• Biomolecules & Therapeutics
• /
• v.24 no.2
• /
• pp.156-162
• /
• 2016

Iridoid glycosides (mainly geniposide) and crocetin derivatives (crocins) are the two major active constituents in Gardenia jasminoides Ellis. In the present study, geniposide, crocins, crocin-1 and crocetin were separated from gardenia chromatographically. Then, mice were orally administrated with geniposide (400 mg/kg b.w.), crocins (400 mg/kg b.w.), crocin-1 (400 mg/kg b.w.) and crocetin (140 mg/kg b.w.) once daily for 7 days with $CCl_4$. Hepatoprotective properties were evaluated by biochemical parameters: Administration of geniposide, crocins, crocin-1and crocetin significantly lowered serum alanine transaminase (ALT), aspartate transaminase (AST) and alkaline phosphatase (ALP) levels in $CCl_4$-treated mice. The reduced glutathione (GSH) levels and antioxidant enzymes (SOD and CAT) activities were also increased by geniposide, crocins, crocin-1 and crocetin. Histopathological examination of livers showed that these components reduced deformability, irregular arrangement and rupture of hepatocyte in $CCl_4$-treated mice. These biochemical results and liver histopathological assessment demonstrated that geniposide, crocetin derivatives and crocetin show comparative beneficial effects on $CCl_4$-induced liver damage via induction of antioxidant defense. Therefore, contents of geniposide and crocetin derivatives should be both considered for hepatoprotective efficacy of Gardenia jasminoides Ellis.

• Natural Product Sciences
• /
• v.19 no.3
• /
• pp.206-214
• /
• 2013

The crocetin derivatives, crocin (1), gentiobiosyl glucosyl crocetin (3), and mono-gentiobiosyl crocetin (4) were isolated from the fruit of Gardenia jasminoides (Gj) and crocetin (2) from the processed fruit of Gj (PGj) by column chromatography. Their structures were determined on the basis of spectroscopic methods including IR, MS, and NMR (1D and 2D). These compounds were evaluated for their inhibition activity on melanin production in ${\alpha}$-MSH (melanocyte stimulating hormone) activated B16F10 cells. Compounds 1 - 4 reduced melanin content in a dose-dependent manner at concentrations of 20 - 60 uM. They also suppressed tyrosinase protein and m-RNA expressions dose dependently, assayed by western blot analysis, and RT-PCR experiment in B16F10 murine melanoma cells.

• Korean Journal of Food Science and Technology
• /
• v.31 no.5
• /
• pp.1184-1187
• /
• 1999

The Gardenia jasminoides yellow pigment and converted pigments were completely separated by Amberlite XAD-4 column chromatography. These Pigments were gel filtrated on Sephadex LH-20 column chromatography. The characteristics of absorption spectra of eluate and fractionated pigments were investigated. The pigment converted by Lactobacillus plantarum showed a single blue color with an absorption peak at 588 nm and its molecular size was bigger than that of crocetin. The pigment, converted by Staphylococcus epidermidis, Showed blue-green color, which was composed of yellow color with an absorption peak at 418 nm and blue color at 588 nm. Molecular size of the yellow pigment was smaller than crocetin and that of blue color.

• Korean Journal of Food Science and Technology
• /
• v.31 no.4
• /
• pp.945-951
• /
• 1999

A simple and practical method for the determination of gardenia yellow in foods was developed. In this method, analysis of gardenia yellow in food products has been carried out by the detection of crocetin and/or geniposide as indicator compounds. As a new analytical method for gardenia yellow, we adopted crocetin, which is produced from colored components of gardenia yellow by alkaline hydrolysis, as an indicator compound. The analysis of gardenia yellow was performed by reverse phase high performance liquid chromatography using a Capcell pak $C_{18}$ column at wave length 240 nm (geniposide) and 435 nm (crocetin). The recovery rates of geniposide and crocetin were found to be 93.4% and 87.8% for Dan Mu Ji, 90.2% and 85.9% for milk, 92.8% and 86.5% for snack, respectively. With this method, the range of crocetin and geniposide contents $({\mu}g/g)$ were as follows: $ND{\sim}1.7$ and $ND{\sim}14.1$ for Dan Mu Ji, $ND{\sim}0.2$ and $ND{\sim}13.6$ for milk, $ND{\sim}1.6$ and $ND{\sim}0.9$ for snack, respectively. The detection limits of crocetin and geniposide were 0.07 ${\mu}g/g$ and 0.05 ${\mu}g/g$, respectively.

• Asian Pacific Journal of Cancer Prevention
• /
• v.13 no.8
• /
• pp.3757-3761
• /
• 2012

Objective: Crocin has been proposed as a promising candidate for cancer chemoprevention. The purpose of this investigation was to investigate the chemopreventive action and the possible mechanisms of crocin against human colon cancer cells in vitro. Methods: Cell proliferation was examined using MTT assay and the cell cycle distribution fractions were analyzed using fow cytometric analysis after propidium iodide staining. Apoptosis was detected using theTUNEL Apoptosis Detection Kit with laser scanning confocal microscope. DNA damage was assessed using the alkaline single-cell gel electrophoresis assay, while expression levels of p53, cdk2, cyclinA and P21 were examined by Western blot analysis. Results: Treatment of SW480 cells with crocetin (0.2, 0.4, 0.8 mmol/L) for 48 h signifcantly inhibited their proliferation in a concentration-dependent manner. Crocetin (0.8 mmol/L) signifcantly induced cell cycle arrest through p53-independent mechanisms accompanied by P21 induction. Crocetin (0.8 mmol/L) caused cytotoxicity in the SW480 cells by enhancing apoptosis and decreasing DNA repair capacity in a time-dependent manner. Conclusions: This report provides evidence that crocetin is a potential anticancer agent, which may be used as a chemotherapeutic drug.

• Asian Pacific Journal of Cancer Prevention
• /
• v.13 no.11
• /
• pp.5605-5611
• /
• 2012

Background: In the last two decades, pioneering research on anti-tumour activity of saffron has shed light on the role of crocetin, picrocrocin and safranal, as broad spectrum anti-neoplastic agents. However, the exact mechanisms have yet to be elucidated. Identification and characterization of the targets of bioactive constituents will play an imperative role in demystifying the complex anti-neoplastic machinery. Methods: In the quest of potential target identification, a dual virtual screening approach utilizing two inverse screening systems, one predicated on idTarget and the other on PharmMapper was here employed. A set of target proteins associated with multiple forms of cancer and ranked by Fit Score and Binding energy were obtained from the two independent inverse screening platforms. The validity of the results was checked by meticulously analyzing the post-docking binding pose of the picrocrocin with Hsp90 alpha in AutoDock. Results: The docking pose reveals that electrostatic and hydrogen bonds play the key role in inter-molecular interactions in ligand binding. Picrocrocin binds to the Hsp90 alpha with a definite orientation appropriate for nucleophilic attacks by several electrical residues inside the Hsp90-alpha ATPase catalytic site. Conclusion: This study reveals functional information about the anti-tumor mechanism of saffron bioactive constituents. Also, a tractable set of anti-neoplastic targets for saffron has been generated in this study which can be further authenticated by in vivo and in vitro experiments.

• Journal of Life Science
• /
• v.34 no.2
• /
• pp.138-144
• /
• 2024

Crocin is a major carotenoid of the Gardenia jasminoides fruit and Crocus sativus stigma (saffron), which are used in various cuisines as flavoring and coloring agents, as well as in phytomedicine for the treatment of several disorders, including headache, fever, edema, fatty liver, viral hepatitis, respiratory disease, menstruation disorders, insomnia, and hypertension. Crocin (C₄₄H₆₄O₂₄) is a chemical diester composed of the dicarboxylic acid crocetin and disaccharide gentiobiose. Many in vitro and in vivo studies have been conducted about the biological and pharmacological function and toxicity of crocin. Crocin has been revealed to have no genotoxicity and pathological manifestation. Crocin acts as an antioxidant, anti-cancer, memory enhancer, anxiolytic, antidepressant, aphrodisiac, anti-atherosclerotic, cardioprotector, and hepatoprotector. Here, an inclusive review of crocin is introduced based on previously explored studies referred to in the literature. Different studies have confirmed the protective role of crocin in the pathogenesis of inflammatory diseases, including inflammatory bowel diseases, gastritis, asthma, atherosclerosis, rheumatoid arthritis, multiple sclerosis, type 1 diabetes, Alzheimer's disease, Parkinson's disease, and depression. It is surmised that crocin suppresses inflammatory, antioxidant, and apoptotic processes through multiple mechanisms. Crocin is considered a safe and effective therapeutic choice for patients with inflammatory conditions, although more research investigating its mechanisms and results acquired in clinical trials are needed.

• Journal of Microbiology and Biotechnology
• /
• v.16 no.7
• /
• pp.1084-1089
• /
• 2006

The fructus of Gardenia jasminoides Ellis (GF) has been widely used as a natural colorant in Asian countries, and also as a Chinese traditional medicine for its homeostatic, antiphlogistic, analgesic, and antipyretic effects. In the present study, its main component, crocin, was fermented with lactic acid bacteria (LAB) and their antihyperlipidemic activity was measured. The GF extract, fermented GF (F-GF), crocin, and fermented crocin (F-crocin) significantly inhibited the increase of serum triglyceride (TG) level in corn oil feeding-induced triglyceridemic mice, as well as that of serum TG and total and LDL cholesterol levels in Triton WR-1339-induced hyperlipidemic mice. These agents also showed hypolipidemic activity in hyperlipidemic mice induced by high fat diet for 5 weeks. F-GF and F-crocin exhibited more potent hyperlipidemic effects than GF and crocin. The results suggest that the hypolipidemic effect of GF and crocin can be synergistically activated by LAB, and that F-GF and F-crocin may improve hyperlipidemia in clinic, compared with GF and crocin.

• Journal of Microbiology and Biotechnology
• /
• v.18 no.6
• /
• pp.1109-1114
• /
• 2008

To understand the role of intestinal microflora in the biological effect of functional herbs, which have been used in Korea, Japan, and China as traditional medicines, and suggest new bioactive compounds transformed from herbal constituents, the metabolic activities of the functional herb components (ginsenoside Rb1, crocin, amygdalin, geniposide, puerarin, ginsenoside Re, poncirin, hesperidin, glycyrrhizin, and baicalin) toward their bioactive compounds (compound K, crocetin, benzaldehyde, genipin, daidzein, ginsenoside Rh1, ponciretin, hesperetin, 18b-glycyrrhetic acid, and baicalein) were measured in fecal specimens. The metabolic activities of these components were $882.7{\pm}814.5$, $3,938.1{\pm}2,700.8$, $2,375.5{\pm}913.7$, $1,179.4{\pm}795.7$, $24.6{\pm}10.5$, $11.4{\pm}10.8$, $578.8{\pm}206.1$, $1,150.0{\pm}266.1$, $47.3{\pm}58.6$, and $12,253.0{\pm}6,527.6\;{\mu}mol/h/g$, respectively. No differences were found in the metabolic activities of the tested components between males and females, although these metabolic activities between individuals are extensively different. The metabolites of functional herb components showed more potent cytotoxicity against tumor cells than nonmetabolites. These findings suggest that intestinal microflora may activate the pharmacological effect of herbal food and medicines and must be the biocatalytic converter for the transformation of herbal components to bioactive compounds.

• Journal of the Korean Applied Science and Technology
• /
• v.34 no.1
• /
• pp.163-172
• /
• 2017

The purpose of this study was to measure the bioactivity and antioxidant activity of peel from Gardenia jasminoides Ellis fructus (GJE). GJE have been known to contain functional materials such as crocin, crocetin, geniposide, gardenosid, geniposidic acid, iridoid glycosides etc. We were separated into GJE peel. After that, we determined proanthocyanidin. GJE peel were extracted by 70% methanol, ethyl acetate (EA) and distilled water (DW) of three solvents. To investigate by the solvent extract of flavonoid content and value as a functional food ingredient of GJE peel through antioxidant activities (DPPH radical scavenging activity, ABTS radical scavenging activity, superoxide dismutase like ability, hydroxyl radical scavenging activity, ferrous ion-chelating capacity) were performed. Solvent extract antioxidant activity of increasing concentrations (0.2, 0.4, 0.6 mg/mL) were significantly increased (p<0.05). GJE peel extracts showed lower activity than positive control (ascorbic acid, BHA, EDTA). These results, by a solvent of peel were found that the relationship with the increase of flavonoid content increased physiological activity. The antioxidant activity of the extract from the other except for the EA extract on peel was observed at a high level. The results suggest that GJE peel can be used as nutraceutical foods and natural antioxidant.