APPLIED BIOCHEMISTRY AND BIOTECHNOLOGY
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2023
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IF 3
Zhao Xia,Guo Meijing,Li Xian,Liu Bo,Li Binglin,Wang Jiao
Phospholipase D (PLD) with the higher transphosphatidylation activity was screened from Streptomyces sp. LD0501 basing on the protoplast mutagenesis technology. Then, it was successfully bio-imprinted to form a hyperactivated structure and rigidified by the intramolecular cross-linking, which was immobilized on the nonporous nanoscale silica. Characterization techniques were employed to investigate the structure and physicochemical properties of the catalysts, including Fourier transform infrared (FTIR) spectra and scanning electron microscopy (SEM) analysis. Transphosphatidylation activity and selectivity were improved significantly when immobilized PLD was used. The maximum yield for the production of phosphatidylserine (PS) reached 97% and the side reaction, the hydrolysis, was minimized. These results were further confirmed by the nuclear magnetic resonance (NMR) and mass spectrometry (MS) analysis. The imprint-induced characteristics of PLD was successfully “remembered” even in the present of much water. In addition, this immobilized hyperactivated PLD showed the excellent operational stabilities and environmental tolerances. Graphical abstract
研究领域:
生物化学
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酶工程
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DOI
PubMed
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
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2019
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IF 3.414
Jin-Xiu Liang,Qun-Qun Zhang,Yan-Fei Huang,Han-Qing Pang,Xin-Guang Liu,Wen Gao,Ping Li,Hua Yang
Ethnopharmacological relevance Monascus -fermented rice product (MFRP) has been regarded as a dietary supplement and traditional medicine with circulation-promoting effects in China and other countries for centuries. Aim of the study This study was carried out to profile the chemical components in MFRP, and provide available information for elucidating the potential lipid-lowering compounds other than monacolins. Materials and methods High-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (HPLC-QTOF MS) and gas chromatography coupled with mass spectrometry (GC-MS) methods were applied to comprehensive analysis of chemical components in MFRP. Potential small molecules were identified by comparing with reference standards, or tentatively characterized by comparing their retention time and high-resolution mass spectral data with previous literature. The lipid-lowering properties of ten major non-monacolin compounds were evaluated in cholesterol-fed zebrafish larvae. And one with optimum lipid-lowering activity was subsequently evaluated in high fat diet-fed C57BL/6 J mice, with the dyslipidemia and ectopic lipid deposition being investigated. Results A total of 99 compounds were characterized in MFRP, including 38 monacolins, 5 decalins , 6 isoflavones , 13 pigments, 8 azaphilonoids, 11 amino acids, 4 nucleosides , 9 lipid acids, 4 phytosterols and glycerol. The preliminary screening showed that ergosterol remarkably reduced cholesterol levels in zebrafish larvae. Moreover, ergosterol delayed body weight gain and decreased circulating total cholesterol, triglyceride , low density lipoprotein cholesterol levels in high fat diet-fed mice. Ectopic lipid accumulation was also ameliorated in the liver and heart of obese mice . Conclusion Global analysis of chemical components and screening of lipid-lowering non-monacolin compounds in MFRP have improved our understanding of its therapeutic material basis.
研究领域:
药理学
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代谢组学
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营养学
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PubMed
高影响因子
ACS Applied Bio Materials
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2019
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IF 0
Dong Wang,Xuecheng Zhang,Hui Li,Yuxia Luan,Guangcheng Wei,Jiqian Wang
Molecular modification and self-assembly are clinically proved successful strategies in drug design to enhance the treatment efficiency. Herein, the lipidation method is used to modify the anticancer tripeptides tyoservaltide (YSV) into lipidated YSV, C16-EEYSV-NH2, and C16–KKYSV-NH2. We found the lipidated YSV performed better aggregation property from the critical aggregation concentration (CAC) measurements, transmission electron microscope (TEM) and atomic force microscope (AFM) observation. The cytotoxicity experiments showed that the lipidated YSV had better anticancer efficiency due to their excellent self-assembly. Meantime, the lipidated YSV shows superior biostability and cells internalization which can be proved by high performance liquid chromatography (HPLC), inverted fluorescence microscope, and flow cytometry (FCM). For in vivo experiments, the results also showed that lipidated YSV have better performance, and the final histology analysis shows low toxicity to the body organs. Considering the advantages of lipidated YSV, we hope that our study would demonstrate a powerful strategy to improve the application of peptide drugs.
研究领域:
药学
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生物技术
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癌症研究
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材料科学
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PubMed
INTERNATIONAL JOURNAL OF PHARMACEUTICS
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2025
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IF 5.2
Honglin Li,Ya Chen,Yue Qiu
Autism spectrum disorder (ASD) is a neurodevelopmental condition characterized by deficits in social interaction and repetitive, stereotyped behaviors. There is no universally effective pharmacological treatment targeting its core symptoms. Oxytocin, an endogenous polypeptide known as the “social hormone”, has shown potential in improving emotional recognition and social interactions in individuals with ASD. However, its clinical application has been limited due to its short half-life and poor blood–brain barrier penetration. To address these challenges, we utilized peptide lipidation technology to enhance the pharmacokinetic properties and brain bioavailability of oxytocin. A series of lipidated oxytocin analogs was designed and synthesized, exhibiting superior brain distribution and pharmacokinetic profiles in valproic acid-induced autistic rat models compared to unmodified oxytocin. Among these analogs, C16-modified oxytocin (C16-OT), administered intrathecally, achieved the most extensive brain distribution with limited presence in the blood, resulting in long-lasting improvements in autistic behaviors. These improvements, including enhanced social behaviors and reduced stereotypical actions, were sustained for up to 42 days, contrasting with the brief effects typically reported in previous studies. Furthermore, a comparison of administration routes revealed that intrathecal injection achieved higher brain concentrations and more prolonged social behavioral improvements than intranasal delivery. These findings provide robust preclinical evidence that C16-OT, through optimized lipidation and intrathecal delivery, offers sustained central nervous system activity and significant, long-term reversal of social behavioral deficits in rats with autism.
研究领域:
神经科学
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药理学
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行为科学
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分子生物学
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PubMed
高影响因子
BIOTECHNOLOGY PROGRESS
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2019
·Vol. 35
·期 3
·e2777
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IF 2.406
Binglin Li,Jiao Wang,Jing Li,Xiaoli Zhang,Wenyu Yu,Huan Wang,Dandan Duan,Binxia Zhao
The efficient and environmentally friendly aqueous-solid systems employed Triton-X-100-modified silica as the “artificial interface” to adsorb phosphatidylcholine (PC) in purely aqueous solutions and silica-adsorbed PC was successfully used for phospholipase D (PLD)-mediated transphosphatidylation. Three kinds of silicas with different sizes were employed to investigate advantages and disadvantages of batch and continuous technologies for PLD-catalyzed transphosphatidylation in aqueous-solid systems. The highest yields of product were obtained in the batch technology, but the continuous production had the simplest operational process and highest space–time yield. After transphosphatidylation, the product adsorbed on carriers were eluted by coconut oil and used to manufacture relevant hard, soft, and micro-capsules. Special attention has been paid to the preparation of microcapsules. Toxic solvents were completely avoided in the whole technological process including production and product packaging. © 2019 American Institute of Chemical Engineers Biotechnol. Prog ., 35: e2777, 2019.
研究领域:
化学工程
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生物技术
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环境科学
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PubMed
高影响因子
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