Gardeniae Fructus Research Articles

Quality evaluation of commercial Huang-Lian-Jie-Du-Tang based on simultaneous determination of fourteen major chemical constituents using high performance liquid chromatography

Huang-Lian-Jie-Du-Tang (HLJDT), comprising Coptidis Rhizoma, Scutellariae Radix, Phellodendri Cortex and Gardeniae Fructus, is one of the commonly used Chinese medicine formulas for clearing heat and detoxifying. Quality control of the herbal complex like Chinese medicine formulas still remains a challenge. The successful approval of botanical drug Veregen by FDA indicated the importance of quantitative analysis in quality control of herbal medicines. In this study, an effective quantitative method based on conventional HPLC–DAD was developed for simultaneous determination of fourteen major ingredients (seven alkaloids, four flavonoids, three terpenes) in HLJDT. The established method was well validated in terms of linearity, sensitivity, precision, accuracy and stability and then successfully applied to quality evaluation of commercial HLJDT samples. The developed method can quantitatively determine up to 70% of the chemicals of commercial HLJDT sample and effectively revealed the significant variation in the quality of the commercial HLJDT samples collected from different locations.

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

ObjectiveTo investigate the anti-platelet aggregation and antithrombotic effects in rats of iridoid glycosides extracted from Zhizi (Fructus Gardeniae). MethodsThe 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. ResultsIGs 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 (100 or 200 mg/kg) had no significant effect on APTT and PT, but did lengthen TT at a higher dose. ConclusionThese 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.

치자(梔子)의 부위별 Geniposide정량 및 항산화효능비교

Objectives : The objective of the paper was to study cutting method of Gardeniae frutus, that tends to show symptom of separations in a packing, in accordance with the comparison experiment of quantification and antioxidant effect proceed with the intact Gardeniae fructus(Gf), seed of Gardeniae fructus (Gs) and the pericarp of Gardeniae fructus (Gp) separately. Methods : The Gf, Gs, and Gp were extracted using 80% MeOH, followed by quantizing geniposide contained in each group. A MTT assay was conducted and ROS generation and NO production were measured for comparing its antioxidant effect. Results : As a result of quantizing geniposide contained in the Gf, Gp, and Gs, respectively, the geniposide content was shown to be the highest in the Gs. MTT assay showed that no cytotoxicity was observed in the groups treated with Gf, Gp, and Gs, respectively, at a dose of 500 <TEX>${\mu}g/ml$</TEX>. The ROS generation was shown to have more significantly decreased in the group pretreated with Gf 500 <TEX>${\mu}g/ml$</TEX> than in the group treated with LPS. The NO level was shown to have more significantly decreased in the group pretreated with Gp 500 <TEX>${\mu}g/ml$</TEX> than in the group treated with LPS. Conclusion : As the geniposide content and antioxidant effect of Gf varies according to its each part, it is recommended that Gf should be distributed as an intact form other than segregation in packing.

Comparative study on hepatic toxicity of Gardeniae Fructus and Huanglian Jiedu decoction

To observe the effect of ingredients in Huanglian Jiedu decoction (HLJDT) combined with Gardeniae Fructus on the hepatic toxicity of Gardeniae Fructus and its mechanism. Rats were given Gardeniae Fructus and HLJDT decoction at the dose of 10 times of clinical dosage for 3 days. Their ALT AST, ALP, TBA were detected, and their liver weight index was calculated. SOD activity, MDA content, GSH-PX activity, TNF-alpha content in hepatic tissues were determined. The cell apoptosis in liver tissue was determined by TUNEL, and the expressions of apoptosis related proteins Bax, Bcl-2 were measured by immunohistochemical method. Compared with the normal control group, the Gardeniae Fructus group showed significant increase in the liver weight index, ALT, AST, TBA and ALP, notable decrease in SOD, SOD/MDA and GSH-PX, and remarkable rise in MDA, TNF-a concentration, accumulated optical density, apoptosis index, Bax and Bax/Bcl-2. Compare with that in the Gardeniae Fructus group, the liver index, ALT, AST, TBA, ALP reduced obviously; SOD, SOD/MDA and GSH-PX markedly increased; MDA and TNF-alpha significantly reduced; the accumulated optical density and apoptosis index significantly reduced; and Bax/Bcl-2 was much lower in HLJDT group. The hepatic toxicity caused by Gardeniae Fructus may be related to inflammation, oxidative stress-induced hepatocyte necrosis and apoptosis. Other ingredients in HLJDT, apart from Gardeniae Fructus, can decrease the hepatic toxicity caused by Gardeniae Fructus by increasing the enzyme activity eliminating radicals and inhibiting hepatocyte injury caused by inflammatory reaction against Gardeniae Fructus.

황련해독탕(黃連解毒湯)의 아토피 피부염 개선 효과(效果)

Objectives : The water extract of Hwangnyeonhaedok-tang (HHT), composed of the Scutellariae Radix, Coptidis Rhizoma, Phellodendri Cortex and Gardeniae Fructus has been traditionally used to treat fever, inflammation, gastritis and hypertension in east asia. However, little is known about the ameliorative effects of HHT on atopic dermatitis. Therefore, the purpose of this study was to investigate the therapeutic effect of HHT on atopic dermatitis Methods : We investigated the inhibitory effects of HHT on the production of proinflammatory cytokines in rat peritoneal mast cells (RPMCs), on the scratching behavior in ICR mice, and on atopic dermatitis symptoms in 2,4-dinitrofluorobenzene (DNFB)-induced atopic dermatitis-like model hairless mice. Results : Levels of TNF- and IL- increased by PMA plus A23187 co-treatment were significantly inhibited by HHT in a dose-dependent manner. HHT also inhibited the histamine release from RPMCs stimulated by compound 48/80, which promotes histamine release. The oral administration of HHT reduced the scratching behavior induced by compound 48/80 and histamine in ICR mice. Furthermore, the intradermal treatment of HHT reduced the ear edema, skin lesions, and atopic molecular marker (IgE and IL-4) in DNFB-induced atopic dermatitis model mice. Conclusions : These results suggest that HHT may be used as a potential treatment for AD as a prescription for treatment of atopic dermatitis.

Ameliorating effect of Zhizi (Fructus Gardeniae) extract and its glycosides on scopolamine-induced memory impairment

ObjectiveTo study the chemical constituents of Zhizi (Fructus Gardeniae) and their antiamnesic effect in a mouse model of Alzheimer's disease. MethodsAmeliorating effects of the extracts, fractions and constituents on scopolamine-induced memory impairment in vivo using a passive avoidance task system and their inhibitory activities on acetylcholinesterase (AChE) in vitro were examined. The isolation of components was performed by chromatographic techniques and their structures were identified on the basis of spectral analysis. ResultsActivity-guided fractionation of the total extracts resulted in the isolation of two glycosides, geniposide and crocin from the n-butanol fraction and genipin and crocetin from the ethylacetate fraction. Among the fractions tested, n-butanol fraction showed the strongest AChE inhibition (43.4% at a final dose of 0.03 mg/mL) and also exhibited outstanding efficacy (65.9% at a dose of 250 mg/kg) in an experimental model of amnesia. Geniposide showed a 22.8% AChE inhibitory activity and a potent ameliorating effect on scopolamine-induced memory impairment in amnesic mice of 93.4% as compared to the control group. ConclusionGeniposide, a main constituent of gardenia should be considered a candidate for further clinical study for the purpose of developing a cognition activator and its mechanism of action may be mediated, at least in part, by the acetylcholine enhancing cholinergic nervous system.

D-Galactosamine으로 유발된 흰쥐의 간손상에 대한 치자두시탕 추출액이 미치는 영향

Objectives : To investigate the hepatoprotective effect of Gardeniae Fructus (Ga) and Glycine semen preparatum (Gl) aqueous extract against D-galactosamine (D-GalN, 300㎎/㎏ bo dy weight) was administered to the male Sprague Dawley (SD) rats. Materials and Methods : The study was carried out on male SD rats (age matched, weight 250±10 g). Experimental groups (Exp) divided four : Normal group (Nor) was administered saline, Control (Con) group was only received D-GalN (300 ㎎/㎏) intraperitoneally. Exp was oral ly administered Ga (200 mg/kg; Ga group), Gl (700 mg/kg; Gl group), and Chizadochi-Tang (200 mg/kg+700 mg/kg, GG group) after D-GalN treatment during 14 days (n=6). Results : D-GalN administration induced hepatotoxicity in rats which was manifested by increased levels of aspartate aminotransferase (AST), alanine aminotransferase (ALT ), alkaline phosphatase (ALP) and lactate dehydrogenase (LDH) but decreased total cholesterol (HDL C) and triglyceride (TG). The serum TG concentrations were significantly increased ( # p<0.05) in the Ga group compared with Con. AST and ALP activities were significantly decreased ( # p<0.05) in the all experimental groups compared with Con. ALT activities were significantly decreased ( # p<0.05) in the Ga group compared with Con. LDH activities were significantly decreased ( # p<0.05) in the GG group compared with Con. On the light microscopic study, a number

과루인(瓜蔞仁), 치자(梔子), 백지(白芷)의 시험관내 항균 및 항염 효과

Objectives: The object of this study was to observe the in vitro anti-bacterial and anti-inflammatory effects of three single aqueous herbal extracts(Trichosanthes Semen, Gardeniae Fructus, and Angelicae Dahuricae Radix), traditionally used for treating various gynecological diseases including mastitis in Korea, against Staphylococcus aureus and lipopolysaccharide(LPS)-activated Raw 264.7 cells. Methods: Anti-bacterial activities of three single aqueous herbal extracts against S. aureus were detected using standard agar microdilution methods. In addition, the effects on the cell viability, <TEX>$PGE_2$</TEX>, NO, TNF-<TEX>${\alpha}$</TEX>, IL-<TEX>$1{\beta}$</TEX> and IL-6 productions of LPS activated Raw 264.7 cells. The anti-bacterial and anti-inflammatory effects were compared with lincomycin and piroxicam, respectively in the present study. Results: MIC of three single aqueous herbal extracts against S. aureus were detected as over 25, <TEX>$4.063{\pm}2.096$</TEX> and <TEX>$1.641{\pm}0.972$</TEX> mg/ml, respectively. MIC of lincomycin was detected as <TEX>$0.469{\pm}0.297{\mu}g/ml$</TEX> at same conditions. In addition, <TEX>$ED_{50}$</TEX> against LPS-induced cell viabilities and cytokine releases of three single aqueous herbal extracts were as follows - cell viability: 7.635, 13.761, 6.986 mg/ml, NO production : 4.808, 22.015, 2.949 mg/ml, <TEX>$PGE_2$</TEX> production : 3.040, 4.312, 0.821 mg/ml, TNF-<TEX>${\alpha}$</TEX> production : 9.563, 54.931, 1.240 mg/ml, IL-<TEX>$1{\beta}$</TEX> production : 1.362, 1.801, 0.534 mg/ml, IL-6 production : 0.371, 0.797, 0.202 mg/ml, respectively. <TEX>$ED_{50}$</TEX> of piroxicam against LPS-induced cell viabilities, NO, <TEX>$PGE_2$</TEX>, TNF-<TEX>${\alpha}$</TEX>, IL-<TEX>$1{\beta}$</TEX> and IL-6 were detected as 35.179, 6.552, 1.162, 7.273, 7.101 and 5.044 <TEX>${\mu}g/ml$</TEX>, respectively at same conditions. Conclusions: The results of the study showed anti-bacterial effects against S. aureus in the order of Gardeniae Fructus and Angelicae Dahuricae Radix aqueous extracts, except for Trichosanthes Semen. They also showed anti-inflammatory effects against LPS-activated Raw 264.7 cells in the order of Angelicae Dahuricae Radix, Trichosanthes Semen, and Gardeniae Fructus aqueous extracts. These three herbs are expected to be great substitutes to reduce side-effect of lincomycin and piroxicam, if the amount of those three single aqueous herbal extracts is adjusted appropriately.

Inhibition of enterovirus 71 infections and viral IRES activity by Fructus gardeniae and geniposide

Fructus gardeniae has long been used by traditional Chinese medical practitioners for its anti-inflammatory, anti-oxidant, anti-tumor and anti-hyperlipidemic characteristics. Here we describe our finding that F. gardeniae greatly reduces anti-enterovirus 71 (EV71) activity, resulting in significant decreases in EV71 virus yields, EV71 infections, and internal ribosome entry site activity. We also found that geniposide, a primary F. gardeniae component, inhibited both EV71 replication and viral IRES activity. Our data suggest the presence of a mechanism that blocks viral protein translation. According to our findings, F. gardeniae and geniposide deserve a closer look as potential chemopreventive agents against EV71 infections.

Anti-Hyperglycemic Effect of Single Administered Gardeniae Fructus in Streptozotocin-Induced Diabetic Mice by Improving Insulin Resistance and Enhancing Glucose Uptake in Skeletal Muscle

The mechanisms of Gardeniae Fructus (GF) for anti-hyperglycemic action were demonstrated in streptozotocin (STZ)-diabetic mice. Six hours after single intraperitoneal administration of GF (300 mg/kg) or H2O into 3 hour-fasted STZ-diabetic mice, glucose and insulin tolerances were assessed by intraperitoneal glucose (1.5 g/kg) tolerance test (IPGTT) and intraperitoneal insulin (0.65 U/kg) tolerance test (IPITT), respectively. Effects of GF on insulin signaling pathways in soleus muscle such as glucose uptake, expression of glucose transporter 4 (GLUT4) in the plasma membrane and phosphorylation of Akt (P-Akt) in cytosolic fraction were examined in STZ-diabetic mice. In IPGTT test, GF significantly accelerated clearance of exogenous glucose and its glucose-lowering action was greater than H2O-treated controlin STZ-diabetic mice. GF also promoted an exogenous glucose-increased insulin level in STZ-diabetic mice. In IPITT test, GF decreased glucose level to the greater extent than H2O-treated control in STZ-diabetic mice. Furthermore, GF significantly decreased high HOMA-IR in STZ-diabetic mice from 21.6 ± 2.4 to 12.4 ± 1.9 (mg/dl × μU/ml). These results implied that GF improved insulin resistance in STZ-diabetic mice. GF increased glucose uptake of soleus muscle 1.5 times greater than H2O-treated control in STZ-diabetic mice. GF enlarged insulin (10 nmol/ml)-increased glucose uptake to 1.8 time-greater. Correspondingly, GF increased expression of GLUT4 in the plasma membrane of soleus muscle to 1.4 time-greater, and P-Akt in the cytosolic fraction of soleus muscle to 1.9 time-greater than those in H2O-treated control. In conclusion, the improvement of GF on insulin resistance is associated with the repair of insulin signaling via P-Akt, GLUT4 and glucose uptake pathway in soleus muscle of STZ-diabetic mice.

Effects of Single Administered Bofutsushosan-Composed Crude Drugs on Diabetic Serum Parameters in Streptozotocin-Induced Diabetic Mice

The 18 crude drugs in Bofutsushosan (BOF: Pulvis ledebouriellae compositae: 防風通聖散) are separated into 6 groups such as diaphoretic, cathartic, antidote, antipyretic, neutralizer and diuretic groups. The effects of single administered BOF and composed crude drugs in 6 groups were investigated on the levels of diabetic parameters (serum glucose, insulin, triglyceride and cholesterol) in streptozotocin-induced diabetic mice. The anti-hyperglycemic action of BOF was depended on Ephedrae Herba, Saposhnikoviae Radix and Schizonepetae Spica in diaphoretic group, Forsythiae Fructus, Saposhnikoviae Radix, Schizonepetae Spica and Cnidii Rhizoma in antidote group, Scutellariae Radix, Gardeniae Fructus and Gypsum Fibrosum in antipyretic group and Paeoniae Radix in neutralizer group. In these crude drugs, Ephedrae Herba, Saposhnikoviae Radix, Schizonepetae Spica, Forsythiae Fructus, Scutellariae Radix, Gypsum Fibrosum and Paeoniae Radix increased serum insulin level, but Cnidii Rhizoma and Gardeniae Fructus did not affect serum insulin level. From these results, it suggested that anti-hyperglycemic action of BOF was through insulin-dependent and insulin independent manners. The lowering effect of BOF on serum triglyceride level was dependent on actions of Platycodi Radix in antidote and diuretic groups and Gardeniae Fructus in antipyretic group. The lowering effect of Gardeniae Fructus was parallel with its anti-hyperglycemic action. The lowering effect of BOF on high serum triglyceride level also included both direct action and indirect action. The reducing effect of BOF on serum cholesterol level was observed together with the actions of Ephedrae Herba and Zingiberis Rhizoma in diaphoretic group, Schizonepetae Spica in diaphoretic and antidote groups and Paeoniae Radix in neutralizer group. The lowering effects of Ephedrae Herba, Schizonepetae Spica and Paeoniae Radix on serum cholesterol level were parallel with their anti-hyperglycemic actions. Zingiberis Rhizoma in diaphoretic group might be direct reducing effect on serum cholesterol level but no serum glucose level. The Ephedrae Herba in diaphoretic group, Schizonepetae Spica in diaphoretic and antidote groups and Paeoniae Radix in neutralizer group might have reduced serum cholesterol level by reducing blood glucose level. From these results, composed crude drugs in 6 groups show various mechanisms in the action of BOF.

Effect of Traditional Chinese Herbal Medicine with Antiquorum Sensing Activity onPseudomonas aeruginosa

Traditional Chinese herbal medicines (TCHMs) were tested for their ability of antiquorum sensing. Water extracts of Rhubarb, Fructus gardeniae, and Andrographis paniculata show antiquorumsensing activity when using Chromobacterium violaceum CV12472 as reporter; the sub-MIC concentrations of these TCHMs were tested against AHL-dependent phenotypic expressions of PAO1. Results showed significant reduction in pyocyanin pigment, protease, elastase production, and biofilm formation in PAO1 without inhibiting the bacterial growth, revealing that the QSI by the extracts is not related to static or killing effects on the bacteria. The results indicate a potential modulation of bacterial cell-cell communication, P. aeruginosa biofilm, and virulence factors by traditional Chinese herbal medicine. This study introduces not only a new mode of action for traditional Chinese herbal medicines, but also a potential new therapeutic direction for the treatment of bacterial infections, which have QSI activity and might be important in reducing virulence and pathogenicity of pathogenic bacteria.

Characterization of the Constituents Absorbed in Rats After Oral Administration of Fructus Gardeniae Effective Fraction

Characterization of the Constituents Absorbed in Rats After Oral Administration of Fructus Gardeniae Effective Fraction

Wound-healing plants from TCM: in vitro investigations on selected TCM plants and their influence on human dermal fibroblasts and keratinocytes

Wound-healing plants from Traditional Chinese Medicine and described for wound healing in the Pharmacopoeia of People's Republic of China (2005 ed.) were investigated by in vitro bioassay on human skin cells. Therefore water and EtOH–water extracts (6:4, v/v) from 12 plants were tested on human primary dermal fibroblasts (pNHDF) and human HaCaT keratinocyte cell line by quantification of cell viability (MTT assay) and cellular proliferation (BrdU incorporation ELISA). No functional activity was found for extracts from Achyranthis bidentatae rhizoma, Cimicifugae rhizoma, Corydalis rhizoma, Gardeniae fructus, Houttuyniae herba, Lonicerae japonicae caulis, Paeoniae rubrae radix and Rehmanniae radix. Extracts from Notoginseng radix et rhizoma, Angelicae sinensis radix and Lonicerae japonicae flos showed moderate activity, while extracts from Moutan cortex (the root bark of Paeonia suffruticosa Andr., Ranunculaceae) increased cell viability of HaCaT keratinocytes and pNHDF in a dose-dependent manner significantly. Bioassay-guided fractionation yielded paeonol 1, the flavan-3-ols catechin 2 and epicatechin-3-O-gallate 3, the dimeric proanthocyanidin epicatechin-(4β→8)-catechin 4, a mixture of trigalloyl-glucoses 5 and 1,2,3,4,6-penta-O-galloyl-β-d-glucose (PGG) 6. The proanthocyanidin-containing fractions as well as PGG-containing fractions contributed substantially to the stimulating effects. Especially PGG-containing fractions enhanced cell viability and cellular proliferation of HaCaT keratinocytes at concentration of 100nM.From these data we conclude that indication claims for TCM herbal materials must be carefully investigated in order to establish evidence-driven use of such plants. In case of Moutan cortex skin cell stimulating effects have clearly been proven. These effects can be related to the polyphenol fractions of condensed and hydrolysable tannins.

Semen Ziziphi Spinosae and Fructus Gardeniae extracts synergistically improve learning and memory of a mouse model

Semen Ziziphi Spinosae (SZS) and Fructus Gardeniae (FG) are two herbs commonly used in traditional Chinese medicine. Previous studies have suggested that Fructus Gardeniae as well as Semen Ziziphi Spinosae are able to regulate the function of the central nervous system. However, their effect on learning and memory has yet to be elucidated. In this study, we examined the effect of SZS and FG on the learning and memory of mice using the methods of step-through and -down passive avoidance tasks and Morris water maze tasks. The results showed that SZS and FG extracts have certain effects on improving the performance of the learning and memory-impaired mouse model. Of note, compound extracts of SZS and FG have a synergistic effect on the learning and memory of mice.

A theoretical and experimental study on the Fuzzy evaluation model of biological performance of Chinese materia medica with an either cold or hot herbal property

The concepts of cold and hot herbal properties in traditional Chinese medicine (TCM), reflecting the efficacy trends of medicinal herbs, have the Fuzzy characteristics. It is suited for the application of Fuzzy mathematics in research of herbal properties. For a comprehensive evaluation of herbal properties, this work constructed and made a practice of the Fuzzy discrimination model regarding the biological performance of Chinese materia medica. Firstly, TCM formulas of cold or hot property were employed for setting the reference values and calculating the membership functions of cold and hot Fuzzy sets with Fisher discriminant. Then the model parameters of cold performance function (CPF) and hot performance function (HPF) were acquired. Second, the experimental data from studies on changes in multisystem indicators of animals given the classical cold formula (Sanhuang Fang) and hot formula (Jiangfugui Fang) were collected to calculate CPF and HPF. Then an experiment of administration of hot property herbs, Rougui (Cortex Cinnamomi) and Xianmao (Rhizoma Curculiginis), and cold property herbs, Huangbai (Cortex Phellodendri) and Zhizi (Fructus Gardeniae) to normal animals and animals with glucocorticoid-induced yang-deficiency or yin-deficiency state was designed. The relative changes in animal states were analyzed by the evaluation model to find the way in which herbal properties are represented. The HPF values of biological performance were higher than the CPF values in administration of Rougui to animals of normal (0.528>0.221), yang-deficiency (0.203>-0.490) and yin-deficiency (1.750>-0.479) states, and in administration of Xianmao to animals of normal (0.474>-1.601) and yang-deficiency (0.288>-1.923) states, which represented the hot property. The HPF values of biological performance were lower than the CPF values in administration of Huangbai to animals of normal (-0.870<0.798) and yang-deficiency (-0.339<0.194) states, and in administration of Zhizi to animals of yin-deficiency (-1.802<0.354) state, which represented the cold property. The herbal properties and the biological performance characteristics of herbal formulas are ascertained by using the Fuzzy evaluation model. The personalities, as well as commonalities of herbal properties are key areas for focus because of the multi-approach biological performance of cold and hot property.

Simultaneous determination of eight iridoid glycosides in Gardeniae Fructus by HPLC

To establish an HPLC method for simultaneous determination of eight iridiods in Gardeniae Fructus. Kromasil C18 column (4. 6 mm x 250 mm, 5 microm) was adopted, with acetonitrile-water-trifluoroacetic acid (6:94: 0.05) as the mobile phase at the flow rate of 1.0 mL x min(-1). The detection wavelength was set at 238 nm, and the column temperature was 40 degrees C. The linear ranges of geniposide, gardoside, shanzhiside, geniposidic acid, deacetyl asperulosidic acid methyl ester, gardenoside, scandoside methyl ester, and genipin gentiobioside were 1.5036 - 15.036, 0.04256 - 0.4256, 0.1038 - 1.038, 0.00992 - 0.0992, 0.02332 - 0.2332, 0.4128 - 4.128, 0.02040 - 0.2040 and 0.4656 - 4.656 microg, respectively. Their average recoveries were 99.6% , 100.6% , 101.2%, 99.5%, 100.3% , 98.7%, 99.8% and 100.1%, respectively. The method shows good separation and it is so simple, accurate and highly repeatable that it can be used for providing basis for quality control of Gardeniae Fructus.

The different inhibitory effects of Huang-Lian-Jie-Du-Tang on cyclooxygenase 2 and 5-lipoxygenase

BackgroundHuang-Lian-Jie-Du-Tang (HLJDT), a famous traditional Chinese prescription with wide anti-inflammatory applications, is an aqueous extract of four herbal materials: Rhizoma coptidis, Radix scutellariae, Cortex phellodendri, and Fructus gardeniae. Its effects on the cyclooxygenase (COX)-2 and 5-lipoxygenase (5-LOX) pathways are thought to be responsible for its anti-inflammatory activity. However, our previous work found that the inhibitory effects of HLJDT act on the 5-LOX pathway but not on the COX pathway. The possibility that HLJDT inhibits COX-2- or 5-LOX-catalyzed eicosanoid generation by downregulating enzyme expression requires further investigation. Aim of the studyTo observe the effects of HLJDT and its four major components (baicalin, baicalein, berberine and geniposide) on COX-2- or 5-LOX-catalyzed eicosanoid generation and to distinguish the effects of HLJDT on enzyme activity from those on enzyme expression. MethodsThe topical anti-inflammatory activities and inhibition of eicosanoid formation of HLJDT and its components were observed in an arachidonic acid (AA)-induced mouse ear edema model. Macrophage-based systems were established to observe the effects of the drugs on enzyme activity and enzyme expression of COX-2 and 5-LOX. Further experiments were carried out to confirm these effects at the mRNA and protein levels. ResultsTopical treatment of HLJDT significantly inhibited AA-induced mouse ear edema and reduced PGE2 and LTB4 release in the edematous ears. Baicalein, geniposide, and berberine also ameliorated the symptoms and suppressed eicosanoid generation with varying efficacies. Cell-based assays showed that HLJDT and baicalein inhibited the PGE2 levels by decreasing COX-2 enzyme expression without affecting COX-2 enzyme activity in RAW 246.7 murine macrophages. The other experiments on rat peritoneal macrophages indicated that HLJDT and baicalein exerted significant inhibition on LTB4 production by decreasing 5-LOX enzyme activity. The real-time PCR and western blotting data demonstrated that HLJDT and baicalein reduced COX-2 expression at the mRNA and protein levels, whereas no inhibition on 5-LOX expression was observed. ConclusionsHLJDT can suppress eicosanoid generation via both the COX and LOX pathways, which definitely contributes to its topical anti-inflammatory activity. We have confirmed that its dual inhibition on the COX and LOX pathways mainly result from the downregulation of COX-2 expression and direct inhibition of 5-LOX activity, respectively. Baicalein worked as a potent active component in most of the tests. These findings about the different inhibitory effects of HLJDT on COX-2 and 5-LOX help to better understand the mechanism of HLJDT and promote safer applications of drug.

Melanogenesis Inhibitory Activity of Monoterpene Glycosides from Gardeniae Fructus

A new iridoid glycoside, 10-O-(4"-O-methylsuccinoyl)geniposide (7), and two new pyronane glycosides, jasminosides Q and R (13 and 14, resp.), along with nine known iridoid glycosides, 1-6 and 8-10, and two known pyronane glycosides, 11 and 12, were isolated from a MeOH extract of Gardeniae Fructus, the dried ripe fruit of Gardenia jasminoides (Rubiaceae). The structures of new compounds were elucidated on the basis of extensive spectroscopic analyses and comparison with literature. Upon evaluation of compounds 1-14 on the melanogenesis in B16 melanoma cells induced with α-melanocyte-stimulating hormone (α-MSH), three compounds, i.e., 6-O-p-coumaroylgeniposide (3), 7, and 6'-O-sinapoyljasminoside (12), exhibited inhibitory effects with 21.6-41.0 and 37.5-47.7% reduction of melanin content at 30 and 50 μM, respectively, with almost no toxicity to the cells (83.7-106.1% of cell viability at 50 μM).

Effects of different harvest times and processing methods on quality of Gardeniae Fructus

To study effects of different harvest times and processing methods on the quality of Gardeniae Fructus. The content of asminoidin and the similarity of the fingerprint of Gardeniae Fructus were determined and applied for assessment of the quality. Gardeniae Fructus harvested in October with yellow-green appearance was the better time point for harvest. Drying in the sun and boiling in the water is the better processing method for Gardeniae Fructus. Different harvest times and processing methods can affect the quality of Gardeniae Fructus.