Action Mechanism of Components from Gardenia jasminoides on Eye Skin Based on Network Pharmacology

[Objectives]To explore the pharmacological effects of Gardenia jasminoides and its potential benefits on eye skin.[Methods]TCMSP and SymMap databases were used to screen the active components and corresponding targets of G.jasminoides.Human eye skin-related targets were screened,and the active component-target network and protein-protein interaction(PPI)network were established.Gene ontology(GO)analysis and Kyoto Encyclopedia of Genes and Genomes(KEGG)pathway analysis were performed.[Results]Twenty-six active compounds were screened out from G.jasminoides,and 277 targets were obtained.From the Gencards database,26652 disease targets were retrieved and 205 related gene targets were screened.The active component-action target network of G.jasminoides constructed by Cytoscape software revealed the potential of G.jasminoides to play a role in multiple biological pathways.In addition,PPI-network analysis,GO function analysis and KEGG pathway enrichment analysis revealed that the active components of G.jasminoides mainly regulate the biological processes such as inflammatory response,oxidative stress and apoptosis,involving MAPK,NF-κB and other important signaling pathways.[Conclusions]This study provides a theoretical basis for the eye skin protection of G.jasminoides and an important clue for future drug development.

A new iridoid glycoside from Gardenia jasminoides

A new iridoid glycoside, 6＇-O-sinapoylgeniposide, was isolated from Gardeniajasminoides Ellis and its structure was elucidated on the basis of 1D and 2D NMR, HR-ESI-MS techniques.

Gardenia jasminoides attenuates hepatocellular injury and fibrosis in bile duct-ligated rats and human hepatic stellate cells

AIM:To investigate the anti-hepatofibrotic effects of Gardenia jasminoides in liver fibrosis.METHODS:Male Sprague-Dawley rats underwent common bile duct ligation(BDL) for 14 d and were treated with Gardenia jasminoides by gavage.The ef-fects of Gardenia jasminoides on liver fibrosis and the detailed molecular mechanisms were also assessed in human hepatic stellate cells(LX-2) in vitro.RESULTS:Treatment with Gardenia jasminoides decreased serum alanine aminotransferase(BDL vs BDL + 100 mg/kg Gardenia jasminoides,146.6 ± 15 U/L vs 77 ± 6.5 U/L,P = 0.0007) and aspartate aminotransferase(BDL vs BDL + 100 mg/kg Gardenia jasminoides,188 ± 35.2 U/L vs 128 ± 19 U/L,P = 0.005) as well as hydroxyproline(BDL vs BDL + 100 mg/kg Gardenia jasminoides,438 ± 40.2 μg/g vs 228 ± 10.3 μg/g liver tissue,P = 0.004) after BDL.Furthermore,Gardenia jasminoides significantly reduced liver mRNA and/or protein expression of transforming growth factor β1(TGF-β1),collagen type?Ⅰ?(Col?Ⅰ) and α-smooth muscle actin(α-SMA).Gardenia jasminoides significantly suppressed the upregulation of TGF-β1,Col?Ⅰand α-SMA in LX-2 exposed to recombinant TGF-β1.Moreover,Gardenia jasminoides inhibited TGF-β1-induced Smad2 phosphorylation in LX-2 cells.CONCLUSION:Gardenia jasminoides exerts antifibrotic effects in the liver fibrosis and may represent a novel antifibrotic agent.

Gardenia jasminoides protects against cerulein-induced acute pancreatitis

AIM： To investigate the effect of Garden/a fasm/noides （GJ） on cerulein-induced acute pancreatitis （AP） in mice. METHODS： C57BL/6 mice weighing 18-20 g were divided into three groups. （1） Normal salinetreated group, （2） treatment with GJ at a dose of 0.1 g/kg, （3） treatment with GJ at a dose of 1 g/kg. GJ was administered orally （n = 6 per group） for 1 wk. Three hours later, the mice were given anintraperitoneal injection of cerulein （50 μg/kg）, a stable cholecystokinin （CCK） analogue, every hour for a total of 6h as described previously. The mice were sacrificed at 6 h after completion of cerulein injections. Blood samples were obtained to determine serum amylase, lipase and cytokine levels. The pancreas was rapidly removed for morphologic examination and scoring. A portion of pancreas was stored at -70℃ and prepared for the measurement of tissue myeloperoxidase （MPO） activity, an indicator of neutrophil sequestration, and for reverse-transcriptase PCR （RT-PCR） and real-time PCR measurements. RESULTS： Treatment with G.1 decreased significantly the severity of pancreatitis and pancreatitis-associated lung injury. Treatment with G.1 attenuated the severity of AP compared with saline-treated mice, as shown by reduction in pancreatic edema, neutrophil infiltration, serum amylase and lipase levels, serum cytokine levels, and mRNA expression of multiple inflammatory mediators. CONCLUSION： These results suggest that GJ attenuated the severity of AP as well as pancreatitisassociated lung injury.

Responses of Gardenia jasminoides Ellis Leaf Traits and Anatomical Structures to Drought Stress in Purple Soil

[Objectives]This study was conducted to investigate the response of Gardenia to purple soil drought stress,hoping to provide a reference for the selection of plants for vegetation restoration in purple soil regions.[Methods]The pot-weighing water control method was used to apply different degrees of drought stress to Gardenia seedlings in purple soil,and the effects of drought stress on the electrical conductivity,chlorophyll content,leaf morphology and structure of Gardenia leaves were explored.[Results]The leaf electrical conductivity increased with the increase of drought stress intensity,and the leaf electrical conductivity under severe drought stress increased by 59.93%compared with the control;the chlorophyll content of Gardenia showed a single-peak changing trend that increased and then decreased with the development of drought stress,and it was the highest in each stress stage under severe drought stress;the leaf thickness,palisade tissue thickness and sponge tissue thickness of Gardenia were reduced with the stress degree increasing,and showed the largest decreases under severe stress;the stomatal length,stomatal width and stomatal opening of Gardenia gradually decreased with the increase of stress,while the stomatal density gradually increased.[Conclusions]This study provides a technical and resource basis for vegetation restoration in purple soil.

Technique of Three-dimensional Cuttage of Gardenia jasminoides Ellis

[Objectives]This study was conducted to improve the propagation efficiency of Gardenia jasminoides Ellis and improve the quality of plantlets.[Methods]A G.jasminoides cutting experiment was carried out with three different cuttage modes and two cutting treatment methods,and the rooting time,rooting rate,root amount and plantlet growth were measured and analyzed.[Results]The three-dimensional cutting model of CL1 could not only shorten the nursery cycle and promote root development,but also effectively improve the quality of plantlets and increase the yield of plantlets per unit area.It is an ideal way to improve the quality and efficiency of cutting plantlets.[Conclusions]This study has a positive role in promoting the healthy development of the nursery stock industry.

Practical Cultivation Techniques of Gardenia jasminoides Ellis for Flowers-Fruits in Hunan Province

In order to protect and develop the local resources of Gardenia jasminoides Ellis with Hunan characteristics,this paper uses the existing technology,analyzes the existing achievements in the cultivation of G.jasminoides Ellis,investigates and analyzes the actual situation of the seedling base and cooperatives in Hunan,and collects the relevant index data related to the cultivation of G.jasminoides Ellis.This paper summarizes the practical techniques related to land selection,soil preparation,seedling breeding,afforestation technology,tending management,pest control and so on,in order to provide reference basis for planting and cultivateon and industrial development of G.jasminoides Ellis in Hunan.

Research and application progress of Gardenia jasminoides

Fruits of Gardenia jasminoides（Zhizi in Chinese） have been used as dietary supplement and traditional Chinese medicine for thousands of years. Recent studies on Gardenia jasminoides reveal that the extracts or the active components play an essential role in oxidative stress, inflammation, hepatoprotection,neuroprotection, anti-diabetes, antitumor and so on. Here, we reviewed G. jasminoides in the aspects of botanical identity, chemical ingredients, pharmacology and pharmacokinetics, safety and toxicity evaluation, clinical application, etc.

栀子(Gardenia jasminoides)GGPPS基因小亚基的克隆及表达分析

香叶基焦磷酸(geranyl pyrophosphate,GPP)是单萜的前体物质,而单萜是栀子内重要的活性成分。香叶基香叶基焦磷酸合酶(GGPPS)在萜类化合物、类胡萝卜素类化合物生物合成中处于关键位置,GGPPS主要分为香叶基香叶基焦磷酸合成酶大亚基(GGPPSlsu)和香叶基香叶基焦磷酸合成酶小亚基(GGPPSssu)。为了研究栀子GGPPS基因在栀子萜类生物合成中的作用,本研究成功从栀子品种‘林海一号’中提取RNA反转录合成cDNA,根据转录组测序拼接结果设计引物扩增得到栀子GGPPSssu的cDNA序列,分别命名为GjGGPPSssu1和GjGGPPSssu2,ORF区分别为1053 bp和915 bp。通过构建基因进化树,栀子GGPPSssu基因和其他植物的GGPPSssu基因聚为一类,属于香叶基香叶基焦磷酸合成酶小亚基基因。通过蛋白质序列比对表明GjGGPPSssu1有一个CxxxC(x为碱性氨基酸)的保守基元和一个FARM的保守基元,没有SARM保守基元,与SSUⅡ类基因相似;GjGGPPSssu2有两个CxxxC的保守基元,没有FARM保守基元和SARM保守基元,与SSUⅠ类基因相似。荧光定量PCR试验结果表明,GjGGPPSssu1在T4和T5时期有较高的表达水平,GjGGPPSssu2在栀子各生长时期的根部和果实中有较高水平的表达。推测GjGGPPSssu1基因与栀子黄色素合成相关,GjGGPPSssu2基因与单萜合成相关。本研究初步解析了栀子GGPPS基因的功能,为提高栀子药用品质提供了理论依据。

Potential mechanism of cholagogic effect about Gardenia Jasminoides Ellis(Zhizi)-mediated increase of bile acids urinary excretion in normal rats

Objectives： Gardenia Jasminoides Ellis（Zhizi）, belonging to Rubiaceae family, has been traditionally used for treatment cholestasis and jaundice for centuries in Asian countries. In the theory of Traditional Chinese Medicines, Zhizi could dispel dampness and heat via the urine to execute its choleretic effects. However, the potential molecular mechanism has been still poorly clarified. Here, we investigated the effect of different dose of Zhizi aqueous extract powder（0.3 g/kg/d and 0.9 g/kg/d） on urinary excretion of bile acids（BAs）, and defined the potential mechanism via renal BAs efflux transporters Mrp2 and Mrp4 in normal rats.Methods： Male Wistar rats were orally administrated with 0.3 or 0.9 g/kg/d dose of Zhizi aqueous extract powder for 2 weeks, then body weight, serum aminotransferase, total BAs concentrations in liver, bile,serum, kidney and urine, 1 h bile flow, 12-h urinary volume, biliary and urinary excretion amount of total BAs as well as protein expression of major renal BAs efflux transporter Mrp2 and Mrp4, were all evaluated.Results： Zhizi especially the high dose of Zhizi aqueous extract powder could reduce hepatic total BAs concentration. Additionally, bile flow and biliary excretion had no significant difference, but the remarkable increasing urinary excretion of BAs and 2 to 3 folds up-regulated renal Mrp2 expression were observed after administrated with Zhizi as compared with the control group.Conclusion： The findings indicate that Zhizi reduces hepatic total BAs level by increasing urinary excretion rather than the biliary excretion of BAs, which, in turn ascribed to elevated protein expression of Mrp2 at apical membrane of renal tubular epithelial cells.

Anti-TMV and Insecticidal Potential of Four Iridoid Glycosides from Gardenia Jasminoides Fruit

In agriculture, pests are largely controlled by agricultural chemicals. The vast majority of these pesticides are synthetic compounds, some of which are based on natural products, and a few of which are synthetic versions of natural products. Pests have evolved resistance to many of the current pesticides, often by alterations in the molecular target site. Thus, pesticides with new molecular target sites and modes of action are needed.

栀子炮制的本草考证

栀子(Gardenia jasminoides Ellis)为药食两用果实类传统中药,生用有护肝利胆的功效,性味苦寒,易伤脾胃,经炮制后可改善,并具凉血、止血的功效。对历代古籍本草和古今文献资料进行研究,发现栀子大多采用去皮取仁并切制、炒制(炒、微炒、炒黄、炒焦和炒黑)和加辅料制(酒制、甘草水制、姜制、盐制、蜜制和童便制)等加工炮制方法。按照历史脉络,通过查阅大量本草文献梳理了栀子炮制与功效的历史沿革,为统一栀子的炮制工艺和栀子不同炮制品的质量评价提供本草学依据。

Effect of Hoechunyangkyeok-San Extract on Melanogenesis

Forsythia fructus has been shown to have antioxidative, anti-inflammatory, antibacterial, anti-aging and whitening effects. Hoechunyangkyeok-san (Forsythia viridissima-prescription) is a traditional herbal medicine, which has been clinically used for treating febrile and inflammatory disorders. This work was carried out to investigate the skin whitening effects of Forsythia viridissima-prescription extract (a hydrolyzed extract of Hoechunyangkyeok-san: SID White HYC) on skin. The effects of SID White HYC were assessed the melanin contents in B161 melanoma cells and the pigmented equivalent with HMB45 and Fontana Masson staining in 3D skin model. Then, we examined the expression of major pigment enzymes regulating melanin synthesis and melanosome transport related proteins in B16F1 cells. SID White HYC significantly inhibited the melanin synthesis (56.7% and 30.6% inhibition at 100 μg/mL, intracellular and secreted, respectively) in B16F1 cells and 3D skin model. In addition, western blotting analysis showed that SID White HYC reduced the expression of melanin synthesis and melanosome transport related proteins in B16F1 cells. In clinical trials, the cream containing 0.05% SID White HYC showed skin depigmentation effect without any irritation. These results suggest that SID White HYC may be useful inhibition of melanogenesis and melanosome transport. Therefore, SID White HYC may have potential as a skin-whitening ingredient in cosmetics.

Iridoid glycosides extracted from Zhizi(Fructus Gardeniae)decrease collagen-induced platelet aggregation and reduce carotid artery thrombosis in an invivo rat model

OBJECTIVE: To investigate the anti-platelet aggregation and antithrombotic effects in rats of iridoid glycosides extracted from Zhizi (FructusGardeniae). METHODS: The present study evaluated the antithrombotic activity of iridoid glycosides (IGs) in a rat model of carotid artery thrombosis. The effects on coagulation, such as thromboplastin time (APTT), thrombin time (TT) and prothrombin time (PT), and the effect on collagen-induced platelet aggregation in vivo were investigated. Rats were intragastrically administered IGs (50, 100 or 200 mg/ kg) twice daily for 3 days. RESULTS: IGs were shown for the first time to have an antithrombotic action through the inhibition of platelet aggregation, with little effect on the coagulation time of peripheral blood. Our results also showed that IGs may significantly and dose-dependently reduce arterial thrombus load in a model of carotid artery thrombosis and inhibit collagen-induced platelet aggregation in rats. IGs (100or 200 mg/kg) had no significant effect on APTT and PT, but did lengthenTT at a higher dose. CONCLUSION: These data, together with the previously reported neuroprotective effects of IGs in rats with cerebral ischemia, suggest that the antithrombotic action of IGs may potentially contribute to the treatment of cerebral ischemic diseases, including cerebral apoplexy.

栀子活性物质石油醚层组分快速抗抑郁作用及机制

本研究旨在研究栀子的石油醚层组分的快速抗抑郁作用及其机制。通过行为测试和蛋白质印迹分析,我们发现栀子石油醚层组分具有显著的抗抑郁效果,并且可以增加海马中BDNF和TrkB的表达。悬尾试验和强迫游泳试验结果显示,栀子石油醚层组分可显著减少不动时间,表明其具有抗抑郁活性。蔗糖偏爱试验结果显示,栀子石油醚层组分可增加小鼠对蔗糖的偏好。研究结果表明,栀子石油醚层组分的抗抑郁作用可能与BDNF-TrkB信号转导途径的调节有关。这些发现为进一步研究栀子石油醚层组分的抗抑郁机制和开发相关药物提供了重要线索。

Hepatic CYP3A4,SULT2A1,and UGT1A1 synergistically mediate metabolic detoxification of genipin

In the present study,we aimed to ascertain the metabolic detoxification routes of genipin via CYP3A4,SULT2 A1,and UGT1 A1 in Hepa RG cells.It was found that the hepatic CYP3A4,SULT2 A1,and UGT1 A1 synergistically mediated the metabolic detoxification of genipin,and the CYP3A4 was the limited enzyme.In detail,the pivotal detoxification pathway was CYP3A4-SULT2 A1/UGT1 A1,indicating that SULT2 A1 and UGT1 A1 further catalyzed the phase II detoxification metabolism followed by the genipin metabolization by CYP3A4 to the phase I metabolites with alleviated toxicity.Our findings provided valuable cues for future studies on the detoxification of genipin,even the compatibility detoxification of Zhi-zi.Moreover,these data facilitated the development and rational administration of genipin and Zhi-zi.