• Title/Summary/Keyword: Active Ingredient

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Antioxidant and Anti-inflammatory Effects of Fermented Blackcurrant Fruit Extracts with Saccharomycopsis fibuligera (Saccharomycopsis fibuligera로 발효된 블랙커런트추출물의 항산화 및 항염증 효과)

  • Jang, Jun-Hwan;Lee, Hyung-Kyu;Bae, Jun-Tae;Lee, Jae-Seob;Hwang, Bang-Yeon
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.46 no.4
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    • pp.403-413
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    • 2020
  • While searching for useful microorganisms, Saccharomycopsis fibuligera which can be used as cosmetic materials were divided from Jeju island's traditional fermented foods. In this study, blackcurrant extract which contains a large amount of anthocyanin glycosides was fermented with S. fibuligera. HPLC analysis was performed to analyze the components of blackcurrant extract (BE) and fermented blackcurrant fruit extract (FBE). As a result, bio-conversion of delphinidin and cyanidin were able to be identified. In order to verify the anti-oxidant effect of BE and FBE, we investigated radical scavenging ability with DPPH and ABTS. In addition, to confirm anti-inflammatory effect, we investigated inhibition effect of nitric oxide (NO) production on lipopolysaccharide (LPS) - stimulated RAW264.7 macrophages, and inhibition effect of the expression of inflammatory-related proteins (iNOS, COX-2) by western blot analysis. As a result, as FBE has anti-oxidant and anti-inflammatory effects, we suggest that it might be used as an active ingredient for cosmetics.

Dermal Papilla Cells Proliferation Constituent of Schisandra chinensis Fruits and Optimization Using Response Surface Methodology (오미자의 모유두세포 증식 활성성분과 반응표면분석을 이용한 추출조건의 최적화)

  • Cho, Hyun Dae;Jeong, JiYeon;Ryu, Hwa Sun;Lee, JungNo;Park, Sung-Min
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.46 no.4
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    • pp.415-424
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    • 2020
  • In the present study, we have refined gomisin N, which represents activity in the proliferation of dermal papilla cells (HFDPCs) from the fruit of Schisandra chinensis (S. chinensis), and have identified optimal extraction conditions for obtaining extracts with high content of gomisin N. The activity of the extracts and fractions was evaluated, and the results indicated approximately 29% proliferation activity in the group treated with 1 ㎍/mL of n-hexane fraction. Column chromatography was used to assess the active ingredient in the n-hexane fraction, and two compounds, namely gomisin N(1) and schisandrin(2), were isolated and identified. When the HFDPCs proliferation activity was tested for the isolated compounds, gomisin N exhibited ≥ 20% proliferation activity. Thus, via response surface methodology (RSM), the optimum extraction conditions to obtain the maximum level of gomisin N from the fruit of S. chinensis were determined, where ethanol proportion, extraction time, and extraction temperature were used as the independent variables. The results revealed coefficient of determination ≥ 0.95 and p-value ≤ 0.05, which confirmed the fit of the model. The optimum extraction conditions to achieve the maximum content of gomisin N were as follows: ethanol proportion 83.8%, extraction temperature 80 ℃, and extraction time 8.7 h. The content of gomisin N using these conditions was predicted as 378,300 ppm, and a mean value close to the predicted value (376,884 ppm) was obtained while validating the aforementioned conditions.

Ginsenoside Rg1 alleviates Aβ deposition by inhibiting NADPH oxidase 2 activation in APP/PS1 mice

  • Zhang, Han;Su, Yong;Sun, Zhenghao;Chen, Ming;Han, Yuli;Li, Yan;Dong, Xianan;Ding, Shixin;Fang, Zhirui;Li, Weiping;Li, Weizu
    • Journal of Ginseng Research
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    • v.45 no.6
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    • pp.665-675
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    • 2021
  • Background: Ginsenoside Rg1 (Rg1), an active ingredient in ginseng, may be a potential agent for the treatment of Alzheimer's disease (AD). However, the protective effect of Rg1 on neurodegeneration in AD and its mechanism of action are still incompletely understood. Methods: Wild type (WT) and APP/PS1 AD mice, from 6 to 9 months old, were used in the experiment. The open field test (OFT) and Morris water maze (MWM) were used to detect behavioral changes. Neuronal damage was assessed by hematoxylin and eosin (H&E) and Nissl staining. Immunofluorescence, western blotting, and quantitative real-time polymerase chain reaction (q-PCR) were used to examine postsynaptic density 95 (PSD95) expression, amyloid beta (Aβ) deposition, Tau and phosphorylated Tau (p-Tau) expression, reactive oxygen species (ROS) production, and NAPDH oxidase 2 (NOX2) expression. Results: Rg1 treatment for 12 weeks significantly ameliorated cognitive impairments and neuronal damage and decreased the p-Tau level, amyloid precursor protein (APP) expression, and Aβ generation in APP/PS1 mice. Meanwhile, Rg1 treatment significantly decreased the ROS level and NOX2 expression in the hippocampus and cortex of APP/PS1 mice. Conclusions: Rg1 alleviates cognitive impairments, neuronal damage, and reduce Aβ deposition by inhibiting NOX2 activation in APP/PS1 mice.

Analytical methods to manage potential impurities in drug substances (의약품 중 잠재적 불순물 관리를 위한 분석법 연구 동향)

  • Park, Kyung Min;Kim, Won Mi;Ahn, Su Hyun;Lee, Ha Lim;Hwang, Su Hyeon;Lee, Wonwoong;Hong, Jongki
    • Analytical Science and Technology
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    • v.35 no.3
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    • pp.93-115
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    • 2022
  • Potential impurities in pharmaceuticals could be produced during manufacture, distribution, and storage and affect quality and safety of pharmaceuticals. In particular, highly reactive impurities could result in carcinogenic (mutagenic) effects on human body. International Conference on Harmonisation (ICH) has provided M7(R1) guideline for "Assessment and Control of DNA Reactive (Mutagenic) Impurities in Pharmaceuticals to Limit Potential Carcinogenic Risk" and recommended an adoption of this guideline to the authorities. ICH M7(R1) guideline provides classification, accepted intakes, and controls of potential impurities in pharmaceuticals. However, since appropriate and unified analytical methods for impurities in pharmaceuticals have not been provided in this guideline, most potential impurities in pharmaceuticals are still difficult to manage and supervise by pharmaceutical companies and regulatory authorities, respectively. In this review, we briefly described definition of unintended mutagenic impurities, basic information in ICH M7(R1) guideline, and analytical methods to determine potential impurities. This review would be helpful to manage and supervise potential impurities in pharmaceuticals by pharmaceutical companies and regulatory authorities.

Effects of Luteolin-7-𝑂-glucoside on melanin synthesis (Luteolin-7-𝑂-glucoside가 멜라닌 합성에 미치는 영향)

  • Choi, Byeong Min;Hong, Hyehyun;Park, Taejin;Kim, Seung-Young
    • 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.

MMP-2 and MMP-9 Inhibitory Effects of Different Solvent Fractions from Corydalis heterocarpa (염주괴불주머니 분획물의 MMP-2, MMP-9 발현 억제 효과)

  • Yu, Ga Hyun;Karadeniz, Fatih;Kong, Chang-Suk
    • Journal of Life Science
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    • v.31 no.11
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    • pp.980-986
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    • 2021
  • Natural products have always been an attractive source in terms of novel anti-metastatic compounds which can hinder MMP expression and activity. Corydalis heterocarpa is a salt marsh plant found in the seashores throughout Korea. Its yellow flowers and spikes have been an ingredient in folk medicine to treat spasm and contractions. The present study assessed the potential of different solvent-based fractions from the crude extract of Corydalis heterocarpa (CHE), a halophyte with reported bioactivities, to suppress the PMA-induced MMP expression in human fibrosarcoma HT-1080 cells. The solvent fractions which were named after the solvent used for fractionation (n-hexane, 85% aqueous (aq.) methanol (MeOH), n-butanol (BuOH), and H2O were shown to inhibit the both elevated mRNA and protein expression levels of MMP-2 and MMP-9 and simultaneously relieved the suppression on the expression of the endogenous MMP inhibitors TIMP-1 and TIMP-2. Results indicated that the CHE fractions might intervene with the PMA-induced activation of the MAPK signaling which is the upstream activator of MMP overexpression. Among tested samples, 85% aq. MeOH and n-hexane fractions of CHE was determined to be the most active and future studies to isolate the bioactive substances responsible for the regulation of the MMP expression are, therefore, urged. In conclusion, C. heterocarpa was shown to be a potential source of anti-metastatic compounds and n-Hexane and MeOH fractions might yield lead molecules to develop novel MMP inhibitors.

Curcumin represses lipid accumulation through inhibiting ERK1/2-PPAR-γ signaling pathway and triggering apoptosis in porcine subcutaneous preadipocytes

  • Pan, Shifeng;Chen, Yongfang;Zhang, Lin;Liu, Zhuang;Xu, Xingyu;Xing, Hua
    • Animal Bioscience
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    • v.35 no.5
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    • pp.763-777
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    • 2022
  • Objective: Excessive lipid accumulation in adipocytes results in prevalence of obesity and metabolic syndrome. Curcumin (CUR), a naturally phenolic active ingredient, has been shown to have lipid-lowering effects. However, its underlying mechanisms have remained largely unknown. Therefore, the study aims to determine the effect of CUR on cellular lipid accumulation in porcine subcutaneous preadipocytes (PSPA) and to clarify novel mechanisms. Methods: The PSPA were cultured and treated with or without CUR. Both cell counting Kit-8 and lactate dehydrogenase release assays were used to examine cytotoxicity. Intracellular lipid contents were measured by oil-red-o staining extraction and triglyceride quantification. Apoptosis was determined by flow cytometry and the terminal deoxynucleotidyl transferase-mediated deoxyuridine triphosphate-nick end labelling assay. Adipogenic and apoptosis genes were analyzed by quantitative polymerase chain reaction and Western blot. Results: The CUR dose-dependently reduced the proliferation and lipid accumulation of PSPA. Noncytotoxic doses of CUR (10 to 20 μM) significantly inhibited extracellular signal-regulated kinase 1/2 (ERK1/2) phosphorylation and expression of adipogenic genes peroxisome proliferation-activity receptor-γ (PPAR-γ), CCAAT/enhancer binding protein-α, sterol regulatory element-binding protein-1c, adipocyte protein-2, glucose transporter-4 as well as key lipogenic enzymes fatty acid synthase and acetyl-CoA carboxylase, while ERK1/2 activation significantly reversed CUR-reduced lipid accumulation by increasing PPAR-γ. Furthermore, compared with differentiation induced media treated cells, higher dose of CUR (30 μM) significantly decreased the expression of AKT and B-cell lymphoma-2 (BCL-2), while increased the expression of BCL-2-associated X (BAX) and the BAX/BCL-2 expression ratio, suggesting triggered apoptosis by inactivating AKT and increasing BAX/BCL-2 ratio and Caspase-3 expression. Moreover, AKT activation significantly rescued CUR inhibiting lipid accumulation via repressing apoptosis. Conclusion: These results demonstrate that CUR is capable of suppressing differentiation by inhibiting ERK1/2-PPAR-γ signaling pathway and triggering apoptosis via decreasing AKT and subsequently increasing BAX/BCL-2 ratio and Caspase-3, suggesting that CUR provides an important method for the reduction of porcine body fat, as well as the prevention and treatment of human obesity.

Effect of Tetramethylpyrazine on Pro-Inflammatory Cytokine Expressions in Mouse Brain Tissue following Intracerebroventricular Lipopolysaccharide Treatment (Tetramethylpyrazine이 LPS의 뇌실주입에 따른 생쥐 뇌조직의 Pro-Inflammatory Cytokines 발현에 미치는 영향)

  • Choi, Yong-Seok;Won, Jong-Woo;Yoo, Inwoo;Shin, Jung-Won;Kim, Seong-Joon;Sohn, Nak-Won
    • The Korea Journal of Herbology
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    • v.28 no.1
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    • pp.83-90
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    • 2013
  • Objectives : Tetramethylpyrazine (TMP) is an active ingredient in Ligusticum wallichii and has a wide range of neuroprotection effects. This study investigated anti-neuroinflammatory effect of TMP on brain regions in intracerebroventricular (i.c.v.) lipopolysaccharide (LPS)-treated C57BL/6 mice. Methods : TMP was administered intraperitoneally at doses of 10, 20, and 30 mg/kg at 1 h prior to LPS (3 mg/kg) i.c.v. injection. mRNA level of pro-inflammatory cytokines, including tumor necrosis factor-${\alpha}$ (TNF-${\alpha}$), interleukin (IL)-$1{\beta}$ and IL-6, was measured in the cerebral cortex, hippocampus, and hypothalamus tissue using real-time polymerase chain reaction at 24 h after the LPS injection. Cyclooxygenase-2 (COX-2) positive cells in the hypothalamus was also observed using immunohistochemistry at 24 h after the LPS injection. Results : At a dose of 30 mg/kg TMP significantly attenuated up-regulation of TNF-${\alpha}$ and IL-$1{\beta}$ mRNA in the cerebral cortex and IL-$1{\beta}$ mRNA in the hippocampus. In the hypothalamus, doses of 20 mg/kg and 30 mg/kg TMP significantly attenuated up-regulation of TNF-${\alpha}$, IL-$1{\beta}$, and IL-6 mRNA induced by the LPS injection. In addition, TMP (30 mg/kg) significantly reduced the number of COX-2 positive cells in the hypothalamus. Conclusion : These results indicate that TMP has an anti-inflammatory effect on neuroinflammation, especially in the hypothalamus, induced by LPS i.c.v. injection and suggest that TMP-containing Ligusticum wallichii may play a modulatory role on the systemic responses following hypothalamic inflammation.

Effects of β-Asarone on Pro-Inflammatory Cytokines and Learning and Memory Impairment in Lipopolysaccharide-Treated Mice (β-Asarone이 Lipopolysaccharide에 의한 생쥐 해마의 염증성 사이토카인 발현과 학습 및 기억 장애에 미치는 영향)

  • Choi, Moon-Sook;Kwak, Hee-Jun;Kweon, Ki-Jung;Hwang, Ji-Mo;Shin, Jung-Won;Sohn, Nak-Won
    • The Korea Journal of Herbology
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    • v.28 no.6
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    • pp.119-127
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    • 2013
  • Objectives : ${\beta}$-Asarone (BAS) is an active ingredient in Acori Rhizoma. This study investigated anti-neuroinflammatory and memory ameliorating effects of BAS in systemic lipopolysaccharide (LPS)-treated C57BL/6 mice. Methods : BAS was administered orally at doses of 7.5, 15, and 30 mg/kg for 3 days prior to LPS (3 mg/kg, intraperitoneal) injection. Pro-inflammatory cytokine mRNA, including tumor necrosis factor-${\alpha}$ (TNF-ㅍ), interleukin (IL)-$1{\beta}$ and IL-6, was measured in hippocampus tissue using real-time polymerase chain reaction at 4 h after the LPS injection. An ameliorating effect of 30 mg/kg BAS on learning and memory impairment in the LPS-treated mice was verified using the Morris water maze test. Results : BAS significantly attenuated up-regulation of TNF-${\alpha}$, IL-$1{\beta}$, and IL-6 mRNA in hippocampus tissue of the LPS-treated mice. In acquisition training test, BAS improved learning performance of the LPS-treated mice with a significant decrease of escape latency to the platform. In memory retention test, BAS also ameliorated memory impairment of the LPS-treated mice with a significant increase of swimming time in zones neighboring to the platform, number of target heading, and memory score. Conclusion : The results suggest that inhibition of pro-inflammatory cytokines and neuroinflammation in the hippocampus by BAS could be one of the mechanisms for BAS-mediated ameliorating effect on learning and memory impairment in LPS-treated mice.

Effect of Ginsenoside Rg3 on COX-2 Expression in Brain Tissue of Lipopolysaccharide-Treated Mice (Ginsenoside Rg3이 Lipopolysaccharide에 의한 생쥐 뇌조직의 Cyclooxygenase-2 발현에 미치는 영향)

  • Choi, Wonik;Cho, Yong-Deok;Lee, Joon-Seok;Shin, Jung-Won;Kim, Seong-Joon;Sohn, Nak-Won
    • The Korea Journal of Herbology
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    • v.27 no.6
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    • pp.131-137
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    • 2012
  • Objectives : Cyclooxygenase (COX) plays a central role in the inflammatory cascade by converting arachidonic acid into prostaglandin. COX-2 is typically induced by inflammatory stimuli in the majority of tissues, it is responsible for propagating the inflammatory response and thus, considered as the best target for anti-inflammatory drugs. The present study investigated the modulatory effect of ginsenoside Rg3, a principle active ingredient in Panax ginseng, on COX-2 expression in the brain tissue induced by systemic lipopolysaccharide (LPS) treatment in C57BL/6 mice. Methods : Because systemic LPS treatment induces COX-2 expression immediately in the brain, ginsenoside Rg3 was treated orally with doses of 10, 20, and 30 mg/kg at 1 hour before the LPS (3 mg/kg, i.p.) injection. At 4 hours after the LPS injection, COX-2 mRNA was measured by real-time polymerase chain reaction method, COX-2 protein levels were measured by Western blotting. In addition, COX-2 expressions in brain tissue were observed with immunohistochemistry and double immunofluoresence labeling. Results : Ginsenoside Rg3 (20 and 30 mg/kg) significantly attenuates up-regulation of COX-2 mRNA and protein expression in brain tissue at 4 hours after the LPS injection. Moreover, ginsenoside Rg3 (20 mg/kg) significantly reduced the number of COX-2 positive neurons in the cerebral cortex and amygdala. Conclusion : These results indicate that ginsenoside Rg3 plays a modulatory role in neuroinflammation through the inhibition of COX-2 expression in the brain and suggest that ginsenoside Rg3 and ginseng may be effective on neurodegenerative diseases caused by neuroinflammation.