• Journal of Applied Biological Chemistry
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• v.65 no.3
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• pp.231-237
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• 2022

Biorenovation is a method that converts existing compounds into new compounds through the enzymatic action of microorganisms. Biorenovation has expected effects such as reducing toxicity of compounds and increasing their activity. In this study, we successfully synthesized Luteolin-7-O-glucoside (L7G) through biorenovation and investigated its inhibitory effect on melanin production in α-Melanocyte stimulating hormone induced B16F10 mouse melanoma cells. We confirmed that Luteolin was toxic at 50, 100 and 200 µM, but our L7G in same concentration was not toxic for B16F10 mouse melanoma cells and also showed significant reduction in melanin production and tyrosinase activity. In addition, while investigating the effect of L7G on factors involved in melanin synthesis through western blotting, we were able to confirm that the MITF and tyrosinase protein synthesis was inhibited in treatment with L7G, however, tyrosinase related protein-1 (TRP-1) and dopachrome tautomerase (TRP-2) expression was not affected. So we derived a conclusion that through biorenovation we could produce compounds like L7G with improved activity and reduced toxicity for possible use as an active ingredient with whitening functionality in cosmetics.It also suggests that the application of biorenovation has potential usefulness in developing anti-inflammatory materials. It also suggests that the application of bio-renovation has potential usefulness in the development of inflammatory material. We applied Biorenovation technology to Distylium racemosum extract (DR) to generate Distylium racemosum biorenovation product (DRB), and investigated the anti-inflammatory properties of DRB in lipopolysaccharide (LPS)-treated RAW264.7 macrophages. We are applying technology to Biorenovation Distylium racemosum extract (DR) Distylium racemosum was to create a biorenovation product (DRB), lipopolysaccharide (LPS) investigated the anti-inflammatory properties of DRB in RAW264.7 macrophages treated for.

• Archives of Pharmacal Research
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• v.29 no.1
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• pp.67-72
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• 2006

The abnormal proliferation of aortic vascular smooth muscle cells (VSMCs) plays a central role in the pathogenesis of atherosclerosis and restenosis after angioplasty and possibly also in the development of hypertension. The present study was designed to examine the inhibitory effects and the mechanism of luteolin 7-glucoside (L7G) on the platelet-derived growth factor (PDGF)-BB-induced proliferation of VSMCs. L7G significantly inhibited the PDGF-BB-induced proliferation and the DNA synthesis of the VSMCs in a concentration-dependent manner. Pre-incubation of the VSMCs with L7G significantly inhibited the PDGF-BB-induced extracellular signal-regulated kinase 1/2 (ERK1/2), Akt and the phospholipase C $(PLC)-{\gamma}1$ activation. However, L7G had almost no affect on the phosphorylation of $PDGF-{\beta}$ receptor tyrosine kinase, which was induced by PDGF-BB. These results suggest that L7G inhibits the PDGF-BB-induced proliferation of VSMCs via the blocking of $(PLC)-{\gamma}1$, Akt, and ERK1/2 phosphorylation.

• Korean Journal of Food Science and Technology
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• v.53 no.3
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• pp.260-266
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• 2021

This study aimed to identify the hepatoprotective effects of a fermented Chrysanthemum indicum L. water extract. The extraction yield, antioxidant activities (ABTS and DPPH), and content of luteolin and luteolin-7-glucoside were significantly higher in the fermented C. indicum L. water extract (FCI) than in the C. indicum L. water extract. Treatment with FCI (200 ㎍/mL) significantly reduced the activities of gamma(γ)-glutamyl transferase, aspartate aminotransferase, alanine aminotransferase, and lactate dehydrogenase in HepG2 cells treated with 3% ethanol. Furthermore, FCI did not affect the viability of the HepG2 cells. These results suggest that FCI can be useful for the development of an effective hepatoprotective agent.

• Korean Journal of Food Science and Technology
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• v.31 no.3
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• pp.815-822
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• 1999

Twenty one flavonoids were isolated from ethyl acetate layer of aqueaus EtOH extracts of Artemisia vulgaris and identified as tricin, jaceosidine, eupafolin, diosmetin, chrysoeriol, homoeriodictyol, isorhamnetin, apigenin, eriodictyol, luteolin, luteolin 7-glucoside, kaempferol 3-glucoside, kaempferol 7-glucoside, kaempferol 3-rhamnoside, kaempferol 3-rutinside, quercetin, quercetin 3-glucoside, quercetin 3-galactoside, quercetrin, quercetin 7-glucoside, rutin, and vietexin. The inhibitory activity for all purified flavonoids were examined against lipid peroxidation in rat liver microsome. All examined flavonoids showed considerable antioxidant activity. Among them, $IC_{50}$ value of apigenin, luteolin, isorhamnetin, quercetin, and eriodictyol were showed higher than that of vitamin E used as positive control. And methoxylated flavonoids, tricin, eupafolin, jaceosidine, diosmetin, and isorhamnetin showed considerable antioxidant activity. Each $IC_{50}$ values were shown at 0.9, 1.0, 1.4, 1.0, and $0.7\;{\mu}g/mL$, respectively.

• Korean Journal of Pharmacognosy
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• v.38 no.3 s.150
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• pp.277-280
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• 2007

In our continuing effort to investigate compounds having anti-inflammatory activity from natural products, Ailanthus altissima was examined. Among six compounds isolated from Ailanthus altissima, Luteolin-7-O-glucoside (L7G) along with ethanol extract of Ailnathus altissima (EAa) were chosen to determine their inhibitory activity on secretory recombinant phospholipase $A_2s$ enzyme activity in vitro. As a results, EAa inhibited human recombinant $sPLA_2-V$ ($IC_{50}$ of about 100 ${\mu}g/ml$) and $cPLA_2$, ($IC_{50}$ of about 59 ${\mu}g/ml$), while L7G showed strong inhibitory effect on $sPLA_2-A$, V and $cPLA_2$ with an $IC_{50}$ value of approximately 40 ${\mu}M$, respectively.

• Natural Product Sciences
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• v.21 no.1
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• pp.42-48
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• 2015

Lactuca raddeana (Compositae) is used to treat obesity and complications due to diabetes. The five phenolic compounds including chlorogenic acid, chicoric acid, luteolin 7-O-glucoside, luteolin 7-O-glucuronide, luteolin were qualitatively identified by LC-ESI-MS analysis. The contents were quantitatively determined by HPLC, under the condition of a Capcell Pak C18 column ($5{\mu}m$, $250mm{\times}4.6mm\;i.d.$) and a gradient elution of 0.05% trifluoroacetic acid (TFA) and 0.05% TFA in $MeOH-H_2O$ (60 : 40). The contents of chicoric acid (100.99 mg/g extract) and luteolin 7-O-glucoside (101. 69 mg/g extract) were high, while those of other three phenolic substances were very low. The 3T3-L1 adipocyte cells treated with chicoric acid and luteolin 7-O-glucuronide significantly suppressed the accumulation of fat, suggesting they are effective against obesity. Since high level of peroxynitrite (ONOO) causes cardiovascular disease in obese patients, its scavenging activity was also studied.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.33 no.3
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• pp.139-144
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• 2007

In the previous study, we reported the antioxidative activity of Equisetum arvense extracts. In this study, its inhibitory effect on elastase and components were investigated. Aglycone fractions obtained from the deglycosylation reaction of ethylacetate fraction among the Equisetum arvense extracts, showed 4 bands and 4 peaks in TLC and HPLC experiments, respectively. Four components were identified as luteolin(composition ratio, 19.12%), quercetin(12.87), apigenin(15.81) and kaempferol(52.20). TLC chromatogram of ethylacetate fraction of Equisetum arvense extract revealed 7 bands and HPLC chromatogram showed 8 peaks, which were identified as kaempferol-3,7-O-diglucoside(composition ratio, 15.74%), luteolin-5-O-glucoside(galuteolin, 11.91), apigenin-5-O-glucoside(12.91), kaempferol-3-O-glucoside(astragalin, 27.94), quercetin-glycoside(10.81, structure was not determined), kaempferol-glycoside (12.33, structure was not determined), luteolin(3.72) and apigenin(4.62) in the order of elution time. The inhibitory effect of aglycone fraction on elastase($IC_{50}$, $9.8{\mu}g/mL$) was very high. But ethylacetate fraction(flavonoid glycosides) rarely exhibited the inhibitory activity on elastase. Combined with the previous results of the antioxidative activity of Equisetum arvense extracts, it is concluded that the inhibitory activity on elastase of the aglycone fraction could be applicable to new functional cosmetics for smoothing wrinkles.

• Natural Product Sciences
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• v.21 no.3
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• pp.155-161
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• 2015

Peroxynitrite (ONOO⁻)-scavenging activities of nine Compositae herbs consisting of three Ixeris, two Youngia, two Cirsium and one of each Lactuca and Taraxacum species were evaluated. The contents of their ONOO⁻ scavengers in the extracts were also determined on a HPLC using seven standard compounds, chlorogenic acid (CGA), chicoric acid (CA), luteolin 7-glucoside (luteolin-7-glc), luteolin 7-glucuronide (luteolin-7-glcU), luteolin, linarin and pectolinarin. Five of those compounds exhibited potent ONOO⁻-scavenging activities: IC₅₀, CA (0.76 μM), CGA (1.34 μM), luteolin (0.81 μM), luteolin-7-glc (0.86 μM) and luteolin-7-glcU (3.13 μM). Both CA and luteolin-7-glc were highly contained in I. dentata (19.71 mg/g and 13.58 mg/g, respectively), I. dentata var. albiflora (17.58 mg/g and 23.83 mg/g, respectively) and I. sonchifolia (65.71 mg/g and 6.99 mg/g, respectively). Among the nine herbs, those three Ixeris species had very low IC₅₀ values over the range of 0.48 - 1.74 μg/mL, suggesting that they could be potential therapeutic vegetables, particularly for preventing diabetic complications or obesity, which can be caused by an excess production of ONOO⁻.

• Natural Product Sciences
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• v.25 no.4
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• pp.326-333
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• 2019

The purpose of our study was to evaluate anti-AD potential of Cirsium maackii flowers. MeOH extract, CH₂Cl₂, EtOAc, and n-BuOH fraction of this flower notably inhibited BACE1 (IC₅₀ = 76.47 ± 1.66, 22.98 ± 1.45, 8.65 ± 0.63, and 72.47 ± 3.04 ㎍/mL, respectively). β-amyrenone (49.70 mg) (1), lupeol acetate (1.43 g) (2), lupeol (1.22 g) (3), lupenone (23.70 mg) (4), β-sitosterol (1.01 g) (6), and β-sitosterol glucoside (13.00 mg) (7) from CH₂Cl₂, apigenin (100.20 mg) (8), luteolin (19.00 mg) (9), apigenin 7-O-glucuronide methyl ester (21.30 mg) (14), and tracheloside (53.70 mg) (5) from EtOAc, apigenin 5-O-glucoside (11.00 mg) (10), luteolin 5-O-glucoside (11.00 mg) (11) and apigenin 7-O-glucuronide (91.00 mg) (12) from n-BuOH, and luteolin 7-O-glucuronide (22.00 mg) (13) from H₂O fraction were isolated. HPLC showed high levels of 8, 9 and 12 in MeOH extract (33.07 ± 0.07, 31. 44 ± 0.17 and 16.89 ± 0.33 mg/g, respectively), EtOAc (161.01 ± 1.78, 96.93 ± 0.34 and 73.38 ± 0.06 mg/g, respectively), and n-BuOH fraction (32.18 ± 0.33, 44.31 ± 0.32 and 105.94 ± 0.36 mg/g, respectively). Since, 3 and 9 are well-known BACE1 inhibitors, the anti-AD activity of C. maackii flower might be attributable to their presence.

• Proceedings of the Korean Society of Postharvest Science and Technology of Agricultural Products Conference
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• 2003.04a
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• pp.22-39
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• 2003

Biological activity of phenolic compounds in seeds and leaves of safflower (Carthamu tinctorius L.) were evaluated using several in vitro and in vivo assays. Six phenolic constituents were isolated from the seeds and identified as N-feruloylserotonia, N- (p-coumaroyl)serotonin, matairesinol, 8′-hydroxyarctigenin, acacetin 7-O-$\beta$-D-glucoside (tilianine) and acacetin. Six phenolic compounds exhibited considerable antioxidative activity, and especially two serotonins showed potent DPPH radical scavenging activity and antiperoxidative activity against rat liver microsomal lipid peroxidation induced by the hydroxyl radical generated via a Fenton-type reaction. Additionally, six phenolic compounds possessed comparable cytotoxicity against three cancer cells, Hela cell, MCF-7 and HepG2 cell, and particularly acacetin and its glycosides had the most potent cytotoxicity. Moreover, we found that feeding safflower seeds attenuated bone loss, and lowered levels of plasma and liver lipids in ovariectomized rats. Serotonins, lignans and flavones stimulated proliferation of the osteoblast-like cells in a dose-dependent manner (10$^{-15}$ ~10$^{-6}$ M), as potently as E$_2$ (17$\beta$-estradiol). Particularly, serotonins were mainly responsible for bone-protecting and lipid lowering effects in ovariectomized rats. Meanwhile, eight flavonoids, including a novel quercetin-7-O-(6"-O-acetyl)-$\beta$-D-glucopyranoside and seven kown flavonoids, luteolin quercetin, luteolin 7-O-$\beta$-D-glucopyranoside, luteolin-7-O-(6"-O-acetyl)-$\beta$-D-gluco-pyranoside, quercetin 7-O- -glucopyranoside, acacetin 7-O-$\beta$-D-glucuronide and apigenin-6-C-$\beta$-D-glucopyranosyl-8-C-$\beta$-D-glucopyranoside were first isolated and identified from safflower leaf. Among these flavonoids, luteolin-acetyl-glucoside and $\beta$quercetin- acetyl-glucoside showed potent antioxidative activities against 2-deoxyribose degradation and lipid peroxidation in rat liver microsomes. Luteolin, quercetin and their corresponding glycosides also exhibited strong antioxidative activity, while acacetin glucuronide and apigenin-6, 8-di-C-glucoside were relatively less active. Finally, changes in phenolic compositions were also determined by HPLC in the safflower seed and leaf during growth stages and roasting process to produce standardized supplement powerds. These results suggest that phenolic compounds in the roasted safflower seed and leaf may be useful as potential sources of therapeutic agents against several pathological disorders such as carcinogenesis, atherosclerosis and osteoporosis.