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| 1 | Analysis on Volatile Constituents in Leaves and Fruits of Ficus carica by GC-MS显示文摘Objective To identify and analyze the volatile constituents in the leaves and fruits of Ficus carica. Methods Gas chromatography (GC) and gas chromatography-mass spectrometry (GC-MS) were used. Results The major components detected in volatile oil of the leaves were psoralen (10.12%), β-damascenone (10.17%), benzyl alcohol (4.56%), behenic acid (4.79%), and bergapten (1.99%), etc. The major components detected in volatile oil of the fruits were furfural (10.55%), 5-methyl-2-furaldehyde (10.1%), and benzeneacetaldehyde (6.59%), etc. Conclusion A total of 121 volatile constituents are identified in the leaves and 108 in the fruits of F. carica, among which 103 constituents are identified for the first time in the leaves and 100 in the fruits. Eighteen volatile constituents are identified in both leaves and fruits. | Jun LI Yu-zeng TIAN Bao-ya SUN Dan YANG Ji-ping CHEN Qi-ming MEN | 2012 | Chinese Herbal Medicines2012，4，1： | 4 |
| 2 | Novel application of bergapten and quercetin with anti-bacterial,osteogenesis-potentiating,and anti-inflammation tri-effects显示文摘The bacteria-mediated inflammatory conditions adversely affect the osseointegration process of endosseous implants,which can even lead to implant malfunction or failure.Local drug delivery has been designed to exert anti-inflammatory and antibacterial activities,but whether this strategy has an effect on the compromised osseointegration under inflammation has rarely been studied.The present study focused on the osteoinductive efficacy of two known phytoestrogens[bergapten(BP)and quercetin(QE)]on implant sites under multiple bacteria-infected conditions in situ.Furthermore,the gene expression profiles of rat bone mesenchymal stem cells(rBMSCs)treated with BP and QE in the presence of Porphyromonas gingivalis-derived lipopolysaccharide were identified.The results showed that both drugs,especially QE,had significant potentiating effects on promoting osteogenic differentiation of rBMSCs,resisting multiple pathogens,and reducing inflammatory activity.Meanwhile,RNA sequencing analysis highlighted the enriched gene ontology terms and the differentially expressed genes(Vps25,Il1r2,Csf3,Efemp1,and Ccl20)that might play essential roles in regulating the above tri-effects,which provided the basis for the drug delivery system to be used as a novel therapeutic strategy for integrating peri-implant health.Overall,our study confirmed that QE appeared to outperform BP in osteogenesis and bacterial killing but not in anti-inflammation.Moreover,both drugs possess favorable tri-effects and can serve as the pivotal agents for the drug delivery system to boost osseointegration at inflammatory implant sites. | Jianxu Wei Xiaomeng Zhang Yuan Li Xinxin Ding Yi Zhang Xue Jiang Hongchang Lai Junyu Shi | 2021 | Acta Biochimica et Biophysica Sinica2021，53，6： | 4 |
| 3 | Effects of psoralens as anti-tumoral agents in breast cancer cells显示文摘This review examines the biological properties of coumarins, widely distributed at the highest levels in the fruit, followed by the roots, stems and leaves, by considering their beneficial effects in the prevention of some diseases and as anti-cancer agents. These compounds are well known photosensitizing drugs which have been used as pharmaceuticals for a broad number of therapeutic applications requiring cell division inhibitors. Despite this, even in the absence of ultraviolet rays they are active. The current paper mainly focuses on the effects of psoralens on human breast cancer as they are able to influence many aspects of cell behavior, such as cell growth, survival and apoptosis. In addition, analytical and pharmacological data have demonstrated that psoralens antagonize some metabolizing enzymes, affect estrogen receptor stability and counteract cell invasiveness as well as cancer drug resistance. The scientific findings summarized highlight the pleiotropic functions of phytochemical drugs, given that recently their target signals and how these are modified in thecells have been identified. The encouraging results in this field suggest that multiple modulating strategies based on coumarin drugs in combination with canonical chemotherapeutic agents or radiotherapy could be a useful approach to address the treatment of many types of cancer. | Maria Luisa Panno Francesca Giordano | 2014 | World Journal of Clinical Oncology2014，5，3： | 3 |
| 4 | Mechanism underlying bergapten-mediated regulation of vincristine transport in MDCK-MDR1 cells显示文摘Objectives: To investigate the effects of bergapten of Angelicae Dahuricae Radix on the transport of vincristine and its possible mechanism.Methods: The apparent permeability coefficient(Papp) for the transport of vincristine through the membrane of MDCK-MDR1 cells was used as an indicator of the effect of bergapten on vincristine transport.Molecular docking was employed to predict the binding force between bergapten and P-glycoprotein(Pgp). The effects of bergapten on P-gp function and P-gp ATPase activity were determined by rhodamine123(Rho123) accumulation and activity analysis, respectively. 1,6-Diphenyl-1,3,5-hexatriene(DPH) was used to study the effects of bergapten on membrane fluidity, and Western blotting and quantitative realtime PCR assays were performed to analyze the effect of bergapten on the protein and mRNA expression of P-gp, respectively. These experiments clarified the effects of bergapten on the transport of vincristine and allowed exploration of the possible mechanism underlying the effects of bergapten.Results: The results showed that bergapten could inhibit the transport of vincristine in MDCK-MDR1 cells,and the binding force between bergapten and P-gp was weaker. Bergapten could reduce the accumulation of Rh123 in MDCK-MDR1 cells, increase the membrane fluidity, and upregulate P-gp protein and mRNA expression but it had no effect on P-gp ATPase activity.Conclusions: Overall, we concluded that the possible mechanism through which bergapten inhibits vincristine transport was related to the bergapten-mediated upregulation of P-gp protein and mRNA expression, membrane fluidity or P-gp enzyme activity. | Xin-li Liang Tao Tang Guo-wei Zhao Wei Dong Xue-jing Guan Zheng-gen Liao Ming Yang | 2018 | Chinese Herbal Medicines2018，10，3： | 1 |
| 5 | A New Approach to the Synthesis of Bergapten显示文摘In this study, bergapten was synthesized in a yield of 55% from phloroglucinol as starting material, via a novel approach including monomethylation, Hoesch reaction, acetylation, deacetoxylation, Pechmann condensation and 2,3-dichloro-5,6-dicyano-1,4-benzoquinone(DDQ) dehydrogenation. With the adoption of the acetylation of enol tautomer, the deacetoxylation and the DDQ dehydrogenation, the novel approach differs greatly from the processes reported previously, though the starting material was the same or similar to those used on previous synthetic processes. The newly adopted reaction underwent easily, affording all reactions in high yields, especially acetylation and deacetoxylation and DDQ dehydrogenation in almost quantitative yields, ensuring a final yield higher than those previously reported. | CAI Xiaoqing JI Dongxin LIU Jiageng HU Maolin JIN Zhimin | 2022 | Chemical Research in Chinese Universities2022，38，6： | 0 |
| 6 | Bergapten inhibits NLRP3 inflammasome activation and pyroptosis via promoting mitophagy显示文摘Inhibition of NLRP3 inflammasome activation produces potent therapeutic effects in a wide array of inflammatory diseases.Bergapten(BeG),a furocoumarin phytohormone present in many herbal medicines and fruits,exibits anti-inflammatory activity.In this study we characterized the therapeutic potential of BeG against bacterial infection and inflammation-related disorders,and elucidated the underlying mechanisms.We showed that pre-treatment with BeG(20μM)effectively inhibited NLRP3 inflammasome activation in both lipopolysaccharides(LPS)-primed J774A.1 cells and bone marrow-derived macrophages(BMDMs),evidenced by attenuated cleaved caspase-1 and mature IL-1βrelease,as well as reduced ASC speck formation and subsequent gasdermin D(GSDMD)-mediated pyroptosis.Transcriptome analysis revealed that BeG regulated the expression of genes involved in mitochondrial and reactive oxygen species(ROS)metabolism in BMDMs.Moreover,BeG treatment reversed the diminished mitochondrial activity and ROS production after NLRP3 activation,and elevated the expression of LC3-II and enhanced the co-localization of LC3 with mitochondria.Treatment with 3-methyladenine(3-MA,5 mM)reversed the inhibitory effects of BeG on IL-1β,cleaved caspase-1 and LDH release,GSDMD-N formation as well as ROS production.In mouse model of Escherichia coli-induced sepsis and mouse model of Citrobacter rodentium-induced intestinal inflammation,pre-treatment with BeG(50 mg/kg)significantly ameliorated tissue inflammation and injury.In conclusion,BeG inhibits NLRP3 inflammasome activation and pyroptosis by promoting mitophagy and maintaining mitochondrial homeostasis.These results suggest BeG as a promising drug candidate for the treatment of bacterial infection and inflammation-related disorders. | Tong Luo Xin Jia Wan-di Feng Jin-yong Wang Fang Xie Ling-dong Kong Xue-jiao Wang Rui Lian Xia Liu Ying-jie Chu Yao Wang An-long Xu | 2023 | Acta Pharmacologica Sinica2023，44，9： | 0 |
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