查找使用阿拉丁产品的科研文献

Encapsulation of zingerone by self-assembling peptides derived from fish viscera: Characterization, interaction and effects on colon epithelial cells

Sirong Huang,Xintong Yao,Boya Cao,Na Zhang,Olugbenga P. Soladoye,Yuhao Zhang,Yu Fu

The purpose of the present work was to encapsulate zingerone (a bioactive compound from ginger) by self-assembling peptides derived from fish viscera. The encapsulation conditions were investigated and the structure of fish peptides-zingerone complex was characterized. The interaction between zingerone and fish peptides was investigated using fluorescence spectroscopy. Further research was performed on the in vitro release of zingerone and fish peptide-zingerone as well as their antiproliferative effects on colon epithelial Caco-2 cells. The results demonstrated that zingerone can be successfully encapsulated by self-assembling peptides derived from fish viscera with high encapsulation efficiency and loading capacity. Furthermore, transmission electron microscope and confocal laser scanning microscope observations revealed the successful encapsulation of zingerone by fish viscera peptides. In addition, in vitro release and antiproliferative activity against Caco-2 cells can be significantly increased by encapsulating zingerone via peptide self-assembly. The current study advances knowledge of encapsulation of bioactive compounds through peptide self-assembly.

Enhanced oral bioavailability and anti-gout activity of [6]-shogaol-loaded solid lipid nanoparticles

Qilong Wang,Qiuxuan Yang,Xia Cao,Qiuyu Wei,Caleb K. Firempong,Min Guo,Feng Shi,Ximing Xu,Wenwen Deng,Jiangnan Yu

[6]-Shogaol, an alkylphenol compound purified from the root and stem of ginger ( Zingiber officinale ), has attracted considerable interest due to its potential anticancer, antioxidative and antirheumatic properties. However, the oral bioavailability of [6]-shogaol has been severely limited because of its poor solubility. In this study, a significant quantity of high-purity [6]-shogaol (yield: 3.6%; purity: 98.65%) was extracted and encapsulated in solid lipid nanoparticles (SLNs) via high-pressure homogenization (encapsulation efficiency: 87.67%) to improve its solubility and oral bioavailability. The resulting [6]-shogaol-loaded solid lipid nanoparticles (SSLNs) were stable, homogeneous and well-dispersed. Its mean particle size and zeta potential were 73.56 ± 5.62 nm and −15.2 ± 1.3 mV, respectively. Importantly, the in vitro release profile and in vivo oral bioavailability of SSLNs were significantly improved compared with the free drug. Furthermore, the SSLNs could remarkably lower the uric acid level via inhibiting the activity of xanthine oxidase and reduce the production of interleukin-1β (IL-1β) and tumor necrosis factor (TNF-α) in the hyperuricemia/gouty arthritis rat model, when compared to the free [6]-shogaol. Collectively, SLNs could serve as a promising drug delivery system to improve the oral bioavailability of [6]-shogaol for effective treatment of gouty arthritis.

Zingerone promotes the survival of ischaemic flap via the KEAP1-Nrf2 pathway

Chengji Dong,Gaoxiang Yu,Xianhui Ma,Zhuliu Chen,Ningning Yang,Xuankuai Chen,Yingying Lai,Jiayi Zhao,Yanlan Gu,Kailiang Zhou,Weiyang Gao,Jian Ding,Xuwei Zhu

Background How to improve flap necrosis in distal flaps is still a popular topic in clinical flap research. Zingerone (ZIN), as a plant extract, has therapeutic effects on many diseases. The purpose of our study was to explore whether ZIN can promote the survival of ischaemic skin flaps and its specific mechanism. Methods An ischemic flap model was established in the dorsal region of mice. The changes of angiogenesis, oxidative stress, apoptosis and Keap1-Nrf2 related proteins in the skin flap were detected by immunofluorescence, western blot and qPCR. Overexpression of Keap1 by adeno-associated virus (AAV) was used to study the specific pathway and mechanism. Results The results showed that ZIN can induce angiogenesis and reduce oxidative stress and apoptosis to promote flap survival. Increased expression of Keap1 reversed the therapeutic effect of ZIN. Conclusion ZIN activates Nrf2 by inhibiting Keap1 activation, thus promoting angiogenesis and inhibiting oxidative stress and apoptosis.

DSF-inspired discovery of novel zingerone-based quorum-sensing inhibitors: an attractive tactic of fighting Xanthomonas bacterial infections

Hong Liang,Yu-Mei Feng,Dan Zeng,Jun-Rong Zhang,Long Cheng,Xi-Chun Fu,Zhou-Qing Long,Xiang Zhou,Li-Wei Liu,Zhi-Bing Wu,Song Yang

BACKGROUND Plant bacterial diseases have precipitated a global crisis in human health and food security. In agriculture, diseases such as the rice white-leaf blight can cause considerable reduction in crop yields and, in extreme cases, complete crop failure. Therefore, there is an urgent need for novel green pesticides with innovative modes-of-action (MoAs). RESULTS A series of zingerone derivatives with an isopropanolamine skeleton were designed and their quorum-sensing effects were estimated using biomimetic strategies. The results showed that the novel compound A 12 effectively inhibits the growth of Xanthomonas oryzae pv. oryzae [ Xoo , median effective concentration (EC 50 ) = 3.55 μg mL −1 ], Xanthomonas axonopodis pv. citri ( Xac , EC 50 = 3.23 μg mL −1 ) and Xanthomonas oryzae pv. oryzicola ( Xoc , EC 50 = 7.48 μg mL −1 ). Molecular docking results revealed that A 12 forms multiple interactions with the RpfF protein, while fluorescence titration experiments further verified the interaction between them. Additionally, A 12 was found to effectively inhibit Xoo biofilm formation, extracellular polysaccharide production and other virulence factors. In vivo pot experiments revealed that compound A 12 exhibited excellent curative (53.59%) and protective (57.65%) activity against Xoo . In conclusion, compound A 12 's primary MoA is achieved by affecting the formation of biofilms and the expression of various virulence factors, including related virulence genes. CONCLUSION In summary, this study highlights that compound A 12 displays notable quorum-sensing sensing activity. The advancement of novel quorum-sensing inhibitors through biomimetic strategies offers promising avenues for future research. © 2025 Society of Chemical Industry.

Active ingredients screening and pharmacological mechanism research of curcumae rhizoma-sparganii rhizoma herb pair ameliorates liver fibrosis based on network pharmacology

Min Hao,Zhouhui Yao,Mengting Zhao,Ziyan Chen,Pingping Wang,Xianan Sang,Qiao Yang,Kuilong Wang,Xin Han,Gang Cao

Ethnopharmacological relevance Curcumae Rhizoma-Sparganii Rhizoma (CR-SR) is a classic herbal pair to promote blood circulation and remove blood stasis in ancient China. However, the molecular mechanism is still unclear. Aim of study To screen out the anti-liver fibrosis active ingredients in CR-SR. Moreover, preliminary exploration the molecular mechanism of CR-SR to ameliorates liver fibrosis . Materials and methods In this research, plant taxonomy has been confirmed in the “The Plant List” database ( www.theplantlist.org ). The chemical components of CR-SR were analysed by ultra-performance liquid chromatography-quadrupole/time-of-flight mass spectrometry (UPLC-Q/TOF-MS). “Component-Target-Pathway-Disease” network of CR-SR components were built by network pharmacology . Then, the interaction between primary components and predicted protein targets based on network pharmacology were validated by molecular docking. The pharmacological actions of CR-SR were verified by blood biochemical indexes, histopathologic examination of CCL 4 induced rats’ model. The core protein targets were verified by Western blot . The effects of screened active components by molecular autodocking were verified by HSC-T6 cell experiment. Results The result shows that 57 chemical constituents in CR-SR herbal pair were identified by UPLC-Q/TOF-MS, in which, 27 compounds were closely connected with liver fibrosis related protein targets. 55 protein targets screened out by “component-target-pathway-disease network” maybe the underlying targets for CR-SR to cure liver fibrosis. Moreover, the 55 protein targets are mainly related to RNA transcription, apoptosis , and signal transduction. The molecular autodocking predicted that ten components can bond well with PTGS2 and RELA protein targets. The blood biochemical indexes, histopathologic examination of CCL 4 induced rats experiment showed that CR-SR has well intervention effect of liver fibrosis. The Western blot analysis indicated that CR-SR could significantly inhibit RELA, PTGS2, IL-6, SRC, and AKT1 protein expression to exert the anti-fibrosis effect. The HSC-T6 cell experiment indicated that both formononetin (FNT) and curdione could significantly inhibit the activation of HSC and reduce the expression of PTGS2, and p-AKT1 which was accordance with the molecular autodocking results. Conclusion This study proved the molecular mechanism of CR-SR multi-component and multi-target anti-liver fibrosis effect through mass spectrometry, network pharmacology, and western blotting technology. The research provides a theoretical evidence for the development and utilization of CR-SR herbal pair.

Molecular mechanism of the substrate promiscuity in GT1 glucosyltransferases: Insights from molecular dynamics simulations and experimental validation

Letian Yang,Zhenyu Ma,Xueting Cao,Limei Xu,Xue Ma,Jingyi Zhu,Min Xiao,Xukai Jiang

Glycosyltransferases (GTs) catalyze the transfer of sugar moieties from activated donors to acceptor molecules, which are widely-used biocatalysts in the industrial biosynthesis of natural products. Members of the GT1 family exhibit remarkable substrate promiscuity, enabling glycosylation of diverse natural products; however, the underlying molecular mechanisms remain poorly understood. Here we integrated all-atom molecular dynamics simulations, bioinformatics and experimental mutations to elucidate the structural and dynamics mechanisms governing the substrate promiscuity of GT1 enzymes. Using the Bs YjiC from Bacillus subtilis as a representative, we interestingly found that its acceptor-binding pocket harbored two flexible binding subsites with distinct geometric features, which enabled structurally diverse substrates to be specifically recognized in different subsites. The site-directed mutagenesis at the subsites and in vitro glycosylation assays further demonstrated the critical role of subsite-mediated substrate recognition. Importantly, the existence of two subsites in the acceptor-binding pocket was found to be a general feature across nine different members of GT1 family. Overall, the characteristic features of the acceptor-binding pocket represent a conserved trait across the GT1 family and provide potential guidance for engineering GTs with tailored substrate specificities.

Zingerone enhances the antitumor activity of attenuated Salmonella-mediated cancer immunotherapy by promoting tumor infiltration by host immune cells

Huimin Xu,Linghua Piao,Xuanri Shen,Xiande Liu

Bacteria-mediated cancer immunotherapy (BCI) suppresses tumor progression in two ways: the bacteria themselves kill tumor cells, and they elicit robust host immune responses. However, this does not eradicate tumors completely or prevent metastasis. Therefore, the immune responses elicited by BCI must be backed up by other therapies such as chemotherapy. Zingerone has anticancer activity and modulates T cell-mediated immune responses. Here, we examined the antitumor effects of zingerone/BCI combination therapy. We show that that zingerone 1) enhances St.ΔppGpp-mediated antitumor effects, but reduces survival of tumor-colonizing bacteria by promoting recruitment of tumor-infiltrating neutrophils; 2) amplifies St.ΔppGpp-mediated immune responses by stimulating tumor infiltration by macrophages, natural killer cells, and CD4 + and CD8 + T cells; and 3) enhances St.ΔppGpp-mediated macrophage phagocytosis, leading to tumor eradication. These findings suggest that the zingerone/St.ΔppGpp combination has synergistic antitumor effects, making it a promising approach to cancer immunotherapy.

Preparation of the high purity gingerols from ginger by dummy molecularly imprinted polymers

Wenhua Ji,Xiuli Ma,Jinghua Zhang,Hongkai Xie,Feng Liu,Xiao Wang

In this work, a dummy molecularly imprinted polymers (MIPs) were developed as the selective sorbents for preparation of the high purity gingerols from ginger for the first time. The dummy template molecule with similar structural skeleton to gingerols, N-vanillylnonanamide, has been designed and synthesized. The performance of the MIPs and non-imprinted polymers (NIPs) were evaluated including selective recognition capacity, adsorption isotherm, and adsorption kinetics. Optimization of various parameters affecting dummy molecular imprinted solid phase extraction (MISPE), such as the type and flow rate of the loading solvent, the composition and volume of the eluting solvent, and the composition and volume of the washing solvent were investigated. Gingerols with the percent recovery of 80 and the percent purity of 99.1 were obtained from the extracts of ginger by MISPE. Besides, gingerols obtained by MISPE had more powerful activity of eliminating free radical compared with extracts before extraction with the MISPE column. Application of MIPs with a high affinity toward three gingerols provides a novel method for obtaining a group of compounds which have likely active groups from natural products.

Novel dual CAFs and tumour cell targeting pH and ROS dual sensitive micelles for targeting delivery of paclitaxel to liver cancer

Chunjing Guo,Wei Zhang,Qiaoyun Zhang,Yanguo Su,Xiaoya Hou,Qiang Chen,Huimin Guo,Ming Kong,Daquan Chen