Neuropharmacological insights into Gardenia jasminoides Ellis: Harnessing therapeutic potential for central nervous system disorders.

BACKGROUND: In China, Gardenia jasminoides Ellis (GJE) has a longstanding history of application. The Ministry of Health has listed it as one of the first pharmaceutical or food resources. In ethnic, traditional, and folk medicine, GJE has been used to treat fever and cold and relieve nervous anxiety. Recent studies have confirmed the significant efficacy of GJE for treating central nervous system (CNS) disorders, including Alzheimer's disease, Parkinson's disease, and major depressive disorder; however, GJE has not been systematically evaluated. PURPOSE: This research systematically summarizes global studies on the use of GJE for treating CNS disorders and explores the potential applications and underlying mechanisms via intestinal flora analysis and network pharmacology, aiming to establish a scientific basis for innovative CNS disorder treatment with GJE. METHODS: The PRISMA guidelines were used, and electronic databases such as the Web of Science, PubMed, and China National Knowledge Infrastructure were searched using the following search terms: "Gardenia jasminoides Ellis" with "central nervous system disease," "neuroprotection," "Alzheimer's disease," "Parkinson's disease," "ischemic stroke," "Epilepsy," and "major depressive disorder." The published literature up to September 2023 was searched to obtain relevant information on the application of GJE for treating CNS disorders. RESULTS: There has been an increase in research on the material formulation and mechanisms of action of GJE for treating CNS disorders, with marked effects on CNS disorder treatment in different countries and regions. We summarized the research results related to the role of GJE in vitro and in vivo via multitargeted interventions in response to the complex mechanisms of action of CNS disorders. CONCLUSION: We systematically reviewed the research progress on traditional treatment for GJE and preclinical mechanisms of CNS disorders and explored the potential of optimizing network pharmacology strategies and intestinal flora analysis to elucidate the mechanisms of action of GJE. The remarkable therapeutic efficacy of GJE, an important resource in traditional medicine, has been well documented in the literature, highlighting its significant medicinal potential.

Geniposide from Gardeniae Fructus exerts antipyretic effect in febrile rats through modulating the TLR4/NF-κB signaling pathway.

ETHNOPHARMACOLOGICAL RELEVANCE: The desiccative ripe fruits of Gardenia (Gardenia jasminoides Ellis) (called Zhizi in China) are known with cold character and the effects of reducing fire except vexed, clearing away heat evil, and cooling blood and eliminating stasis. Zhizi is often clinical formulated to treat various types of fever. Fever is a sign of inflammation and, geniposide from Zhizi has been proved with anti-inflammatory in various inflammatory models. AIM OF STUDY: The aim of this study was to investigate the antipyretic role of geniposide with three classical inflammatory fever models and explore the underlying mechanisms. MATERIALS AND METHODS: Water extract (WE), high polar part (HP), iridoid glycoside part (IG), and gardenia yellow pigment part (GYP) from Gardeniae Fructus (GF) were obtained from Zhizi. The antipyretic activities of these composes were tested with dry yeast induced fever rats. Geniposide was further purified from IG and the antipyretic activity was evaluated by gavage, intraperitoneal injection, and caudal intravenous injection to rats of fever induced by dry yeast, lipopolysaccharide (LPS), and 2, 4-dinitrophenol (DNP) in rats. Then, the mechanism of geniposide by intragastric administration was studied. The contents of thermoregulatory mediators and inflammatory factors relating to TLR4/NF-κB pathway in serum were determined by ELISA and Western blot, and the pathological changes of the hypothalamus were observed by HE staining. RESULTS: The temperature was decreased by geniposide in the three fever model rats. Geniposide can not only inhibit the increase of inflammatory factors in serum but also protect the hypothalamus from fever pathological damage in the three fever models. Western blot showed that geniposide could inhibit the TLR4/NF-κB pathway. CONCLUSION: Geniposide exerts antipyretic effect in febrile rats through modulating the TLR4/NF-κB signaling pathway.

Integration of Deep Learning and Sequential Metabolism to Rapidly Screen Dipeptidyl Peptidase (DPP)-IV Inhibitors from Gardenia jasminoides Ellis.

Traditional Chinese medicine (TCM) possesses unique advantages in the management of blood glucose and lipids. However, there is still a significant gap in the exploration of its pharmacologically active components. Integrated strategies encompassing deep-learning prediction models and active validation based on absorbable ingredients can greatly improve the identification rate and screening efficiency in TCM. In this study, the affinity prediction of 11,549 compounds from the traditional Chinese medicine system's pharmacology database (TCMSP) with dipeptidyl peptidase-IV (DPP-IV) based on a deep-learning model was firstly conducted. With the results, Gardenia jasminoides Ellis (GJE), a food medicine with homologous properties, was selected as a model drug. The absorbed components of GJE were subsequently identified through in vivo intestinal perfusion and oral administration. As a result, a total of 38 prototypical absorbed components of GJE were identified. These components were analyzed to determine their absorption patterns after intestinal, hepatic, and systemic metabolism. Virtual docking and DPP-IV enzyme activity experiments were further conducted to validate the inhibitory effects and potential binding sites of the common constituents of deep learning and sequential metabolism. The results showed a significant DPP-IV inhibitory activity (IC50 53 ± 0.63 µg/mL) of the iridoid glycosides' potent fractions, which is a novel finding. Genipin 1-gentiobioside was screened as a promising new DPP-IV inhibitor in GJE. These findings highlight the potential of this innovative approach for the rapid screening of active ingredients in TCM and provide insights into the molecular mechanisms underlying the anti-diabetic activity of GJE.

Gardenia (Gardenia jasminoides Ellis) fruit: a critical review of its functional nutrients, processing methods, health-promoting effects, comprehensive application and future tendencies.

Gardenia fruit (GF) is the mature fruit of Gardenia jasminoides Ellis, boasting a rich array of nutrients and phytochemicals. Over time, GF has been extensively utilized in both food and medicinal contexts. In recent years, numerous studies have delved into the chemical constituents of GF and their associated pharmacological activities, encompassing its phytochemical composition and health-promoting properties. This review aims to provide a critical and comprehensive summary of GF research, covering nutrient content, extraction technologies, and potential health benefits, offering new avenues for future investigations and highlighting its potential as an innovative food resource. Additionally, the review proposes novel industrial applications for GF, such as utilizing gardenia yellow/red/blue pigments in the food industry and incorporating it with other herbs in traditional Chinese medicine. By addressing current challenges in developing GF-related products, this work provides insights for potential applications in the cosmetics, food, and health products industries. Notably, there is a need for the development of more efficient extraction methods to harness the nutritional components of GF fully. Further research is needed to understand the specific molecular mechanisms underlying its bioactivities. Exploring advanced processing techniques to create innovative GF-derived products will show great promise for the future.

Rapid extraction of bioactive compounds from gardenia fruit using new and recyclable deep eutectic solvents.

The utilization of deep eutectic solvent as an alternative and environmentally friendly option has gained significant attention. This study first proposed a series of benzylammonium chloride based-deep eutectic systems for the extraction of bioactive compounds from Gardenia jasminoides Ellis. Through the implementation of response surface methodology, the optimal solvent was determined to be dodecyldimethylbenzylammonium chloride-levulinic acid (1:3, mol/mol) with 35% (v/v) water, specifically tailored to extract geniposide, genipin-1-ß-d-gentiobioside, crocin-1, and crocin-2 from gardenia fruits with the ratio of solid to liquid of 1:20 at 86°C for 16 min. Their total extraction yields could reach 70.6 mg/g, outperforming those obtained by other solvents and corresponding techniques. Furthermore, the eutectic system was retrieved after first-cycle extraction, and then applied in the subsequent extraction progress, yielding a consistent extraction efficiency of 97.1%. As compared to previous traditional methods, a quick, high-yielding, and green extraction procedure was achieved through simple heating settings that did not constrain the instrument. Therefore, dodecyldimethylbenzylammonium chloride-levulinic acid could serve as a sustainable and reusable solvent for efficient extraction of natural bioactive compounds from plant-based raw materials. The application of deep eutectic solvents has demonstrated their potential as designable solvents with stronger extraction capabilities than traditional organic solvents.

Characterization and quantification of the Chinese medical formula Zhi-Zi-Chi decoction, a systematic strategy for the attenuation and synergy of compatibility mechanism.

Zhi-Zi-Chi decoction (ZZCD), comprising of Gardenia jasminoides Ellis (GJE) and Semen sojae preparatum (SSP), is a classical Chinese medicine formula. A novel analysis strategy was set up to obtain an evaluation of ZZCD on attenuation and synergy of compatibility. High-resolution ion trap/time-of-flight mass spectrometry (LC-IT-TOF-MS) was used for qualitative analysis. Variant ingredients were analyzed to compare the componential differences between ZZCD formula and single herbs. Based on our previous fingerprint studies that combined with chemometric methods, 13 remarkable chemical markers were selected and evaluated for quantitative determination by high performance liquid chromatography (HPLC) in three different ratios of ZZCD. 62 compounds in ZZCD, 55 compounds in GJE and 16 compounds in SSP were characterized. The compatibility of GJE and SSP may lead to the undetection of hepatotoxic components such as genipin and the emergence of protective components such as jasminoside A, which was not found in single herbs. Meanwhile, 13 selected chemical markers were successfully determined in three ratios of ZZCD. The compatibility may lead to the decrease of toxic ingredients and the increase of beneficial ingredients. By comparing the dissolution of chemical markers, iridoids in GJE and flavonoids in SSP had the best dissolution when the compatibility ratio was 1:1. This strategy would be a valuable reference for further study on the compatibility of traditional Chinese medicine formula.

Gardenia jasminoides Ellis polysaccharide ameliorates cholestatic liver injury by alleviating gut microbiota dysbiosis and inhibiting the TLR4/NF-κB signaling pathway.

Gardenia jasminoides Ellis is a well-known herbal medicine. In this study, the effect of G. jasminoides Ellis polysaccharide (GPS) on liver injury in an alpha-naphthylisothiocyanate (ANIT)-induced cholestatic mouse model and the associated molecular mechanisms were investigated. GPS administration dose-dependently ameliorated impaired hepatic function, including a 2-7-fold decrease in aminotransferase levels, ameliorating tissue damage, upregulating the expression of farnesoid X receptor (FXR) and pregnane X receptor (PXR) and their downstream efflux transporters, and decreasing the levels of 12 bile acids (BAs), in cholestatic mice. Furthermore, GPS ameliorated gut microbiota dysbiosis, improved intestinal barrier function, and reduced serum and hepatic lipopolysaccharide levels 1.5-fold. GPS also inhibited the Toll-like receptor 4 (TLR4)/nuclear factor kappa-B (NF-κB) signaling, decreased the expression of inflammatory factor genes, and ameliorated hepatic inflammation. Notably, fecal microbiota transplantation from GPS-fed mice also increased the hepatic expression of FXR, PXR, and efflux transporters; decreased the levels of 12 BAs; restored intestinal barrier function; and decreased hepatic inflammation mediated by the TLR4/NF-κB pathway. In conclusion, GPS has a protective effect against cholestatic liver injury through modulation of gut microbiota and inhibition of the TLR4/NF-κB pathway. Regulating gut microbiota using herbal medicine polysaccharides may hold unique therapeutic promise for cholestatic liver diseases.

Gardenia jasminoides Ellis: Ethnopharmacology, phytochemistry, and pharmacological and industrial applications of an important traditional Chinese medicine.

ETHNOPHARMACOLOGICAL RELEVANCE: Gardenia jasminoides Ellis is a popular shrub in the Rubiaceae family. The desiccative ripe fruits of this plant (called Zhizi in China) are well known and frequently used not only as an excellent natural colourant, but also as an important traditional medicine for the treatment of different diseases, such as reducing fire except vexed, clearing away heat evil, and cooling blood and eliminating stasis to activate blood circulation. It has also been declared as the first batch of dual-purpose plants used for food and medical functions in China. AIM OF THE STUDY: This review aims to provide a critical and systematic summary of the traditional uses, ethnopharmacology, phytochemistry, pharmacology, toxicity and industrial applications of Gardenia jasminoides Ellis and briefly proposes several suggestions for future application prospects. MATERIALS AND METHODS: The related information on Gardenia jasminoides Ellis was obtained from internationally recognized scientific databases through the Internet (PubMed, CNKI, Google Scholar, Baidu Scholar, Web of Science, Medline Plus, ACS, Elsevier and Flora of China) and libraries. RESULTS: Approximately 162 chemical compounds have been isolated and identified from this herb. Among them, iridoid glycosides and yellow pigment are generally considered the main bioactive and characteristic ingredients. Various pharmacological properties, such as a beneficial effect on the nervous, cardiovascular and digestive systems, hepatoprotective activity, antidepressant activity, and anti-inflammatory activity, were also validated in vitro and in vivo. Moreover, geniposide and genipin are the most important iridoid compounds isolated from Gardenia jasminoides Ellis, and genipin is the aglycone of geniposide. As the predominant active ingredient with a distinct pharmacological activity, genipin is also an outstanding biological crosslinking agent. Gardenia yellow pigment has also been widely used as an excellent natural dye-stuff. Hence, Gardenia jasminoides Ellis has been applied to many other fields, including the food industry, textile industry and chemical industry, in addition to its predominant medicinal uses. CONCLUSIONS: According to this review, Gardenia jasminoides Ellis is outstanding traditional medical plant used in medicine and food. Pharmacological investigations support the traditional use of this herb and may validate the folk medicinal use of Gardenia jasminoides Ellis to treat different diseases. Iridoid glycosides are potential medicines. Gardenia yellow pigment has been the most important source of a natural colourant for food, cloth and paint for thousands of years. This herb has made great contributions to human survival and development. Moreover, it has also achieved outstanding progress in human life and even in art. Although Gardenia jasminoides Ellis has extremely high and comprehensive utilization values, it is still far from being completely explored. Therefore, the comprehensive development of Gardenia jasminoides Ellis deserves further analysis.

Comparative anti-arthritic investigation of iridoid glycosides and crocetin derivatives from Gardenia jasminoides Ellis in Freund's complete adjuvant-induced arthritis in rats.

BACKGROUND: Discovering novel compounds with higher activities is a key aim of natural products research. Gardenia jasminoides Ellis is a herb with anti-inflammatory properties. Iridoid glycosides (mainly geniposide) and crocetin derivatives (crocins) are the two major active constituents in this herb and are considered its active ingredients. However, which components are responsible for the anti-inflammatory properties of gardenia have remained to be investigated. PURPOSE: Here, we prepared total iridoid glycocides (TIG) and total crocins (TC) from G. jasminoides Ellis, determined their main chemical constituents, and performed animal studies to evaluate their anti-adjuvant arthritis activities, thus, proposing a reasonable mechenism to explain the anti-inflammatory activities of the active components in this herbal remedy. STUDY DESIGN: TIG and TC were prepared by using HPD-100 macroporous resin, and characterized by UHPLC-DAD-MS and UV-Vis spectrophotometer. Then, freund's complete adjuvant-injected rats underwent drug treatments with TIG (160 mg/kg) and TC (160 mg/kg) for 14 days, and their ankle diameters were measured. Moreover, X-ray radiographs of the adjuvant injected hind paws were evaluated. Finally, histopathological examinations of the ankle joints, spleens and thymus were carried out to evaluate inflammatory reactions, and immunohistochemical measurements were conducted to evaluate TNF-α and TGF-ß1 expression in the ankle joint of the rats. RESULTS: The chemical composition determination of the current study showed that TIG was mainly composed of geniposide and TC was a fraction predominantly with crocin-1, crocin-2 and crocin-3. Calculation of results showed that TIG and TC contained 58.2% total iridoid glycosides and 54.7% total crocins, respectively. Our study suggested TIG and TC treatments markedly decreased paw swelling and ankle diameters of AA rats (both p < 0.05). The radiological analysis showed that administration of TIG and TC ameliorated bone destruction, and reduced the radiological bone destruction scores (TIG p < 0.05, TC p>0.05). Moreover, data from histological assessment demonstrated considerable mitigation of inflammation in the joints (both p < 0.01), spleen and thymus of AA rats treated with TIG and TC. TNF-α and TGF-ß1 protein expression according to immunohistochemistry staining also supported the anti-arthritis activities of TIG and TC (TNF-α: TIG p < 0.01 and TC p < 0.05, TGF-ß1: TIG p < 0.01 and TC p>0.05). CONCLUSION: In the current study, fractionation of gardenia prior to further in vivo investigation has for the first time provided reasonable explanation for the anti-inflammatory activity of this herbal remedy. Our study showed that both TIG and TC from gardenia have anti-inflammatory properties. Overall, these experimental findings suggest that gardenia could be regarded as a potential therapeutic target for arthritis. However, as geniposide has a higher content than crocins in this herbal drug, TIG (mainly geniposide) seems to be primarily responsible for the anti-inflammatory properties of gardenia. Taken together, this maiden attempt demonstrated that TIG (mainly geniposide) is more important in evaluating the anti-inflammatory activity of G. jasminoides Ellis.

Mechanism of crocin compounds from Gardenia jasminoides in Zhejiang Province by network pharmacology / 中草药

Objective: To investigate the pharmacological mechanism of the crocin compounds from Gardenia jasminoides in Zhejiang Province by using network pharmacology. To provide a valuable research strategy for the rational use and in-depth research and development of G. jasminoides from Zhejiang. Methods: Our previous research results showed that the Zhejiang area of Gardenia crocin content and other areas have significant difference. Based on the results, the crocin compounds from G. jasminoides were used to predict the targets according to Pubchem, Uniprot, STITCH, SWISS, and TCMSP online databases. Cytoscape software was used to construct compound-target-disease network of the G. jasminoides crocin ingredients. The targets were analyzed by Gene ontology (GO) enrichment and KEGG pathway analysis using CTD online analysis platform to analyze main biological pathways for obtaining the deep mechanism of G. jasminoides in Zhejiang. Results: The crocin compounds from G. jasminoides in Zhejiang Province were obtained through previous work and network pharmacology screening, such as crocin-1 and crocin-2, and 18 corresponding targets were acted, such as FGF2, VEGFA, KDR, and FLT1. These targets could joint in pathways, such as GPCR, Rap1, and Ras signaling pathway. These ingredients are mainly used to treat 18 related diseases such as cardiovascular diseases, tumors and digestive system. Conclusion: The method based on system pharmacology could help to find the key targets of characteristic high-content chemical constituents of herb from different producing areas, signaling pathway and disease network of traditional Chinese medicine (TCM), and provide useful information and data support for giving a further study on TCM resources in different regions of China.

Research progress on chemical composition and pharmacological effects of Gardenia jasminoides and predictive analysis on quality marker (Q-marker) / 中草药

Gardenia jasminoides is a traditional Chinese herbal medicine, which is also the first batch of being used for both medicine and food issued by Ministry of Health of China. In recent years, G. jasminoides has been applied widely in medicine and health food, so the quality evaluation of G. jasminoides has become a key problem urgently needed to be solved in this industry. Based on the review of its chemical composition and pharmacological effects, combined with the definition of Q-marker, this study processed predictive analysis on Q-marker of G. jasminoides from several aspects at chemical composition, new clinical use, measurable composition, traditional medicine properties and efficacy, plasma composition, and storage time, which provides the basis for quality evaluation of G. jasminoides.

A novel strategy for evaluation of natural products acting on the myeloperoxidase/hypochlorous acid system by combining high-performance liquid chromatography-photodiode array detection-chemiluminescence and ultrafiltration-mass spectrometry techniques.

Myeloperoxidase and its product hypochlorous acid are endogenous substances that are involved in the pathogenesis of many inflammatory diseases. In the present study, a novel evaluation strategy has been developed to screen for myeloperoxidase inhibitors and hypochlorous acid scavengers in natural products. The evaluation strategy uses two methods: a multi-hyphenated high-performance liquid chromatography-photodiode array detection-chemiluminescence online method, and an ultrafiltration-high-performance liquid chromatography-mass spectrometry method. Both were used for screening hypochlorous acid scavengers and myeloperoxidase inhibitors. After optimization of operating conditions, including pH of mobile phase and concentrations of myeloperoxidase, hypochlorous acid and luminol, the evaluation strategy was applied to Gardenia jasminoides Ellis (Rubiaceae) extract. Gardenia jasminoides Ellis (Rubiaceae) extract was found to both scavenge hypochlorous acid and inhibit myeloperoxidase. These different bioactivities originate from iridoid glycosides and quinic acid derivatives (25 hypochlorous acid scavengers) and crocetin derivatives (4 myeloperoxidase inhibitors). In a mouse model of acute lung injury, pulmonary histopathology showed that different constituents of Gardenia jasminoides Ellis (Rubiaceae) extract could also attenuate lung injury. Although the screening strategy has two arms, it is still simple, rapid, and effective. The strategy can also potentially be used to discriminate different activities of different constituents contained in the same natural product.

Identification of Steroidogenic Components Derived From Gardenia jasminoides Ellis Potentially Useful for Treating Postmenopausal Syndrome.

Estrogen-stimulating principles have been demonstrated to relieve postmenopausal syndrome effectively. Gardenia jasminoides Ellis (GJE) is an herbal medicine possessing multiple pharmacological effects on human health with low toxicity. However, the therapeutic effects of GJE on the management of postmenopausal syndrome and its mechanism of action have not been fully elucidated. In this study, network pharmacology-based approaches were employed to examine steroidogenesis under the influence of GJE. In addition, the possibility of toxicity of GJE was ruled out and four probable active compounds were predicted. In parallel, a chromatographic fraction of GJE with estrogen-stimulating effect was identified and nine major compounds were isolated from this active fraction. Among the nine compounds, four of them were identified by network pharmacology, validating the use of network pharmacology to predict active compounds. Then the phenotypic approaches were utilized to verify that rutin, chlorogenic acid (CGA) and geniposidic acid (GA) exerted an estrogen-stimulating effect on ovarian granulosa cells. Furthermore, the results of target-based approaches indicated that rutin, CGA, and GA could up-regulate the FSHR-aromatase pathway in ovarian granulosa cells. The stimulation of estrogen production by rat ovarian granulosa cells under the influence of the three compounds underwent a decline when the follicle-stimulating hormone receptor (FSHR) was blocked by antibodies against the receptor, indicating the involvement of FSHR in the estradiol-stimulating activity of the three compounds. The effects of the three compounds on estrogen biosynthesis- related gene expression level were further confirmed by Western blot assay. Importantly, the MTT results showed that exposure of breast cancer cells to the three compounds resulted in reduction of cell viability, demonstrating the cytotoxicity of the three compounds. Collectively, rutin, chlorogenic acid and geniposidic acid may contribute to the therapeutic potential of GJE for the treatment of postmenopausal syndrome.

Research and application progress of Gardenia jasminoides / 中草药·英文版

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.

Comparative investigation on the pharmacokinetics of geniposide in type 2 diabetic and normal rats after oral administration of Fructus Gradeniae extract.

Fructus Gradeniae, the fruit of Gardenia jasminoides Ellis, was used alone or in combination with other herb medicines in the treatment of type 2 diabetes mellitus in China for a long time. In present investigation, the HPLC method for the determination of geniposide in rat plasma was developed and validated, and the pharmacokinetics of geniposide in type 2 diabetic rats after oral administration of Fructus Gradeniae extract or pure was studied. The results showed that the pharmacokinetic profile (especially the area under the plasma concentration-time curve, AUC) of geniposide in type 2 diabetic rats after orally administered with Fructus Gradeniae extract or pure geniposide was remarkably different from that in normal rats. The results indicated that the increased AUC of geniposide in type 2 diabetic rats did not result from the effects of other components contained in Fructus Gradeniae. It could be speculated that the increased AUC of geniposide might result from the pathological state of type 2 diabetes mellitus which resulted in the pharmacokinetic alterations of geniposide.

A strategy for identification and structural characterization of compounds from Gardenia jasminoides by integrating macroporous resin column chromatography and liquid chromatography-tandem mass spectrometry combined with ion-mobility spectrometry.

In this paper, an analysis strategy integrating macroporous resin (AB-8) column chromatography and high performance liquid chromatography-electrospray ionization-tandem mass spectrometry (HPLC-ESI-MS/MS) combined with ion mobility spectrometry (IMS) was proposed and applied for identification and structural characterization of compounds from the fruits of Gardenia jasminoides. The extracts of G. jasminoides were separated by AB-8 resin column chromatography combined with reversed phase liquid chromatography (C18 column) and detected by electrospray ionization tandem mass spectrometry. Additionally, ion mobility spectrometry (IMS) was employed as a supplementary separation technique to discover previously undetected isomers from the fruits of G. jasminoides. A total of 71 compounds, including iridoids, flavonoids, triterpenes, monoterpenoids, carotenoids and phenolic acids were identified by the characteristic high resolution mass spectrometry and the ESI-MS/MS fragmentations. In conclusion, the IMS-MS technique achieved the separation of isomers in crocin-3 and crocin-4 according to their acquired mobility drift times differing from classical analysis by mass spectrometry. The proposed strategy can be used as a highly sensitive and efficient procedure for identification and separation isomeric components in extracts of herbal medicines.

Two standardized fractions of Gardenia jasminoides Ellis with rapid antidepressant effects are differentially associated with BDNF up-regulation in the hippocampus.

ETHNOPHARMACOLOGICAL RELEVANCE: Gardenia jasminoides Ellis (GJ) is one of the five constituents of Yueju pill, a Traditional Chinese Medicine for treatment of syndromes associated with mood disorders. Recently, preclinical and clinical studies suggest that Yueju pill confers rapid antidepressant effects. GJ is identified as the constituent primary for Yueju pill's rapid antidepressant effects. GJ's antidepressant action is temporally associated with up-regulated expression of brain-derived neurotrophic factor (BDNF) in the hippocampus. The present study aimed to identify chemical fractions responsible for the rapid antidepressant efficacy of GJ and its association with BDNF signaling. MATERIALS AND METHODS: Four fractions of GJ were extracted using standardized procedure. The four fractions were screened for rapid antidepressant potential, using the behavioral paradigm of forced swimming test (FST) and tail suspension test (TST) assessed at 24h post a single administration. A single dose of the putatively effective fractions was further tested in mice exposed to chronic mild stress (CMS), followed with a comprehensive behavioral testing including TST, FST, sucrose preference test (SPT), and novelty suppressed-feeding (NSF). To test the association of BDNF signaling with rapid antidepressant effects of effective factions, the expressions of BDNF and its receptor tropomyosin receptor kinase B (TrkB) in the hippocampus were assessed at different times post a single administration of effective fractions. RESULTS: Both petroleum ether (GJ-PE) and n-butyl alcohol fraction (GJ-BO) fractions of GJ displayed rapid antidepressant potential in the FST. In the TST, the antidepressant effects of GJ-PE lasted for a longer time than GJ-BO. Acute administration of either GJ-PE or GJ-BO significantly reversed the behavioral deficits in the tests of TST, FST, SPT and NSF in chronically stressed mice, confirming both fractions conferred rapid antidepressant efficacy. Interestingly, GJ-PE, but not GJ-BO, increased the expression of BDNF and TrkB in the hippocampus post a single administration. CONCLUSION: Two standardized fractions GJ-PE and GJ-BO exhibited comparable rapid antidepressant-like effects on the CMS mice. However, only the effects of GJ-PE was associated with BDNF signaling.

Chemical fingerprinting of Gardenia jasminoides Ellis by HPLC-DAD-ESI-MS combined with chemometrics methods.

A fingerprint analysis method has been developed for characterization and discrimination of Gardenia jasminoides Ellis from different areas. The chemometrics methods including similarity evaluation, principal components analysis (PCA) and hierarchical clustering analysis (HCA) were introduced to identify more useful chemical markers for improving the quality control standard of dried ripe fruits of G. jasminoides Ellis. Then the selected chemical markers were analyzed by high performance liquid chromatography-diode array detection-electrospray ionization mass spectrometry (HPLC-DAD-ESI-MS) qualitatively and quantitatively. 23 characteristic peaks were assigned while 19 peaks of them were identified by comparing retention times, UV and MS spectra with authentic compounds or literature data. Moreover, 14 of them were determined quantitatively which could effectively evaluate the quality of G. jasminoides Ellis. This study was expected to provide comprehensive information for the quality evaluation of G. jasminoides Ellis, which would be a valuable reference for further study and development of this herb and related medicinal products.

Isolation and purification of six iridoid glycosides from gardenia jasminoides fruit by medium-pressure liquid chromatography combined with macroporous resin chromatography.

Gardeniae fructus is one of the most frequently used herbs in traditional Chinese medicine. In the present study, a process for the enrichment of six iridoid glycosides from Gardeniae fructus was developed using medium-pressure liquid chromatography combined with macroporous resin and reversed-phase chromatography. The purities of different fractions from Gardeniae fructus were assessed using quantitative high-performance liquid chromatography. After fractionation using HPD-100 column chromatography, a 30% ethanol fraction was selected based on high-performance liquid chromatography and liquid chromatography with mass spectrometry qualitative analysis to separate and purify. Based on the orientation analysis results, six compounds-deacetyl asperulosidic acid methyl ester, gardenoside, ixoroside, scandoside methyl ester, genipin-1-O-ß-d-gentiobioside, and geniposide-were successfully isolated and purified in three to four combined steps from Gardeniae fructus. The purities of these compounds were found by high-performance liquid chromatography analysis to be 97.9, 98.1, 95.5, 96.3, 97.1, and 98.7%, respectively. Moreover, their structures were elucidated by NMR spectroscopy and liquid chromatography with tandem mass spectrometry. The separation process was highly efficient, rapid, and accurate, making it a potential approach for the large-scale production of iridoids in the laboratory and providing several marker compounds for quality control. This procedure may be meaningful for the purification of other natural products used in traditional Chinese medicine.

Some results of the study to establish the quality indicators of tsusan bolor capsules / Монголын Анагаах Ухаан

Introduction Along with the changes occurred in nutrition, climate over the years, the prevalence of blood disorder related diseases, such as Аllergic purpura (AP), Idiopathic thrombocytopenic purpura (ITP) is increasing. The current perspective of health service is focused on the treatment of AP and ITP by using combined therapeutic methods of modern and Mongolian medical approach. Mongolian traditional medicine has an advantage of reducing complications in reducing the recovery duration and also preventing from re-occurrence. Consequently, there is a need for investigation of formulating clinically effective preparation that complies with pharmaceutical standards. Objective The objective of this study was to develop the technology to obtain Tsusan Bolor capsules and establish its some quality criteria indicators. Materials and Methods The medicinal raw materials Gardenia Jasminoides Ellis, Rubia cordiofolia L, Picrorhiza serophulariflora Pennell, Arnebia guttatа, Crocus sativus, L, Pulvis Cornus Bubali and Artificial Bezoar were provided by Traditional medicine factory of the Inner Mongolian University for Nationalities, PRC. The L9(34) experiment test was used to obtain the extracts from crude medicinal plants and TLC, HPLS and pharmacopeias methods were used for the establishing quality criteria indicators of the capsules. Results Within the technological study the appropriate methods to obtain alcohol and water extracts from the medicinal raw materials and the technological scheme to obtain Tsusan bolor capsules were developed. As the results of quality criteria investigation indicated, the total content of gardenia glycoside is 1.71±0.02 mg, water content- 6.25±0.1%, heavy metal and arsenic content less than 10 μg/g and 2μg/g and disintegration time of the capsules is 20±3.