PROGRESS IN NEURO-PSYCHOPHARMACOLOGY & BIOLOGICAL PSYCHIATRY
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2022
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IF 5.201
Lina Ruan,Kaiyu Guan,Yue Wang,Ming Gu,Yue Chen,Lisha Cai,Ruixuan Ye,Zhengwei Huang,Anqi Guo,Zhengkang Su,Xi Li,Jianchun Pan
Post-traumatic stress disorder (PTSD) is a serious mental disease featured by a stress dysfunction that occurs after an individual has faced intense mental stress, often accompanied by anxiety and chronic pain. Currently, the mainstream drug for PTSD is serotonin reuptake inhibitors (SSRIs), however, their pain management for patients is limited. Baicalein , a Chinese traditional herbal medicine, has shown promising results in treating anxiety, depression, and pain. In this study, we found that baicalein may alleviate single prolonged stress (SPS)-induced PTSD-like behaviors in mice without altering baseline nociceptive sensitivity or activity. Meanwhile, baicalein increased the noradrenaline (NE) and serotonin (5-HT) content and decreased the ratio of 5-hydroxyindoleacetic acid (5-HIAA)/5-HT by inhibiting the activity of monoamine oxidase A (MAO-A) in SPS-induce mice. The anxiolytic and antinociceptive effects induced by baicalein were totally abolished by 5-HT depleting agents. Moreover, the anxiolytic effects of baicalein could be abolished by the 5-HT 1A receptor antagonist WAY-100635, and the analgesic effects could be abolished by delta-opioid receptor antagonists in the spinal. Taken together, our study provides compelling evidence that baicalein reversed anxiety-like behaviors and neuropathic pain in PTSD through serotonergic system and spinal delta-opioid receptors.
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Food and Bioprocess Technology
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2024
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IF 5.3
Fu Jin-Xian,Jiao Jiao,Gai Qing-Yan,He Xiao-Jia,Fu Yu-Jie,Feng Xue,Gao Jie
Baicalein and wogonin, two health-promoting flavonoid aglycones in Scutellaria baicalensis Georgi roots, have better bioactivity and bioavailability than their glycoside precursors (baicalin and wogonoside). The search for novel microorganisms for the fermentation of S. baicalensis roots to improve the yields of baicalein and wogonin is of great interest in the food and nutraceutical industries. In this study, a novel endophytic fungus ( Penicillium rubens ) capable of producing cellulase (0.82 ± 0.12 U/mL) and β-glucosidase (4.55 ± 0.97 U/mL) was used to ferment S. baicalensis roots to obtain high yields of baicalein and wogonin. Semi-solid-state fermentation with homogeneous fungal cultures was found to be the appropriate strategy. Under the optimal fermentation parameters (temperature 30 °C, inoculation dose of fungal cultures 4 mL/g, and time 60 h), the yields of baicalein and wogonin (46.95 ± 4.98 mg/g DW and 31.41 ± 9.36 mg/g DW) from S. baicalensis roots were tremendously increased by 16.13-fold and 15.47-fold over control, respectively. Results of industrial enzyme bioprocessing and scanning electron microscope indicated that the remarkable increase in aglycone product yields could be due to the synergistic effects of cellulase and β-glucosidase produced by P. rubens on cell wall hydrolysis and glycoside deglycosylation. In addition, extracts of S. baicalensis roots fermented by P. rubens showed a significant increase in antioxidant and antimicrobial activities. Overall, the semi-solid-state fermentation of S. baicalensis roots using the novel P. rubens was an effective strategy that could yield high quantities of baicalein and wogonin, which had promising potential in the food and nutraceutical industries. Graphical Abstract
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EUROPEAN JOURNAL OF PHARMACOLOGY
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2024
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IF 4.2
Yufang Ma,Zhenming Ma,Yiyuan Zhang,Chunyun Luo,Puxin Huang,Jing Tong,Hong Ding,Honghui Liu
Apigenin and baicalein are structurally related flavonoids that have been reported to have multiple pharmacological activities. The aim of this study was to investigate the protective effects and potential mechanisms of apigenin and baicalein in D-galactose-induced aging rats. First, apigenin and baicalein showed remarkable antioxidant activity and anti-glycation activity in vitro. Secondly, the protective effects of apigenin and baicalein on aging rats were investigated. We found that apigenin and baicalein supplementation significantly ameliorated aging-related changes such as declines in the spatial learning and memory and histopathological damage of the hippocampus and thoracic aorta. In addition, our data showed that apigenin and baicalein alleviated oxidative stress as illustrated by decreasing MDA level, increasing SOD activity and GSH level. Further data showed that they significantly reduced the accumulation of advanced glycation end products (AGEs), inhibited the expression of RAGE, down-regulated phosphorylated nuclear factor (p–NF–κB (p65)). Our results suggested that the protective effects of apigenin and baicalein on aging rats were at least partially related to the inhibition of AGEs/RAGE/NF-κB pathway and the improvement of oxidative damage. Overall, apigenin and baicalein showed almost equal anti-aging efficacy. Our results provided an experimental basis for the application of apigenin and baicalein to delay the aging process.
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ENVIRONMENTAL POLLUTION
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2023
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IF 8.9
Xiaojing Li,Qian Wu,Dan Chen,Yichen Bai,Yuhong Yang,Shiwen Xu
Cadmium (Cd) is a major contaminant in natural environments and exerts adverse effects on aquatic biota at low concentrations. Gill is as vital respiratory organ and may cause pollutants to enter fish during gas exchange. Baicalein (BAI), as a kind of flavonoids, possess antioxidant properties through inactivating free radicals. To confirm the potential effects and approaches of BAI addition in maintaining the gill stability, 90 common carps ( Cyprinus carpio L.) were selected and randomly divided into water environment exposure group (0.22 mg/L Cd) and/or feed added with 0.10 g/kg BAI for 30 days. The analysis of ion content in serum showed that Cd exposure disturbed ion homeostasis , and BAI could reduce serum Cd concentration. The histopathological results of gills showed that Cd exposure caused gill tissue lesions and structural damage, and BAI feeding effectively alleviated this damage. In addition, BAI could enhance antioxidant activity and activate Nrf2/HO-1 axis, thereby reducing oxidative stress and endoplasmic reticulum (ER) stress. Moreover, BAI lightened cytokine imbalance, inflammatory response, and necroptosis. Overall, the results indicated that BAI feeding could maintain gill homeostasis against Cd poisoning via the ROS/ER stress signaling. This trial revealed the properties of BAI resistance to metal Cd in aquaculture and partially elucidated its mechanism.
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JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY
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2017
·Vol. 72
·期 9
·2562-2569
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IF 5.071
Dai Chongshan,Tang Shusheng,Wang Yang,Velkov Tony,Xiao Xilong
BackgroundNephrotoxicity is the major adverse effect patients experience during colistin therapy. The development of effective nephroprotective agents that can be co-administered during polymyxin therapy remains a priority area in antimicrobial chemotherapy.ObjectivesTo investigate the nephroprotective effect of baicalein, a component of the root of Scutellaria baicalensis, against colistin-induced nephrotoxicity using a mouse model.MethodsC57BL/6 mice were randomly divided into the following groups: control, baicalein 100 mg/kg/day (administered orally), colistin (18 mg/kg/day administered intraperitoneally) and colistin (18 mg/kg/day) plus baicalein (25, 50 and 100 mg/kg/day). After 7 day treatments, histopathological damage, the markers of renal functions, oxidative stress and inflammation were examined. The expressions of Nrf2, HO-1 and NF-κB mRNAs were also further examined using quantitative RT–PCR examination.ResultsBaicalein co-administration markedly attenuated colistin-induced oxidative and nitrative stress, apoptosis, the infiltration of inflammatory cells, and caused decreases in IL-1β and TNF-α levels (all P < 0.05 or 0.01) in the kidney tissues. Baicalein co-administration up-regulated expression of Nrf2 and HO-1 mRNAs and down-regulated the expression of NF-κB mRNA, compared with those in the colistin alone group.ConclusionsTo the best of our knowledge, this is the first study demonstrating the protective effect of baicalein on colistin-induced nephrotoxicity and apoptosis by activating the antioxidant defence mechanism in kidneys and down-regulating the inflammatory response. Our study highlights that oral baicalein could potentially ameliorate nephrotoxicity in patients undergoing polymyxin therapy.
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POULTRY SCIENCE
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2024
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IF 3.8
Jianting Gao,Yingsai Fan,Chenyue Lu,Xinghua Zhao,Xin He
ABSTRACT Baicalein ( BAI ) is a natural flavonoid with antioxidant, antitumor and antibacterial properties. However, the bioavailability of BAI was limited due to low solubility. This study aims to improve the solubility of BAI through the amorphous solid dispersion ( ASD ) and evaluate changes in its pharmacokinetics and pharmacodynamics in Taihang chickens. Polyethylene caprolactam-polyvinyl acetate-polyethylene glycol grafted copolymer ( Soluplus ) was chosen as the carrier, and ASD was prepared by rotary evaporation and was characterized by powder X-ray diffractions ( PXRD ), differential scanning calorimetry (DSC ) and fourier transform infrared spectroscopy (FT-IR ). In vitro dissolution assays were used to screen the optimal ratio of drug to carrier, in vivo pharmacokinetic assays were conducted to investigate the promoting effect on the absorption. In addition, the effects of ASD on the growth performance, meat quality, antioxidant capacity and intestinal flora were investigated. ASD (1:9 and 2:8) did not exhibit crystal diffraction peaks of BAI in PXRD or endothermic peaks in DSC, indicating the successful preparation of ASD. The results of in vitro dissolution assay showed that the cumulative dissolution rate of ASD (2:8) within 600 min was 52.67%, which was 7.84-fold higher than BAI. The pharmacokinetic results showed that the peak concentration ( C max ) and the area under the drug-time curve ( AUC 0∼24 ) of ASD (2:8) was (5.20 ± 0.82) μg/mL and (17.03 ± 0.67) μg·h/mL, which was 1.91 and 2.64-fold higher than BAI, respectively. Dietary supplementation of BAI and ASD could increase average daily gain ( ADG ), while decrease feed conversion ratio ( FCR ), but there was no significant difference ( P > 0.05). The drip loss of BAIASD group was lower than BAI group ( P < 0.05). In addition, the antioxidant capacity of Taihang chickens were enhanced, the diversity and the abundance of beneficial bacteria was improved. Results of BAI upon the dietary supplementation tested in Taihang chickens, after preparation of ASD, indicating a superior enhancement effect in growth performance, meat quality, antioxidant capacity and intestinal flora due to an improved solubility and optimized bioavailability.
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JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
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2023
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IF 5
Xin Liu,Wei Niu,Jiamin Liu,Zhao Cui,Jiazheng Li,Zhenhai Zhang,Jianming Ju
β-cyclodextrin and hydroxypropyl-β-cyclodextrin were combined with baicalein to improve its solubility in water. The physicochemical properties and pharmacokinetic characteristics of the two complexes and their therapeutic effects on dextran sulfate sodium-induced ulcerative colitis were studied in mice. Differential scanning calorimetry , X-ray diffraction, infrared spectroscopy , and scanning electron microscopy showed that the two complexes were successfully prepared and significantly improved baicalein's solubility and dissolution. The t 1/2 , C max , and AUC 0-∞ values of the inclusion complexes were substantially better than those of the original drug in rats. Analysis of the tissue distribution of acute ulcerative colitis in mice showed that the peak concentrations of baicalein and its metabolite, baicalin , in the small intestines, liver, and colon were higher than that of the free drug. The therapeutic effect of the inclusion compound was significantly better than that of the original drug. This study provides a new reference for applying cyclodextrin inclusion complex in ulcerative colitis.
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MICROCHEMICAL JOURNAL
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2024
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IF 4.9
Xiaoqian Sun,Rongjie Li,Yilin Wang,Kaijia Liu,Yuhui Qiu,Kunxiang Deng,Yixi Xie,Pengcheng Zhao,Junjie Fei
The remarkable pharmacological activities of flavonoids and their effects on human health have prompted many studies. To solve the problem that flavonoids are difficult to be accurately quantified, a novel photoelectrochemical (PEC) sensor based on CdIn 2 S 4 /b-TiO 2 /GO was created to detect the baicalein (BCA). By using physical ultrasonic compounding, a straightforward and effective CdIn 2 S 4 /b-TiO 2 /GO composite was created. The composite’s photoelectric effect was 14 times greater than that of the individual material. When BCA was present, a flavonoid-TiO 2 nanoconjugate was formed based on the interaction between b-TiO 2 and BCA. This interaction prevented the formation and decreased charge transfer of photoporous holes, resulting in a significant decline in photocurrent. Therefore, the PEC sensor based on the change of the electrode surface state can realize the sensitive detection of BCA. The PEC sensor has a wide linear detection range of 1 nM − 30 μM with a limit of detection of 0.5 nM. In addition, the sensor has exhibited excellent accuracy in detecting BCA in the roots and leaves of Scutellaria baicalensis, which can be used for the detection of actual samples.
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