Gardeniae Fructus Research Articles

Microbial transformation of geniposide in Gardeniae Fructus under the fermentation with Aspergillus niger DQWM-G11

Gardeniae Fructus, the dried fruit of Gardenia jasminoides, was fermented with Aspergillus niger DQWM-G11. The antibacterial activities of the fermented and non-fermented products were measured and the transformation of chemical constituents was detected. The results revealed that A. niger DQWM-G11 fermented Gardeniae Fructus (AFGF) possessed a stronger antibacterial effect with a minimal inhibitory concentration (MIC) value of 256 μg/mL, compared to the raw material (MIC: > 1024 μg/mL). An undescribed microbial transformation reaction was discovered, where geniposide (1) was transformed into 1β-methoxyl-4-epigardendiol (2), which was then verified. The produced component exhibited a stronger antibacterial effect (MIC: 256 μg/mL) than raw geniposide (1) (MIC: >1024 μg/mL), indicating that the increased activity of Gardeniae Fructus was due to the biotransformation. The discovery of this microbial transformation reaction will provide an important theoretical basis for further developing and applying Gardeniae Fructus and geniposide.

Calcification of the mesenteric veins suspected of idiopathic mesenteric phlebosclerosis associated with long‐term herbal medicine ‘inchinkoto’ prescribed for biliary atresia: A multicenter study

AbstractAimInchinkoto (ICKT) is administered to patients with biliary atresia (BA) after surgery. Gardeniae fructus which is contained in ICKT is reported to be associated with idiopathic mesenteric phlebosclerosis (IMP). We investigated the influence of ICKT on calcification of the mesenteric veins suspected of IMP in BA patients.MethodsAll BA patients with native liver survival who received ICKT after Kasai portoenterostomy were reviewed. All patients underwent abdominal computed tomography (CT) during treatment. Calcification of the mesenteric veins on the most recent CT scan after the initiation of ICKT was assessed.ResultsTwenty patients (6 males and 14 females) were enrolled in this study. Of these patients, 17 (85.0%) and 10 (50%) patients had used ICKT for ≥5 years and >10 years, respectively. Calcification of the mesenteric veins was detected in one patient, who was a 14 year old girl. The total dosage of Gardeniae fructus was 21 800 g.ConclusionsThe incidence of calcification of the mesenteric veins in BA patients receiving ICKT was low. However, it is necessary to be aware that ICKT containing Gardeniae fructus is associated with the risk of developing calcification of the mesenteric veins suspected of IMP.

Characterization of carbon dots from fructus gardeniae (Zhi-zi) and gardenia charcoal (black Zhi-zi) via microwave-assisted extraction

Characterization of carbon dots from fructus gardeniae (Zhi-zi) and gardenia charcoal (black Zhi-zi) via microwave-assisted extraction

A refined formula derived from Jiawei-Xiaoyao pill exerts rapid antidepressant-like effects in LPS-induced depression by reducing neuroinflammation and restoring neuroplasticity signaling

Ethnopharmacological relevanceJiawei-Xiaoyao Pill (JWX), a classic formula in traditional Chinese medicine, is derived from Xiaoyao Pill by adding significant amounts of Gardeniae Fructus (GF) and Moutan Cortex (MC). It is frequently used for the treatment of depression. JWX has been demonstrated to uniquely elicit rapid antidepressant-like effects within the prescribed dosage range. To date, GF has been shown to have rapid antidepressant-like effects, but a much higher dose is required than its proportion in JWX. It is assumed that the synergism of GF with a minimum number of other herbs in JWX serves as a refined formula that exerts these rapid antidepressant-like effects. Identification of a refined formula is important for prioritizing the herbs and ingredients to optimize the quality control of JWX. However, such a refined formula for JWX has not been identified yet. Aim of the studyHere we aimed to identify a refined formula derived from JWX for optimized rapid antidepressant-like effects. Since the neuroinflammation mechanism involving in depression treatment has not been previously investigated for JWX, we tested the mechanism for both JWX and the refined formula. Materials and methodsIndividual herbs (MC; ASR, Angelica Sinensis Radix; Bupleuri Radix; Paeonia Radix Alba) that show antidepressant-like responses were mixed with GF at the proportional dosage in JWX to identify the refined formula. Rapid antidepressant-like effects were assessed by using NSF (Novelty Suppressed Feeding Test) and other behavioral tests following a single administration. The identified formula was further tested in a lipopolysaccharide (LPS)-induced depressive model, and the molecular signaling mechanisms were investigated using Western blot analysis, immunofluorescence, and pharmacological inhibition of mTOR signaling. Scopolamine (Scop) was used as a positive control for induction of rapid antidepressant effects. ResultsA combination of GF, MC and ASR (GMA) at their dosages proportional to JWX induced behavioral signs of rapid antidepressant-like responses in both normal and LPS-treated mice, with the antidepressant-like effects sustained for 5 d. Similar to JWX or Scop, GMA rapidly reduced the neuroinflammation signaling of Iba-1-NF-кB, enhanced neuroplasticity signaling of CaMKII-mTOR-BDNF, and attenuated the upregulated expressions of the NMDAR sub-units GluN1 and GluN2B in the hippocampus of LPS-treated mice. GMA, JWX and Scop rapidly restored the number of BDNF-positive cells reduced by LPS treatment in the CA3 region of the hippocampus. Furthermore, rapamycin, a selective inhibitor of mTOR, blunted the rapid antidepressant-like effects and hippocampal BDNF signaling upregulation by GMA. ConclusionGMA may serve as a refined formula from JWX, capable of inducing rapid antidepressant-like effects. In the LPS-induced depression model, the effects of GMA were mediated via rapidly alleviating neuroinflammation and enhancing neuroplasticity.

A metabolomics study on the mechanisms of Gardeniae fructus against α-naphthylisothiocyanate-induced cholestatic liver injury.

Gardeniae fructus (GF) is known for its various beneficial effects on cholestatic liver injury (CLI). However, the biological mechanisms through which GF regulates CLI have not been fully elucidated. This study aimed to explore the potential mechanisms of GF against α-naphthylisothiocyanate (ANIT)-induced CLI. First, HPLC technology was used to analyze the chemical profile of the GF extract. Second, the effects of GF on serum biochemical indicators and liver histopathology were examined. Lastly, metabolomics was utilized to study the changes in liver metabolites and clarify the associated metabolic pathways. In chemical analysis, 10 components were identified in the GF extract. GF treatment regulated serum biochemical indicators in ANIT-induced CLI model rats and alleviated liver histological damage. Metabolomics identified 26 endogenous metabolites as biomarkers of ANIT-induced CLI, with 23 biomarkers returning to normal levels, particularly involving primary bile acid biosynthesis, glycerophospholipid metabolism, tryptophan metabolism, and arachidonic acid metabolism. GF shows promise in alleviating ANIT-induced CLI by modulating multiple pathways.

Neuroprotective effect of GJ-4 against cognitive impairments in vascular dementia by improving white matter damage

BackgroundWhite matter lesions (WMLs) are increasingly linked to the pathological process of chronic vascular dementia (VaD). An effective crocins fraction extracted from Gardenia Fructus, GJ-4, has been shown to improve cognitive function in several Alzheimer's disease models and VaD models. ObjectivesTo explore the potential mechanisms of GJ-4 on WMLs in a chronic VaD mouse model. MethodsThe chronic VaD mouse model was established, and WMLs were characterized by cerebral blood flow (CBF), behavioral tests, LFB staining, and immunohistochemistry. The anti-oxidative effect of GJ-4 was validated by examining biochemical parameters (SOD, MDA, and GSH) and the Keap1-Nrf2/HO-1 pathway. The impact of GJ-4 on lipid metabolism in WM was further investigated through lipidomic analysis. ResultsGJ-4 significantly attenuated cognitive impairments and improved the CBF of BCAS (bilateral common carotid artery stenosis)-induced mice. Mechanism research showed that GJ-4 could enhance cognition by promoting the repair of WMLs by inhibiting oxidative stress. Furthermore, GJ-4 treatment significantly reduced chronic cerebral hypoperfusion (CCH)-induced WMLs via improving lipid metabolism disorder in the WM. ConclusionThis research has provided valuable insights into the significance of WMLs in CCH-induced VaD and underscored the potential of GJ-4 as a therapeutic agent for improving cognitive function by targeting WMLs. These findings suggest that GJ-4 is a promising candidate for the treatment of VaD.

Exploring the anxiolytic mechanism of Fructus gardeniae based on metabolomics, network pharmacology, and molecular docking.

To explore the effect and anxiolytic mechanism of a natural remedy called Fructus gardeniae (FG). The elevated-plus maze (EPM) test was used to confirm the anxiolytic effect of FG. The potential and anxiolytic components, targets, and route processes of FG were investigated using the network pharmacology method in conjunction with metabolomics and molecular docking technologies. FG could greatly enhance the proportion of time and times of opening arms, according to the EPM data. As to the metabolomics findings, a total of 61 distinct metabolites were found, mainly involved in glycine, serine, and threonine metabolism as well as alanine, aspartate, and glutamate metabolism. The primary active ingredients of FG, nicotiflorin, jasminodiol, and crocetin, demonstrated substantial binding affinities with monoamine oxidase A (MAOA), monoamine oxidase A (ACHE), malate dehydrogenase 2 (MDH2), glutamate decarboxylase 2 (GAD2), glutamate decarboxylase 1 (GAD1), and nitric oxide synthase (NOS1), according to the findings of network pharmacology and molecular docking. FG exerts an anxiolytic action via targeting MAOA, ACHE, MDH2, GAD2, GAD1, and NOS1, and regulating the metabolism of glycine, serine, and threonine as well as alanine, aspartic acid, and glutamic acid.

Sub-chronic toxicity of the active fraction of a modified Huang-Lian-Jie-Du Decoction

A traditional Chinese herbal medicine formula named Huang-Lian-Jie-Du Decoction (HLJDD) has been used to cure various inflammatory diseases with a long history. However, one component of HLJDD Gardeniae fructus has remarkable liver and kidney toxicities. Therefore, it was altered with Dictamni cortex to form a modified HLJDD (MHLJDD). In this study, we aimed to evaluate the sub-chronic toxicity of the active fraction of MHLJDD (MHLJDD-F) in rats. Adult rats of both sexes were intragastrically administered with vehicle or MHLJDD-F (at the dose of 170, 340, and 680 mg/kg/day) once daily for 90 days. Half of the rats from each group were kept for an additional 30-day period to observe the drug withdrawal effect. The signs of toxicity and mortality of the rats were observed, and the body weight and food consumption were recorded. Blood was collected for hematological and biochemical analyses and major organs were weighed and harvested for histopathological examinations. The results revealed that no systemic toxicity of MHLJDD-F was found during the experiments. Organ coefficients and pathological alterations of major organs were comparable to the control rats. The no-observed adverse effect level (NOAEL) of MHLJDD-F was found up to 680 mg/kg/day. All these results demonstrated that long-term oral administration of MHLJDD-F did not cause significant toxicity, which is worthy to be widely applied as a new herbal medicine in pre-clinical and clinical studies.

Discrimination between raw and ginger juice processed Fructus Gardeniae based on UHPLC-Q-TOF-MS and Heracles NEO ultra-fast gas phase electronic nose.

Fructus Gardeniae (ZZ), a traditional Chinese herb, has been used in treating patients with jaundice, inflammation, etc. When mixed with ginger juice and stir-baked, ginger juice-processed Fructus Gardeniae (JZZ) is produced, and the chemical compositions in ZZ would be changed by adding the ginger juice. To illuminate the differential components between ZZ and JZZ. HPLC, UHPLC-Q-TOF-MS, and Heracles NEO ultra-fast gas phase electronic nose were applied to identify the differential components between ZZ and JZZ. HPLC fingerprints of ZZ and JZZ were established, and 24 common peaks were found. The content determination results showed that the contents of shanzhiside, geniposidic acid, genipin-1-β-D-gentiobioside and geniposide increased, while the contents of crocin I and crocin II decreased in JZZ. By UHPLC-Q-TOF-MS, twenty-six possible common components were inferred, among which 11 components were different. In further investigation, eight components were identified as the possible distinctive non-volatile compounds between ZZ and JZZ. By Heracles NEO ultra-fast gas phase electronic nose, four substances were inferred as the possible distinctive volatile compounds in JZZ. Shanzhiside, caffeic acid, genipin-1-β-D-gentiobioside, geniposide, rutin, crocin I, crocin II, and 4-Sinapoyl-5-caffeoylquinic acid were identified as the possible differential non-volatile components between ZZ and JZZ. Aniline, 3-methyl-3-sulfanylbutanol-1-ol, E-3-octen-2-one, and decyl propaonate were inferred as the possible distinctive volatile compounds in JZZ. This experiment explored a simple approach with objective and stable results, which would provide new ideas for studying decoction pieces with similar morphological appearance, especially those with different odors.

Predicting the Content of the Main Components of Gardeniae Fructus Praeparatus Based on Deep Learning

Predicting the Content of the Main Components of Gardeniae Fructus Praeparatus Based on Deep Learning

Inhibition of compound action potentials in the frog sciatic nerve by inchinkoto, a traditional Japanese medicine used for oral mucositis

ObjectiveThis study aimed to determine the effects of traditional Japanese (Kampo) medicines used to treat oral mucositis on nerve conduction. MethodsThe effects of Kampo medicines, crude drugs, and chemical compounds on compound action potentials (CAPs) were analyzed using extracellular recordings in frog sciatic nerves. ResultsAmong the Kampo medicines, inchinkoto demonstrated the most significant reduction in CAP amplitude, with a half-maximal inhibitory concentration (IC50) of 5.4 mg/mL. Hangeshashinto, shosaikoto, hochuekkito, and juzentaihoto also showed a significant reduction. Regarding inchinkoto, Artemisiae Capillari Spica (artemisia) was the most effective crude drug, with an IC50 of 4.2 mg/mL for CAP amplitude reduction, whereas Gardeniae Fructus (gardenia) exerted no significant effect. However, the combined use of artemisia and gardenia reduced the CAP amplitude more effectively than artemisia alone, indicating a synergistic interaction. The chemical ingredient eugenol from artemisia administered at 1 and 3 mmol/L reduced CAP amplitude, whereas other chemical ingredients administered at 0.1 and 1 mmol/L had no significant effects. ConclusionsInchinkoto exhibited the most effective reduction in CAP amplitude in the sciatic nerve of frogs, primarily through the action of artemisia, with potential synergistic interaction between artemisia and gardenia.

Comprehensive quality evaluation of different types of Gardeniae Fructus (Zhizi) and Shuizhizi based on LC-MS/MS.

Gardeniae Fructus (Zhizi) serves as both a medicinal and edible substance and finds widespread use in various industries. There are often two kinds of medicinal materials in the market: Zhizi and Shuizhizi. Typically, Zhizi with small, round fruit is used for medicinal purposes, while Shuizhizi, characterized by large, elongated fruit, is employed for dyeing. Market surveys have revealed a diverse range of Zhizi types, and modern research indicates that Shuizhizi contains rich chemical components and pharmacological activities. In this study, we collected 25 batches of Zhizi and Shuizhizi samples, categorizing them based on appearance into obovate and round fruits, with seven length grades (A-G). Using the ultra-high performance liquid chromatography coupled with triple quadrupole mass spectrometry (UHPLC-QQQ-MS/MS) method, we simultaneously quantified 13 main chemical components in fruits of Gardenia species. In addition, we compared the weight percentage of the pericarp, flesh, and seeds parts of samples with different traits, and quantified 13 chemical components in different parts. Results indicated that, aside from a few instances of overlapping fruit size ranges, Shuizhizi generally exhibits larger and longer dimensions than Zhizi. The weight proportion of the Shuizhizi pericarp is often higher than that of the Zhizi pericarp. Quantitative results highlighted significant differences in the chemical component content between Zhizi and Shuizhizi, with Shuizhizi generally containing higher levels of iridoids. The PCA and OPLS-DA analysis distinctly divided Shuizhizi and Zhizi, among which three iridoids, two organic acids, and one flavonoid made significant contributions to their classification. Cluster heatmap analysis also demonstrated complete separation between Zhizi and Shuizhizi, with clear distinctions among Zhizi samples from different origins. The distribution of the 13 chemical components in different Zhizi and Shuizhizi parts remained consistent, with iridoids and pigments concentrated in the seeds and flesh, and two organic acids and one flavonoid enriched in the pericarp. In summary, this study contributes valuable insights for classifying Zhizi and offers guidance on the rational use of Shuizhizi and the different parts of Zhizi.

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

Ethnopharmacological relevanceThe 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 studyThe 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 methodsWater 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. ResultsThe 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. ConclusionGeniposide exerts antipyretic effect in febrile rats through modulating the TLR4/NF-κB signaling pathway.

Effects of medicine food homologous materials on food allergy-associated factors: intestinal oxidative stress, intestinal inflammation and Th2 immune response.

Food allergies could be regulated via Th1/Th2 balance, intestinal oxidative stress and inflammation, which were considered as food allergy-associated factors. Medicine-food homologous materials (MFHM) were considered as a significant factor with respect to preventing human diseases. To evaluate the associations between MFHM and food allergy-associated factors, two types of MFHM with the remarkable function of anti-oxidation and anti-inflammation, Gardeniae fructus (Gar) and Sophorae glos (Sop), were chosen. By constructing an H2O2-induced oxidative stress model of Caco-2 cells and an intestinal inflammatory cell model of Caco-2 cells with tumor necrosis factor-α and interleukin (IL)-13, the contents of anti-oxidative enzymes (SOD and GSH), inflammatory factor (IL-8) and tight junction proteins (zonula occludens-1, occludin and claudin-1) in Caco-2 cells were determined. Moreover, the anti-allergic effects of digestive Sop and Gar were evaluated by measuring the levels of Th1/Th2/Treg cytokines in the spleen cells of sensitized mice. The results showed that the SOD and GSH were obviously increased and the gene and protein expression of IL-8 and claudin-1 were improved with the incubation of digested Sop. Th2 cytokine was reduced and Th1/Th2 balance was promoted on coincubation with ovalbumin (OVA) and digested Sop in the splenocytes. However, the digested Gar had no effect. The digested Sop not only had suppressive effects on intestinal oxidative stress and inflammation, but also had regulative effects on Th1/Th2 balance. This finding demonstrated that not all of the MFHM with anti-oxidant and anti-inflammatory effects have anti-allergic activities. The present study may be contributing toward establishing a screening model to identify the anti-allergic MFHM. © 2024 Society of Chemical Industry.

The growth performance, anti-oxidative capacity, immunity and resistance to heat stress of abalone Haliotis discus hannai can be improved by a mixture of herbs

An 84-day feeding trial was carried out to assess the effects of dietary Chinese herbs mixture (CHM) on the growth performance, anti-oxidative capacity, immunity and resistance to heat stress of abalone Haliotis discus hannai. The CHM included, Scutellariae Radix (Scutellaria baicalensis, Gardeniae Fructus (Gardenia jasminoides), Artemisiae Scopariae Herba (Artemisia capillaris), Uncariae Ramulus Cum Uncis (Uncaria rhynchophylla), Polygoni Cuspidati Rhizoma et Radix (Polygonum cuspidatum). Six diets containing 0.00% (control group), 0.02%, 0.04%, 0.06%, 0.08% and 0.10% of CHM were formulated and fed to abalone (initial weight: 3.59 ± 0.03 g). The group with 0.04% of dietary CHM exhibited the highest weight gain rate (WGR), while the survival was not significantly affected by dietary CHM. The optimal level of dietary CHM for abalone was determined to be 0.049% on the basis of the quadratic regression model for WGR. Dietary CHM significantly elevated the activities of lipase, trypsin, cellulase, Na+/K+-ATPase, acid phosphatase, alkaline phosphatase and lysozyme and total anti-oxidative capacity. Besides, dietary CHM significantly reduced the malondialdehyde content and alanine amino transferase activity. The mRNA levels of cationic amino acid transporter 1 (cat1) and nuclear factor erythroid 2-related factor 2 (nrf2) were significantly up-regulated in the group with 0.04% of dietary CHM. While the mRNA levels of kelch-like ECH-associated protein 1 (keap1), nuclear factor-κb (nf-κb) and tumor necrosis factor-α (tnf-α) were decreased in dietary CHM supplemented groups. The glucose and cortisol content in the CFH and the falling rate of abalone were significantly lower in the CHM supplemented groups than that in the control group. In conclusion, dietary supplementation of CHM improved the growth performance, anti-oxidative capacity, immunity and the resistance to heat stress of abalone. The recommended level of CHM supplemented in diets for abalone was 0.049%.

Genipin inhibits proliferation of gastric cancer cells by inducing ferroptosis: an integrated study of network pharmacology and bioinformatics study.

Ferroptosis has been demonstrated to suppress cancer development and is targeted for cancer therapy. Genipin, an iridoid constituent in Gardeniae Fructus, has been reported to exert anti-cancer abilities. However, whether genipin could induce ferroptosis remains unclear. The purpose of this study is to explore the anti-gastric cancer (GC) effects of genipin by inducing ferroptosis and to identify the potential targets. CCK-8 and colony formation assays were performed to evaluate the anti-GC effects of genipin. Flowcytometry and western blot were used to indicate ferroptosis-inducing ability of genipin. The potential targets of genipin were analyzed by network pharmacology, screened using UALCAN and KM-plotter database and evaluated by molecular docking. The results showed that genipin inhibited cell viability and proliferation of GC cells. Genipin treatment decreased levels of GPX4 and SLC7A11, induced accumulation of lipid peroxidation intracellularly and led to ferroptosis in GC cells. Network pharmacology analysis identified that lipid- and ROS-related pathways involved in ferroptosis ranked high among genipin-GC common targets. Data from UALCAN and KM-plotter database demonstrated that expression levels of ferroptosis-related targets, including AURKA, BCAT2, DHODH, and GPI, increased in GC tissues and the higher levels of the above four targets were related to tumor stage, tumor grade, and poor prognosis. Among these four targets, AURKA, BCAT2, and DHODH were confirmed by molecular docking with binding energies less than -5. Taken together, our study demonstrates that genipin could exert anti-GC ability by inducing ferroptosis and provides evidence for the potential application of genipin in GC treatment.

Transcriptional profiling of geniposide bioconversion into genipin during gardenia fructus extract fermentation by Lactobacillus (Lactiplantibacillus) plantarum SN13T.

Lactiplantibacillus plantarum SN13T is a probiotic plant-derived lactic acid bacterium that can grow in various medicinal plant extracts. In this study, we fermented an aqueous extract of gardenia fructus, the fruit of a medicinal plant, with SN13T, such that the bioactivity of the extract was potentiated after fermentation to suppress the release of inflammatory mediators, such as nitric oxide (NO), reactive oxygen species (ROS), interleukin-6 (IL-6), and tumor necrosis factor-alpha (TNF-α), as well as downregulate inflammatory genes in lipopolysaccharides (LPS)-stimulated RAW 264.7 cells. This increased antioxidant and anti-inflammatory activity was mediated through bioconversion of the iridoid glycoside geniposide to its aglycone genipin via the supposed hydrolytic action of β-glucosidases harbored by SN13T. In the complete genome of SN13T, ten putative genes encoding β-glucosidases of glycosyl hydrolase (GH) family 1 organized among eight gene operons were identified. Transcriptional profiling revealed that two 6-phospho-β-glucosidase genes, pbg9 and SN13T_1925, located adjacently in the gene operon SN13T_1923, were transcribed significantly more than the remaining genes during fermentation of the gardenia extract. This suggests the role of these β-glucosidases in bioconversion of geniposide to genipin and the subsequent enhanced bioactivity of the gardenia fructus extract after fermentation with SN13T.

Acute and 90-day toxicological safety assessment of Shang-Ke-Huang-Shui lotion in New Zealand White rabbits

Ethnopharmacological relevanceShang-Ke-Huang-Shui lotion (SKHS), an experiential formula based on the theory of traditional Chinese medicine as a hospital preparation, combines Coptidis Rhizoma, Phellodendri Chinensis Cortex, Gardeniae Fructus, Arnebiae Radix, Menthae Haplocalycis Herba and Alumen. While it has acquired positive effects on the treatment of soft tissue injuries, there is no systematic safety assessment in recent studies. Aim of the studyThe study aimed to investigate the acute and long-term toxicity in New Zealand White rabbits using topical administration of SKHS. Materials and methodsIn the acute toxicity study, rabbits were given topical administration of SKHS extract (2.775 g crude drug/mL) 3 times daily in normal and broken skin. In the long-term toxicity study, rabbits underwent topical administration of SKHS extract (1.390, 0.694, 0.139 g crude drug/mL) 1 time per day in normal and broken skin for 90 days. Their general behavior, body weight, food intake, biochemical and hematologic parameters, organ coefficients, and pathological morphology were analyzed. ResultsMild skin irritation was observed in rabbits with normal or broken skin following acute exposure to the high dose of SKHS. Evidence of toxicity was not observed in the rabbits exposed to SKHS for an extended period. Although some parameters have been significant changes, they cannot be considered treatment-related because they have remained within normal limits. ConclusionTopical administration of SKHS could be considered relatively safe and did not reveal any severe toxicity or side effects in this study.

Identification strategy of Fructus Gardeniae and its adulterant based on UHPLC/Q-orbitrap-MS and UHPLC-QTRAP-MS/MS combined with PLS regression model

Fructus Gardeniae (FG) is the desiccative and ripe fruits of Gardenia jasminoides Ellis in the Rubiaceae family, which is a commonly used in traditional Chinese medicine (TCM) for clearing away heat, detoxification, relieving restlessness, and eliminating blood stasis. At the same time, it has also been announced as the first batch of TCM with homology of medicine and food. Fructus Gardeniae Grandiflorae (FGG), the fruit of Gardenia jasminoides Ellis var. grandiflora Nakai (Rubiaceae), is a common counterfeit herbal medicine of FG, which still appears in the TCM market, and causes a certain degree of confusion. In order to effectively distinguish FG and its adulterant, the compounds in these two species were thoroughly characterized firstly by ultrahigh-performance liquid chromatography/quadrupole–orbitrap mass spectrometry (UHPLC/Q-Orbitrap MS). Furthermore, a pseudo-targeted metabonomics method with 60 targeted ion pairs was established based on UHPLC-triple quadrupole-linear ion trap mass spectrometry (UHPLC-QTRAP-MS) for discrimination. Multivariate statistical analysis showed that FG and FGG were clustered obviously, and 13 significantly differential markers were screened out by variable importance for projection (VIP) > 1 and p < 0.05 for the construction of the partial least squares (PLS) regression prediction model. The validation of the model proved that its prediction ability was quite satisfactory. Moreover, based on the absolute quantitative analysis of these 13 characteristics, the quality control standards of FG and FFG were established. In summary, an integral method of pseudo-targeted metabonomics combined with chemometrics analysis and a PLS regression model was proposed to provide an effective identification strategy for discrimination FG and FGG.

Preparative separation of iridoid glucosides and crocins from Gardeniae Fructus using sequential macroporous resin column chromatography and evaluation of their anti-inflammatory and antioxidant activities

Iridoid glycosides (geniposide (GP), genipin-1-gentiobioside (GB), etc.) and crocins (crocin Ⅰ (CR1), crocin Ⅱ(CR2), etc.) are two main bioactive components in Gardeniae Fructus (GF), which is a famous traditional Chinese medicine. Iridoid glycosides exhibit many activities and are used to manufacture gardenia blue pigment for the food industry. Crocins are rare natural water-soluble carotenoids that are often used as food colorants. A sequential macroporous resin column chromatography technology composed of HC-500B and HC-900B resins was developed to selectively separate iridoid glucosides and crocins from GF. The adsorption of GP on HC-900B resin was an exothermic process. The adsorption of CR1 on HC-500B resin was an endothermic process. The two kinds of components were completely separated by a sequential resin column. GB and GP were mainly found in product 1 (P1) with purities of 11.38% and 46.83%, respectively, while CR1 and CR2 were mainly found in product 2 (P2) with purities of 12.32% and 1.40%, respectively. The recovery yields of all the compounds were more than 80%. The above results showed that sequential resin column chromatography technology achieved high selectivity and recovery yields. GF extract, P1 and P2 could significantly inhibit the secretion of nitric oxide (NO), tumor necrosis factor α (TNF-α) and interleukin-6 (IL-6) in lipopolysaccharide (LPS)-induced RAW264.7 cells, indicating that iridoid glycosides and crocins provide a greater contribution to the anti-inflammatory activity of GF. At the same time, compared to the GF extract and P1, P2 exhibited stronger scavenging activities against 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2′-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radicals, indicating that crocins may provide a significant contribution to the antioxidant activity of GF.