Drug Design Development and Therapy
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2017
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IF 2.822
Bohong Guo,Danqiao Xu,Xiaohong Liu,Jun Yi
In this study, folate–poly(ethylene glycol)3400–cholesterol conjugates (FA–PEG–Chol) were enzymatically synthesized in one step and incorporated into liposomes to prepare folate (FA)-functionalized liposomes for targeted drug delivery. The FA-functionalized liposomes loaded with betulinic acid (BA) (FA-L-BA) were prepared by thin lipid film method. The FA-L-BA was characterized by their morphology, particle size, zeta potential, encapsulation efficiency (EE), stability, cell cytotoxicity and cellular uptake. The average size of FA-L-BA was 222±8 nm. The spherical particles exhibited a negative electrical charge of −20.12±1.45 mV and high EE of 91.61%±1.16%. The liposomes were taken up selectively by HepG2 cells. FA-L-BA showed enhanced cytotoxicity (50% inhibitory concentration [IC50] =63.07±2.22 μg/mL) compared to nontargeted control normal liposomes loaded with BA (L-BA; IC50 =93.14±2.19 μg/mL) in HepG2 cells in vitro. In addition, FA-functionalized liposomes loaded with Ir-1 (FA-L-Ir-1) showed significantly higher cellular uptake in HepG2 cells compared to nontargeted control normal liposomes loaded with Ir-1 (L-Ir-1). This novel approach for the liposomes surface modified with FA by a one-step enzymatic amidation was expected to provide potential application as a drug carrier for active targeted delivery to tumor cells.
研究领域:
药剂学
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肿瘤学
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生物化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
FOOD RESEARCH INTERNATIONAL
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2025
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IF 8
Xiaoting Wang,Shiyao Fu,Ying Han,Xuening Yang,Jing Wang,Xin Yang
The research constructed a co-assembly nanoparticles (NPs) of ursolic acid (UA) and betulinic acid (BA) as carriers to load the active substance curcumin (CCM) by co-precipitation method, aiming to improve the stability and bioavailability of CCM in the human body and enabling CCM to play more functions in the production of functional foods. The average particle size of UA-BA-CCM NPs was 222.6 nm and zeta potential was −26.63 mV. The UA-BA-CCM NPs had small size and great stability. The drug loading was up to 20.42 %. Moreover, the hydrogen bonds and π-π stacking existed in the three molecules. The result was verified by Molecular Dynamics Simulation, FITR, and UV experiments. In simulated in vitro release experiments, the release rate of the NPs was lower than free CCM in gastric phase, improving CCM bioavailability. Meanwhile, the UA-BA-CCM NPs performed better clearing free radicals than free CCM. Thus, UA-BA-CCM NPs delivery system not only could improve stability and bioavailability of CCM, but also might make CCM play a role in the functional food.
研究领域:
食品科学
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药剂学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2018
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IF 3.909
Jianan Wu,Yongwu Niu,Yingchun Jiao,Qihe Chen
Agaricus bisporus (Lange) Sing. Chaidam, a special brown mushroom with thick body indigenous in Chaidam basin, was used for fungal chitosan extraction. FTIR, XRD and DSC spectra showed that fungal chitosan was similar to commercial chitosan from aquatic sources. Fungal chitosan and commercial chitosan were used to coat on betulinic acid-loaded liposomes modified with biosurfactants mannosylerythritol lipid A (MEL-A), respectively. After chitosan coating, the mean size, zeta potential and encapsulation efficiency of both liposomes increased. The liposomes coated with fungal chitosan were discovered to have smaller size and higher zeta potential. Furthermore, the wall material MEL-A and coating material chitosan endue liposomes with increased antioxidant capacity. Fungal chitosan coated liposomes also have stronger antioxidant effects than commercial chitosan. The findings implied that the fungal chitosan coated liposomes modified with MEL-A can be considered as a promising delivery system with enhanced antioxidant effects for bioactive compounds.
研究领域:
药剂学
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材料科学
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食品科学
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生物技术
✓ 已验证
DOI
PubMed
高影响因子
PHYTOMEDICINE
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2025
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IF 8.3
Wenying Qi,Xu Cao,Yue Chen,Hening Chen,Ningyi Zhang,Ruijia Liu,Wei Wang,Qiyao Liu,Shihao Zheng,Size Li,Xiaoke Li,Xiaobin Zao,Yong'an Ye
Background Metabolic-associated fatty liver disease (MAFLD) is a prevalent chronic liver condition globally, characterized by suboptimal treatment outcomes. Traditional therapies often fail to address the multifaceted pathogenesis of MAFLD, which involves lipid metabolism, inflammation, and gut–liver axis dysregulation. JiGuCao Capsule formula (JCF), a patented Chinese medicine, has demonstrated clinical efficacy in liver disease treatment, indicating its potential as a new therapeutic option for MAFLD. Purpose This study aimed to investigate the therapeutic effects and underlying mechanisms of JCF in treating MAFLD, particularly focusing on its impact on liver pathology, intestinal health, and gut microbiota composition. Methods A MAFLD mouse model was developed by administering a high-fat diet and 5% fructose water for 16 weeks. At week 8, mice exhibited significant steatosis, inflammation, and insulin resistance. Fifty mice were allocated into two groups: the normal diet (ND) group with 19 mice and the high-fat feed diet (HFD) group with 31 mice. Seven mice from each group were sacrificed at week 8 for serological and histopathological assessments. The remaining mice were allocated into ND ( n = 6), HFD ( n = 6), HFD + JCFL (human equivalent dose,780 mg/kg, n = 6), HFD + JCFH (threefold the human equivalent dose, 2340 mg/kg, n = 6), HFD + Polyene Phosphatidylcholine (PPC) (human equivalent dose,177.84 mg/kg, n = 6) and ND+ JCF (human equivalent dose,780 mg/kg, n = 6) groups. Daily gavage started at week 9. At week 16, after fasting, body weight and liver condition were recorded, and mice were euthanized with pentobarbital sodium. Mouse tissues and feces were collected for histopathological, molecular biological, and multi-omics analyses. Results JCF effectively slowed MAFLD progression in mice by decreasing hepatic lipid accumulation and inflammation. Treatment with JCF significantly reduced hepatic triglycerides and inflammatory markers, including TNF-α and IL-6. JCF enhanced lipid metabolism, repaired the intestinal barrier, and lowered inflammatory cytokines in the intestines, as indicated by reduced serum LPS and restored tight junction proteins expression, such as claudin-1 and occludin. Fecal microbiota analysis indicated that JCF treatment elevated Lactobacillus levels and reduced Colidextribacter levels, correlating with enhanced metabolic profiles. The primary bioactive compounds identified in JCF responsible for these therapeutic effects were betulinic acid, cholic acid, deoxycholic acid, oleanolic acid, and pectolinarigenin. Transcriptomic analysis showed that JCF regulated key pathways involved in lipid metabolism, including the pparγ–cd36 axis and modulation of ox-LDL levels. The results indicate that JCF effectively mitigates MAFLD by influencing the gut-liver axis and lipid metabolism. Conclusion JCF alleviates MAFLD by modulating the gut–liver axis and lipid metabolism. Its effects involve improving gut barrier function, regulating microbiota, and targeting the pparγ–cd36 axis. Active compounds like betulinic acid support its therapeutic potential. JCF shows promise as a novel treatment for MAFLD, with further clinical studies needed.
研究领域:
药理学
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肝病学
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微生物组研究
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代谢研究
✓ 已验证
产品关联
DOI
PubMed
高影响因子
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