1.Ameliorating vascular endothelial injury for lipolysacharide-induced via mitochondrial targeting function of octaarginine-modified essential oil from Fructus Alpiniae zerumbet (EOFAZ) lipid microspheres.
Lingyan LI ; Zengqiu YANG ; Qiqi LI ; Qianqian GUO ; Xingjie WU ; Yu'e WANG ; Xiangchun SHEN ; Ying CHEN ; Ling TAO
Chinese Herbal Medicines 2025;17(2):340-351
OBJECTIVE:
To investigate the therapeutic potential of octaarginine (R8)-modified essential oil from Fructus Alpiniae zerumbet (EOFAZ) lipid microspheres (EOFAZ@R8LM) for cardiovascular therapy.
METHODS:
EOFAZ@R8LM was developed by leveraging the volatilization of EOFAZ and integrating it with the oil phase of LM, followed by surface modification with cell-penetrating peptide R8 to target the site of vascular endothelial injury. The therapeutic effects of this formulation in alleviating lipopolysaccharide-induced vascular endothelial inflammation were evaluated by assessing mitochondrial membrane potential (MMP), intracellular reactive oxygen species (ROS) levels, as well as inflammatory factors interleukin-6 (IL-6) and interleukin-1β (IL-1β) levels.
RESULTS:
EOFAZ@R8LM effectively delivered EOFAZ to the site of injury and specifically targeted the mitochondria in vascular endothelial cells, thereby ameliorating mitochondrial dysfunction through regulation of MMP and reduction of intracellular ROS levels. Moreover, it attenuated the expression levels of IL-6 and IL-1β, exerting protective effects on the vascular endothelium.
CONCLUSION
Our findings highlight the significant therapeutic potential of EOFAZ@R8LM in cardiovascular therapy, providing valuable insights for developing novel dosage forms utilizing EOFAZ for effective treatment against cardiovascular diseases.
2.Effect of cholesterol on distribution, cell uptake, and protein corona of lipid microspheres at sites of cardiovascular inflammatory injury.
Lingyan LI ; Xingjie WU ; Qianqian GUO ; Yu'e WANG ; Zhiyong HE ; Guangqiong ZHANG ; Shaobo LIU ; Liping SHU ; Babu GAJENDRAN ; Ying CHEN ; Xiangchun SHEN ; Ling TAO
Journal of Pharmaceutical Analysis 2025;15(7):101182-101182
Cholesterol (CH) plays a crucial role in enhancing the membrane stability of drug delivery systems (DDS). However, its association with conditions such as hyperlipidemia often leads to criticism, overshadowing its influence on the biological effects of formulations. In this study, we reevaluated the delivery effect of CH using widely applied lipid microspheres (LM) as a model DDS. We conducted comprehensive investigations into the impact of CH on the distribution, cell uptake, and protein corona (PC) of LM at sites of cardiovascular inflammatory injury. The results demonstrated that moderate CH promoted the accumulation of LM at inflamed cardiac and vascular sites without exacerbating damage while partially mitigating pathological damage. Then, the slow cellular uptake rate observed for CH@LM contributed to a prolonged duration of drug efficacy. Network pharmacology and molecular docking analyses revealed that CH depended on LM and exerted its biological effects by modulating peroxisome proliferator-activated receptor gamma (PPAR-γ) expression in vascular endothelial cells and estrogen receptor alpha (ERα) protein levels in myocardial cells, thereby enhancing LM uptake at cardiovascular inflammation sites. Proteomics analysis unveiled a serum adsorption pattern for CH@LM under inflammatory conditions showing significant adsorption with CH metabolism-related apolipoprotein family members such as apolipoprotein A-V (Apoa5); this may be a major contributing factor to their prolonged circulation in vivo and explains why CH enhances the distribution of LM at cardiovascular inflammatory injury sites. It should be noted that changes in cell types and physiological environments can also influence the biological behavior of formulations. The findings enhance the conceptualization of CH and LM delivery, providing novel strategies for investigating prescription factors' bioactivity.
3.Study on Diversity of Intestinal Flora of Patients with Large Intestine Damp Heat Syndrome and Ulcerative Colitis By High-Throughput Sequencing
Panghua DING ; Juniang LI ; Yi GUO ; Tangyou MAO ; Xingjie ZHAO
World Science and Technology-Modernization of Traditional Chinese Medicine 2018;20(6):967-973
Objective: To explore the difference of intestinal flora between groups of ulcerative colitis and large intestine dampness heat syndrome and healthy group. Methods: A total of 14 stool samples from patients with ulcerative colitis and large intestine dyspepsia syndrome and 14 samples of healthy people were collected. Amplification was designed based on the 16 S r DNA V3-V4 region of the bacteria. Illumina HiSeq 2500 platform was used for high-throughput sequencing.The ultimately sample species information was get by Reads splicing, OTUs (operational taxonomic units) clustering, species annotation, the analysis of alpha diversity and the analysis of principal component. Results: There was a significant difference in intestinal flora between the ulcerative colitis group and the healthy group (P=0.008 < 0.01); and the diversity of intestinal flora in patients with ulcerative colitis and large intestine dyspepsia syndrome was higher than that of healthy people. There a significant difference in the richness degree of intestinal flora patients with ulcerative colitis and large intestine dampness syndrome and the healthy group. Intestinal flora centered on Lactobacillus、Lactobacillaceae、Erysipelotrichaceae、Erysipelotrichales and Akkermansia bacteria was rich in patients with ulcerative colitis. Conclusion: There are significant differences in intestinal flora diversity and bacterial structure between patients with ulcerative colitis and large intestine dampness syndrome and the healthy group.
4.Nanotechnology-based strategies for treatment of ocular disease.
Yuhua WENG ; Juan LIU ; Shubin JIN ; Weisheng GUO ; Xingjie LIANG ; Zhongbo HU
Acta Pharmaceutica Sinica B 2017;7(3):281-291
Ocular diseases include various anterior and posterior segment diseases. Due to the unique anatomy and physiology of the eye, efficient ocular drug delivery is a great challenge to researchers and pharmacologists. Although there are conventional noninvasive and invasive treatments, such as eye drops, injections and implants, the current treatments either suffer from low bioavailability or severe adverse ocular effects. Alternatively, the emerging nanoscience and nanotechnology are playing an important role in the development of novel strategies for ocular disease therapy. Various active molecules have been designed to associate with nanocarriers to overcome ocular barriers and intimately interact with specific ocular tissues. In this review, we highlight the recent attempts of nanotechnology-based systems for imaging and treating ocular diseases, such as corneal d iseases, glaucoma, retina diseases, and choroid diseases. Although additional work remains, the progress described herein may pave the way to new, highly effective and important ocular nanomedicines.
5.Comparative study on different anti-adhesion agents in preventing tubal obstruction after interventional recanalization
Yi HUANG ; Zhenzhen GUO ; Hanwei CHEN ; Weihua LIANG ; Yan XU ; Li YANG ; Zhitao LIANG ; Xingjie WU ; Li HE
Chinese Journal of Obstetrics and Gynecology 2009;44(11):821-824
Objective To study the efficacy of different anti-adhesion agents used in preventing tubal obstruction after recanalization.Methods Five hundred and eight patients with tubal obstruction were divided into 245 cases in control group,108 cases in chitosan group;113 cases in sodium hyaluronate group and 42 cases in lipiodol group.The patients in control group were injected with anti-inflammation agents after recanalizatian,while other groups were injected with chitosan,sodium hyaluronate or lipiodol at dose of 2-3 ml in every therapeutic group.The rate of location of tubal obstruction and tubal recanalization were recorded during operation.Then patients in every group were followed up on tubal patency after 3 months,and pregnancy rate after 12 months.Results Among 1016 fallopian tubes in 508 patients,there were 330 tubes occlusion at isthmus portion and 563 tubes occlusion at interstitial portion of fallopian tube.Thirtyseven fallopian tubes were ablated because of ectopic pregnancy,86 fallopian tubes were unobstructed.(1)The recanalization rate were 95.7% (179/187) in chitosan group,97.9% (191/195) in sodium hyaluronate group,98.7% (75/76) in lipiodol group and 97.7% (425/435) in control group,which did not show statistical difference (P>0.05).(2) The rates of tubal patency after 3 months of 91.7% (99/108) in chitosan group and 88.5% (100/113) in sodium hyaluronate group were significantly higher than 71.4% (30/42) in lipiodol group and 74.3% (182/245) in control group (P <0.05).(3)The rates of intrauterine pregnancy after 12 months were 48.1% (52/108) in chitosan group and 41.6% (47/113) in sodium hyaluronate group,which were significantly higher than 23.8% (10/42) in lipiodol group and 24.1% (59/245) in control group (P < 0.05).Conclusion Chitosan and sodium hyaluronate could be effective to prevent tubal obstruction after interventional recanalization and increase pregnancy rate.
6.Determination of 22 Kinds of Free Amino Acid in Urine of Hypertensive Patient by Pre-column Derivatization HPLC with Fluorescence Detection
Xiaowei ZHU ; Xinxing GAO ; Fang AN ; Xingjie GUO
China Pharmacy 2007;0(30):-
0.990 0) with an average recovery ranged from 86.1% to 109.0%.The injection RSD were within 0.84%~3.1%(n=6).CONCLUSIONS:The method is successfully applied for simultaneous determination of 22 kinds of free amino acids.
7.Analysis of polysaccharide composition of Hedyotis difusa Willd polysaccarides by pre-column derivatization HPLC
Ludan BAO ; Guofang XU ; Zheng MA ; Na GUO ; Xingjie GUO
Chinese Traditional Patent Medicine 1992;0(03):-
AIM:The polysaccharides of Hedyotis difusa Willd of different sources were extracted and its content and composition of the polysaccharide was analyzed. METHODS: The microwave was employed for the aqueous extract of Hedyotis difusa Willd and the content of total sugar was determined by phenol-sulfur test,the monosaccharides composition was determined by HPLC with pre-column derivatization. RESULTS: The polysaccharide obtained from the samples of Guangdong Province had the highest content.The analytic data showed that the composition of monosaccharides in hydrolytic polysaccharides of Hedyotis difusa Willd were mannose,glucose,galactose,arabinose and rhamnose,the average content of polysaccharides was 9.82%. CONCLUSION: The HPLC method with pre-column derivatization is appropriate for the analysis of monosaccharide composition of Hedyotis difusa Willd polysaccharides and the method is simple,quick and accurate.

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