• Food Science and Biotechnology
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• v.17 no.6
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• pp.1165-1170
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• 2008

The deposition of the amyloid $\beta}$ ($A{\beta}$)-peptide following proteolytic processing of amyloid precursor protein (APP) by $\beta$-secretase (BACE1) and $\gamma$-secretase is critical feature in the progress of Alzheimer's disease (AD). Consequently, BACE1, a key enzyme in the production of $A{\beta}$, is a prime target for therapeutic intervention in AD. In the course of searching for BACE1 inhibitors from natural sources, the ethyl acetate fraction of Petasites japonicus showed potent inhibitory activity. Two BACE1 inhibitors quercetin (QC) and kaempferol 3-O-(6"-acetyl)-$\beta$-glucopyranoside (KAG) were isolated from P. japonicus by activity-guided purification. QC, in particular, non-competitively attenuated BACE1 activity with $IC_{50}$ value of $2.1{\times}10^{-6}\;M$ and $K_i$ value of $3.7{\times}10^{-6}\;M$. Both compounds exhibited less inhibition of $\alpha$-secreatase (TACE) and other serine proteases including chymotrypsin, trypsin, and elastase, suggesting that they ere relatively specific and selective inhibitors to BACE1. Furthermore, both compounds significantly reduced the extracellular $A{\beta}$ secretion in $APP_{695}$-transfected B103 cells.

• Food Science and Biotechnology
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• v.17 no.6
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• pp.1361-1364
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• 2008

The inhibitory effects of naringenin, kaempherol, and apigenin on the production of cholesterol in HepG2 KCLB 88065 and MCF-7 KCLB 30022 cells were evaluated. In this study, quercetin was used as a reference reagent. After incubation for 3 days, fat-soluble contents of both cell types were extracted by using the Folch method and the cholesterol contents in both cultured cells were determined by high performance liquid chromatography. The concentration of cholesterol in untreated each tissue cells was $12.2{\pm}0.11$ and $8.83{\pm}0.12\;mg/g$ of lipid, respectively. The total concentration of each flavonoid was adjusted to 0, 35, or $350{\mu}M$ in the culture broth. As the results, the addition of 2% methanol and dimethyl sulfoxide (DMSO) to the media (control for flavonoid solvents) did not significantly affect cell growth; however, DMSO caused an increase in the production of cholesterol. Each flavonoid inhibited the production of cholesterol in both HepG2 and MCF-7 cells at the concentration of $35{\mu}M$ above. In addition, the inhibitory effect of kaempherol on the production of cholesterol in these cells was greater than the other flavonoids tested and HepG2 cells are more sensitive to flavonoids than MCF-7. From the results, the inhibitory effects of flavonoids on cholesterol production are different depending on the cell type.

• Plant Breeding and Biotechnology
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• v.5 no.3
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• pp.192-203
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• 2017

Metabolite profile is a powerful analytical technique to identify the functional characterization of plants. In this study, the phytochemicals and secondary metabolites of lentils (Lens culinaris) were analyzed to compare the anti-oxidative activities according to the different colors. The polar metabolites, fatty acids, carotenoids, flavonoids, anthocyanins, total phenolic acids, DPPH activity were analyzed. Three kind of lentils, French green whole lentil (FG), red whole lentil (LR), and green whole lentil (LG) (ASIA SEED Co., LTD), were used for this study. Fatty acids, phytochemicals, and antioxidative components from each lentil varieties were analyzed by official methods. The contents of lutein in carotenoids were 6-9 times higher than zeaxanthin in all lentils, but were not significantly different among three varieties. The content of carotenoids in FG was lower significantly than those in the LR and LG. Myricetin and luteolin were detected in the only FG. Kaempferol and delphinidin were significantly highest in the FG. Most of the phenolic acids except coumarate were higher in FG and LG than in LR. Also antioxidant effects ($EC_{50}$) were higher in FG and LG than in LR. The analyzed metabolites obtained from lentils showed distinct separation in the PCA results according to the varieties. Also, lentils showed different anti-oxidant profiles according to the colors. FG and LG showing higher contents of phytochemicals showed higher antioxidative activity than LG containing relative low contents of phytochemicals.

• Journal of Ginseng Research
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• v.46 no.6
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• pp.790-800
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• 2022

Background: Panax ginseng Meyer is one of the most valuable medicinal plants which is enriched in anti-microbe secondary metabolites and widely used in traditional medicine. Botrytis cinerea is a necrotrophic fungus that causes gray mold disease in a broad range of hosts. B. cinerea could overcome the ginseng defense and cause serious leaf and root diseases with unknown mechanism. Methods: We conducted simultaneous transcriptomic and metabolomic analysis of the host to investigate the defense response of ginseng affected by B. cinerea. The gene deletion and replacement were then performed to study the pathogenic gene in B. cinerea during ginseng - fungi interaction. Results: Upon B. cinerea infection, ginseng defense responses were switched from the activation to repression, thus the expression of many defense genes decreased and the biosynthesis of antifungal metabolites were reduced. Particularly, ginseng metabolites like kaempferol, quercetin and luteolin which could inhibit fungi growth were decreased after B. cinerea infection. B. cinerea quercetin dioxygenase (Qdo) involved in catalyzing flavonoids degradation and ∆BcQdo mutants showed increased substrates accumulation and reduced disease development. Conclusion: This work indicates the flavonoids play a role in ginseng defense and BcQdo involves in B. cinerea virulence towards the P. ginseng. B. cinerea promotes disease development in ginseng by suppressing of defense related genes expression and reduction of antifungal metabolites biosynthesis.

• Genomics & Informatics
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• v.19 no.4
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• pp.46.1-46.11
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• 2021

Moringa oleifera is nowadays raising as the most preferred medicinal plant, as every part of the moringa plant has potential bioactive compounds which can be used as herbal medicines. Some bioactive compounds of M. oleifera possess potential anti-cancer properties which interact with the apoptosis protein p53 in cancer cell lines of oral squamous cell carcinoma. This research work focuses on the interaction among the selected bioactive compounds derived from M. oleifera with targeted apoptosis protein p53 from the apoptosis pathway to check whether the bioactive compound will induce apoptosis after the mutation in p53. To check the toxicity and drug-likeness of the selected bioactive compound derived from M. oleifera based on Lipinski's Rule of Five. Detailed analysis of the 3D structure of apoptosis protein p53. To analyze protein's active site by CASTp 3.0 server. Molecular docking and binding affinity were analyzed between protein p53 with selected bioactive compounds in order to find the most potential inhibitor against the target. This study shows the docking between the potential bioactive compounds with targeted apoptosis protein p53. Quercetin was the most potential bioactive compound whereas kaempferol shows poor affinity towards the targeted p53 protein in the apoptosis pathway. Thus, the objective of this research can provide an insight prediction towards M. oleifera derived bioactive compounds and target apoptosis protein p53 in the structural analysis for compound isolation and in-vivo experiments on the cancer cell line.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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• v.36 no.1
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• pp.50-63
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• 2023

Objectives : This study used a network pharmacology approach to explore the active compounds and therapeutic mechanisms of Yijin-tang on Meniere's disease. Methods : The active compounds of Yijin-tang were screened via the TCMSP database and their target proteins were screened via the STITCH database. The GeneCard was used to establish the Meniere's disease-related genes. The intersection targets were obtained through Venny 2.1.0. The related protein interaction network was constructed with the STRING database, and topology analysis was performed through CytoNCA. GO biological function analysis and KEGG enrichment analysis for core targets were performed through the ClueGO. Results : Network analysis identified 126 compounds in five herbal medicines of Yijin-tang. Among them, 15 compounds(naringenin, beta-sitosterol, stigmasterol, baicalein, baicalin, calycosin, dihydrocapsaicin, formononetin, glabridin, isorhamnetin, kaempferol, mairin, quercetin, sitosterol, nobiletin) were the key chemicals. The target proteins were 119, and 7 proteins(TNF, CASP9, PARP1, CCL2, CFTR, NOS2, NOS1) were linked to Meniere's disease-related genes. Core genes in this network were TNF, CASP9, and NOS2. GO/KEGG pathway analysis results indicate that these targets are primarily involved in regulating biological processes, such as excitotoxicity, oxidative stress, and apoptosis. Conclusion : Pharmacological network analysis can help to explain the applicability of Yijin-tang on Meniere's disease.

• The Korea Journal of Herbology
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• v.32 no.2
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• pp.65-75
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• 2017

Objectives : This study aimed to evaluate the protective effect of Orostachydis Herba (OH) and Fermented OH (OHF) against the acute liver injury by lipopolysaccharide (LPS). Methods : OHF by 4 lactic bacteria such as (Lactobacillus hilgardii (OHF1), Leuconostoc mesenteroides (OHF2), Pediococcus acidilactici (OHF3), Saccharomyces cerevisiae (OHF4)) were prepared. Samples were selected to OHF0, OHF2, OHF3 based on UPLC analysis, DPPH, ABTS radical scavenging activities. To evaluate the protective effect of OHF on liver injury mice, ICR mice were divided into 5 groups: Normal mice (Nor), LPS (20 mg/kg) treated mice (Veh), administrated OHF0, OHF2 OHF3 200 mg/kg body weight during 8 days before LPS injection. Serum and liver were collected 24 hours after LPS injection. Results : The activity was high in order of OHF0 and OHF3 in DPPH and ABTS radical scavenging activities. The quercetin contents for bioactive ingredient of OH was 5.39, kaempferol contents was 9.94 by UPLC analysis. The LPS-treated vehicle group significantly increased liver weight, and aspartate aminotransferase (AST) and alanine aminotransferase (ALT) levels in serum. In contrast, administrated OHF3 group decreased liver weight, AST, ALT. In addition, OHF3 groups reduced the elevated levels of reactive oxygen species (ROS) in serum and tissues. Moreover, AP-1, iNOS and COX-2 were significantly decreased in OHF2 and OHF3. But $NF-{\kappa}B$ p65 and $TNF-{\alpha}$ only showed a significant reduction in OHF3. Conclusions : Therefore, these results suggest that fermented Orostachydis Herba might be protective effect on liver injury through anti-oxidant effect.

• Journal of the Korean Chemical Society
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• v.67 no.2
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• pp.120-128
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• 2023

Osteoporosis is a disease that causes the weakening of bone by increasing porosity, which often results in fractures. Osteoporosis treatment measures include the use of Bisphosphonates and estrogen. However, these treatments cannot be used in the long term as these treatments have adverse side effects. Therefore, there is a need to identify better and safer treatment options. For this, 63 plant extracts were screened and among them, six extracts showed high anti-osteoclastic activity with low cytotoxicity. Of these six extracts, three extracts, Cudrania tricuspidata (P371), Ulmus davidiana var. japonica (P401), and Torilis japonica (P411), showed more than 50 percent osteoclast inhibition. While the remaining, Stewartia pseudocamellia extracts I and II (P370, P397) and Cuscuta chinensis (P418), showed moderate or between 40-50 percent osteoclast inhibition. Among all the extracts, Torilis japonica (P411) showed the highest inhibitory action against osteoclast development. Torilis japonica (P411) primary components include Kaempferol, Quercetin, and Luteolin, all proven to inhibit osteoclastogenesis. Stewartia pseudocamellia extracts I and II (P370 and P397) showed moderate or 44% osteoclast inhibition. Stewartia pseudocamellia extract II (P397) enhanced the growth of RAW 264.7 cells by 19%. Torilis japonica (P411) and Stewartia pseudocamellia extract II (P397) suppressed the expression of osteoclast-specific genes in RANKL-induced osteoclastogenesis in RAW 246.7 cells. Torilis japonica (P411) extracts even increased osteoblast-specific RUNX2 gene expression. This results provide that six extracts could be used as a potential treatment option for osteoporosis disease with the extracts of Torilis japonica (P411) and Stewartia pseudocamellia (P397) as an ideal candidates. However, the combination of the extract with higher osteoclastic inhibition and less toxic effects with further analysis should be recommended.

• Proceedings of the Plant Resources Society of Korea Conference
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• 2023.04a
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• pp.64-64
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• 2023

콩은 중요한 식량 작물로 단백질, 기름 및 이차대사산물인 이소플라본을 다량으로 함유하고 있다. 이소플라본은 폴리페놀의 일종으로 일부 암을 예방하며 심혈관 질환을 완화하는 데에도 도움을 준다고 알려져 있다. 콩에 인위적으로 식물호르몬인 ABA를 처리할 때 이차대사산물인 kaempferol의 함량이 증가한다고 보고 되었다. 따라서 이 연구는 식물 생장조정제 처리가 콩잎의 이소플라본 함량에 미치는 영향을 알아보기 위해 수행되었다. 연구는 밀양 남부작물부 유리온실에서 수행되었으며, 콩(품종:선풍)은 와그너포트 1/2000에 1주 2본 파종하여 재배하였다. Ethephone(500, 1000, 2000 ppm)과 ABA(100, 200, 400 ppm)를 사용하였으며 각각 R2, R5, R7기에 처리하였다. 처리 후 잎을 5일 간격으로 3회 채취하여 이소플라본 6종과 쿠메스트롤의 함량을 분석하였다. 초고성능 액체 크로마토그래피(Acquity UPLC H-Class system, Waters)를 사용하여 분석하였다. 이소플라본 함량은 R5 단계에서 전반적으로 높게 나타났으며, R2 및 R7 단계에서는 무처리와 유사한 수준을 보였다. ABA를 처리하였을 때 생장조정제 간의 차이가 에테폰보다 더 큰 것으로 나타났다. 쿠메스트롤 함량은 처리시간에 따라 R7, R5, R2 순으로 높은 것으로 확인되었으며, 처리시간이 지날수록 함량이 증가함을 알 수 있었다. 생장조정제 처리에 쿠메스트롤 함량은 ABA보다 에세폰 처리 시 더 높은 경향을 보였다.

• Parasites, Hosts and Diseases
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• v.61 no.4
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• pp.449-454
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• 2023

Free-living amoebae (FLA) rarely cause human infections but can invoke fatal infections in the central nervous system (CNS). No consensus treatment has been established for FLA infections of the CNS, emphasizing the urgent need to discover or develop safe and effective drugs. Flavonoids, natural compounds from plants and plant-derived products, are known to have antiprotozoan activities against several pathogenic protozoa parasites. The anti-FLA activity of flavonoids has also been proposed, while their antiamoebic activity for FLA needs to be emperically determined. We herein evaluated the antiamoebic activities of 18 flavonoids against Naegleria fowleri and Acanthamoeba species which included A. castellanii and A. polyphaga. These flavonoids showed different profiles of antiamoebic activity against N. fowleri and Acanthamoeba species. Demethoxycurcumin, kaempferol, resveratrol, and silybin (A+B) showed in vitro antiamoebic activity against both N. fowleri and Acanthamoeba species. Apigenin, costunolide, (-)-epicatechin, (-)-epigallocatechin, rosmarinic acid, and (-)-trans-caryophyllene showed selective antiamoebic activity for Acanthamoeba species. Luteolin was more effective for N. fowleri. However, afzelin, berberine, (±)-catechin, chelerythrine, genistein, (+)-pinostrobin, and quercetin did not exhibit antiamoebic activity against the amoeba species. They neither showed selective antiamoebic activity with significant cytotoxicity to C6 glial cells. Our results provide a basis for the anti-FLA activity of flavonoids, which can be applied to develope alternative or supplemental therapeutic agents for FLA infections of the CNS.