrated that daphnetin is subject to glucuronidation in vitro. However, daphnetin metabolism is still poorly documented. This study aimed to investigate daphnetin metabolism and its consequent effect on the bioactivity. Metabolic profiles obtained by human liver S9 fractions and human hepatocytes showed that daphnetin was metabolized by glucuronidation, sulfonation, and methylation to form 6 conjugates which were synthesized and identified as 7-O-glucuronide, 8-O-glucuron...
Last. Chun-Su Yuan(U of C: University of Chicago)H-Index: 81
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Baicalin is a major constituent of Scutellaria baicalensis, which is a commonly used herbal medicine in many Asian countries. After oral ingestion, intestinal micro-biota metabolism may change parent compound's structure and its biological activities. However, whether baicalin can be metabolized by enteric microbiota and the related anti-cancer activity is not clear. In this study, using human enteric microbiome incubation and HPLC analysis, we observed that baicalin can be quickly converted to ...
Alzheimer's disease (AD) is an age-related neurodegenerative disorder, the incidence of which is climbing with ever-growing aged population, but no cure is hitherto available. The epidemiological studies unveiled that chronic intake of flavonoids was negatively associated with AD risk. Flavonoids, a family of natural polyphenols widely distributed in human daily diets, were readily conjugated by phase II drug metabolizing enzymes after absorption in vivo, and glucuronidation could occur in 1 min...
Uridine diphosphate (UDP)-glucuronosyl-transferases (UGTs) are enzymes involved in the biotransformation of important endogenous compounds such as steroids, bile acids, and hormones as well as exogenous substances including drugs, environmental toxicants, and carcinogens. Here, a novel fluorescent probe BDMP was developed based on boron-dipyrromethene (BODIPY) with high sensitivity for the detection of UGT1A8. The glucuronidation of BDMP not only exhibited a redemission wavelength (λex/λem = 500...
Transient receptor potential (TRP) channels are non-selective cation channels that are implicated in analgesia, bowel motility, wound healing, thermoregulation, vasodilation and voiding dysfunction. Many natural products have been reported to affect the activity of TRP channels. We hypothesize that numerous traditional herbal medicines (THMs) might exert their pharmacological activity through modulating the activity of TRP channels. The present study aimed to evaluate the effects of flavonoid ag...
Stroke is a leading cause of death and disability worldwide, and approximately 87% of cases are attributed to ischemia. The main factors that cause ischemic stroke include excitotoxicity, energy metabolism disorder, Ca+ overload, oxidative damage, apoptosis, autophagy, and inflammation. However, no effective drug is currently available for the comprehensive treatment of ischemic stroke in clinical applications; thus, there is an urgent need to find and develop comprehensive and effective drugs t...
#1Laiyun Xin(SDUTCM: Shandong University of Traditional Chinese Medicine)H-Index: 1
#2Jialiang Gao(Peking Union Medical College)H-Index: 7
Last. Xiangning Cui(Peking Union Medical College)H-Index: 4
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Cardiovascular disease is the leading cause of high morbidity and mortality worldwide,wnich emphasizes the urgent necessity to develop new pharmacotherapies.In eastern countries, traditional Chinese medicine Scutellaria baicalensis has been widely used clinically for thousands of years. Baicalin is one of the main active ingredients extracted from Chinese medicine Scutellaria baicalensis. Emerging evidences have established that baicalin improves chronic in flammation, immune imbalance, disturba...
#2Vaishali Aggarwal(PGIMER: Post Graduate Institute of Medical Education and Research)H-Index: 10
Last. Manoj Kumar(Maharishi Markandeshwar University, Mullana)H-Index: 6
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Abstract Cancer, being a multifactorial disease has diverse presentation in different subgroups which is mainly attributed to heterogenous presentation of tumor cells. This cancer cell heterogeneity is the major reason for variable response to standard chemotherapeutic regimes owing to which high relapse rate and multi-drug resistance has increasingly been reported over the past decade. Interestingly, the research on natural compounds in combination with standard therapies have reported with int...
#1Yaqing Zhang(CPU: China Pharmaceutical University)H-Index: 2
#2Mei Zhang(CPU: China Pharmaceutical University)H-Index: 2
Last. Rui Song(CPU: China Pharmaceutical University)H-Index: 15
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Abstract Ethnopharmacological relevance A traditional Chinese medicine (TCM) prescription follows the principle of compatibility (peiwu) to achieve the fundamental purpose: to increase efficacy and reduce toxicity. Rhei rhizoma, commonly known as Chinese rhubarb, is the most frequently used herb with Radix Scutellariaee. This classic fixed compatibility is considered for heat-clearing, qi regulation and detoxifying to gain better efficacy and reduce cytotoxicity with respect to unilateral medici...
#1Robert Ancuceanu(UMFCD: Carol Davila University of Medicine and Pharmacy)H-Index: 11
#2Mihaela Dinu(UMFCD: Carol Davila University of Medicine and Pharmacy)H-Index: 6
Last. Vlad Negulescu(UMFCD: Carol Davila University of Medicine and Pharmacy)H-Index: 2
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B-ring unsubstituted flavones (of which the most widely known are chrysin, baicalein, wogonin, and oroxylin A) are 2-phenylchromen-4-one molecules of which the B-ring is devoid of any hydroxy, methoxy, or other substituent. They may be found naturally in a number of herbal products used for therapeutic purposes, and several have been designed by researchers and obtained in the laboratory. They have generated interest in the scientific community for their potential use in a variety of pathologies...
#1Ting Huang(HUST: Huazhong University of Science and Technology)H-Index: 1
#2Yanan Liu(HUST: Huazhong University of Science and Technology)H-Index: 1
Last. Chengliang Zhang(HUST: Huazhong University of Science and Technology)H-Index: 12
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Baicalin is one of the major bioactive components of Scutellaria radix, a Chinese herb that has been used since ancient times. Baicalin has various pharmacological activities, including antitumor, antimicrobial, and antioxidant, and has wide clinical applications. Baicalin displays a distinct pharmacokinetic profile including gastrointestinal hydrolysis, enterohepatic recycling, carrier-mediated transport, and complicated metabolism. The in vivo disposition of baicalin is affected by combination...
