• Title/Summary/Keyword: pharmaceutical ingredient

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The Convergence Effect of Phloretin Existent in Plants on Vascular Contractility (플로레틴(Phloretin)의 혈관내피수축 융합효과와 관련기전 연구)

  • Bang, Joon Seok;Je, Hyun Dong;Min, Young Sil
    • Journal of Convergence for Information Technology
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    • v.10 no.10
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    • pp.143-149
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    • 2020
  • This study tried to observe the ability to inhibit vasocontriction in phloretin - the primary ingredient of apple tree leaves and the Manchurian apricot - through ROCK(Rho-associdated, coiled-coil containing protein kinase) inactivation in rat aortae. A piece of artery that was separated from Sprague-Dawley male rats and retained or damaged the endothelium was suspended in myograph tank with two metal rings, the lower ring fixed to the bottom of the tank, and the upper ring connected to the isotonic force transducer. Interestingly, phloretin inhibited fluoride- or phorbol ester-provoked contraction implying that additional pathways dissimilar from endothelial nitric oxide synthesis such as ROCK or MEK (mitogen activated protein kinase kinase) inactivation might be involved in the vasorelaxation. Therefore, this study provides that phloretin participates in the reduction of ROCK or MEK activity in smooth muscle in addition to the endothelial-dependent action of the endotheliuim in complete blood vessels, and consequently inhibits actin-myosin interaction in smooth muscle. Furthermore, phloretin inhibited thromboxane A2-induced contraction suggesting the mechanism including inhibition of ROCK and MEK.

Stability and Safety of Bee Venom with and without Additives (첨가물에 의한 봉독의 안정화 및 안전성)

  • Bae, Young Hyeon;Lee, Chong Hwan;Kim, Hae Sol;Kim, Ho Sun;Suh, Chang Yong;Kim, No Hyeon;Lee, Jin Ho;Ha, In Hyuk;Kim, Me Riong;Chung, Hwa Jin;Lee, In Hee;Kim, Min Jeong;Kim, Eun Jee;Lee, Jae Woong
    • Journal of Acupuncture Research
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    • v.32 no.3
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    • pp.127-133
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    • 2015
  • Objectives : Previous studies have shown that the amount of melittin, the main active ingredient in bee venom pharmacopuncture, tends to decrease substantially with time during pharmacopuncture manufacture. This study aimed to assess whether the stability of bee venom pharmacopuncture improved with pharmacopuncture additives. Methods : Components were measured using high performance liquid chromatography. Acute toxicity and antigenicity tests by subcutaneous and venous routes were conducted at Korea Pharmaceutical Test & Research Institute and mortality, adverse reactions, and body weight changes were assessed. Results : Stability tests using additives revealed that bee venom without additives was most stable. Bee venom pharmacopuncture without additives was further tested for toxicity in subcutaneous and venous administration in mice and no changes pertaining to toxicity were found over the testing period. Conclusions : Bee venom pharmacopuncture without additives was found to be most stable, and further, it did not show toxicity or antigenicity in subcutaneous and venous administration in mice.

Effect of $Panax$ $ginseng$ C.A. Meyer Extract (Ginseol K-b1) on UVB-induced Skin Damage in Hairless Mice (Hairless Mice에서 UVB로 유도된 피부손상에 인삼추출물(Ginseol K-b1)이 미치는 영향)

  • Chang, Jeong-Hwa;Hwang, Se-Hee;Lee, Eun-Ju;Ohto, Nobuaki;Lee, Jin-Hee
    • Journal of the East Asian Society of Dietary Life
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    • v.22 no.2
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    • pp.224-230
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    • 2012
  • To investigate the effect of Panax ginseng C.A. Meyer extract (Ginseol K-b1), on skin functionality, we evaluated skin appearance and properties, such as wrinkle formation, skin moisture content, and skin elasticity in the skin of hairless mice damaged by UV irradiation. In addition, the effect of Ginseol K-b1 on collagen synthesis in human dermal fibroblasts was investigated. Female hairless mice were orally administered Ginseol K-b1 for 10 weeks with UV irradiation. Wrinkle formation in the Ginseol K-b1-treated group was significantly suppressed compared to the UV-irradiated group. Skin properties, including skin moisture content and elasticity, of the Ginseol K-b1-treated group were better than those of the control group. In the human fibroblast cells, Ginseol K-b1 treatment enhanced cell proliferation and significantly stimulated collagen synthesis. These results suggest that Ginseol K-b1 is a potent ingredient with anti-aging effects.

Isolation of Stenotrophomonas rhizopilae Strain GFC09 with Ginsenoside Converting Activity and Anti-wrinkle Effects of Converted Ginsenosides (사포닌 전환 활성 Stenotrophomonas rhizopilae Strain GFC09 균주의 분리 동정 및 전환 사포닌의 주름 개선 효과)

  • Min, Jin Woo;Kim, Hye-Jin;Joo, Kwang-Sik;Kang, Hee-Cheol
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.41 no.4
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    • pp.375-382
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    • 2015
  • Ginsenosides (ginseng saponin) as the one of important pharmaceutical compounds of ginseng and is responsible for the pharmacological and biological activities. These ginsenoside produces diverse small molecules ginsenoside which have more pharmacological activities including anti-wrinkle, anti-cancer and anti-oxidant effects. In the present study, we isolated bacteria using esculin agar, to produce ${\beta}$-glucosidase, and we focused on the bio-transformation of ginsenoside. Phylogenetic tree analysis was performed by comparing the 16S rRNA sequences; we identified the strain as Stenotrophomonas rhizopilae strain GFC09. In order to determine the optimal conditions for enzyme activity, the crude enzyme was incubated with 1 mM ginsenoside $Rb_1$. Bioconversion of ginsenoside $Rb_1$ were analyzed using TLC and HPLC. The crude enzyme hydrolyzed the ginsenoside $Rb_1$ along the following pathway: LB: $Rb_1{\rightarrow}Rd{\rightarrow}F_2$ into compound K, TSB: $Rb_1{\rightarrow}Rd{\rightarrow}F_2$. The structure of the hydrolyzed metabolites were identified by NMR. The activity screening tests showed that the conversion product induced the production of type I procollagen in a dose-dependent manner. These results suggested that hydrolyzed ginseng product containing the ginsenoside $F_2$ and compound K could be useful as an active ingredient for wrinkle-care cosmetics.

Study on Application of Skin Care Cosmetic and Stabilization of Idebenone by Forming Niosome Vesicle Technology

  • Kim, In-Young
    • Journal of the Korean Applied Science and Technology
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    • v.36 no.2
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    • pp.592-599
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    • 2019
  • This study is to stabilize insoluble and unstable active ingredient which is Idebenone (INCI name: hydroxydecyl ubiquinone) in a multi-lamellar vesicle (MLV) and to stabilize it in the skin care cosmetics. Idebenone is good effective raw material in the treatment of Alzheimer's disease in the medical field and a powerful antioxidant in dermatology. It is well known as a substance that inhibits the formation of melanin and cleans the skin pigment. However, it did not dissolve in any solvent and it was difficult to apply in cosmetic applications. Niosome vesicle was able to develop a nano-particle by making a multi-layer of idebenone encapsulated with a nonionic surfactant, hydrogenated lecithin and glycine soja (soybean) sterols and passing it through a high pressure microfluidizer. Idebenone niosome vesicle (INV) has been developed to have the ability to dissolve transparently in water and to promote transdermal penetration. The appearance of the INV was a yellowish liquid having specific odor, and the particle size distribution of INV was about 10~80 nm. The pH was 5~8 (mean=6.8). This capsulation with idebenone was stored in a $45^{\circ}C$ incubator for 3 months and its stability was observed and quantitatively measured by HPLC. As a result, the stability of the sample encapsulated in the niosome vesicle (97.5%) was about 66.3% higher than that of the non-capsule sample of 32.5%. Idebenone 1% INV was used for the efficacy test and clinical trial evaluation as follows. The anti-oxidative activity of INV was 38.2%, which was superior to that of 12.8% tocopherol (control). The melanin-reducing effect of B16 melanoma cells was better than INV (17.4%) and Albutin (control) (9.6%). Pro-collagen synthesis rate was 128.2% for INV and 89.3% for tocopherol (control). The skin moisturizing effect was 15.5% better than the placebo sample. The elasticity effect was 9.7% better than the placebo sample. As an application field, INV containing 1% of idebenone is expected to be able to develop various functional cosmetic formulations such as skin toner, ampoule essence, cream, eye cream and sunblock cream. In addition, it is expected that this encapsulated material will be widely applicable to emulsifying agents for skin use in the pharmaceutical industry as well as the cosmetics industry.

Bioactive lipids in gintonin-enriched fraction from ginseng

  • Cho, Hee-Jung;Choi, Sun-Hye;Kim, Hyeon-Joong;Lee, Byung-Hwan;Rhim, Hyewon;Kim, Hyoung-Chun;Hwang, Sung-Hee;Nah, Seung-Yeol
    • Journal of Ginseng Research
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    • v.43 no.2
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    • pp.209-217
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    • 2019
  • Background: Ginseng is a traditional herbal medicine for human health. Ginseng contains a bioactive ligand named gintonin. The active ingredient of gintonin is lysophosphatidic acid C18:2 (LPA C18:2). We previously developed a method for gintonin-enriched fraction (GEF) preparation to mass-produce gintonin from ginseng. However, previous studies did not show the presence of other bioactive lipids besides LPAs. The aim of this study was to quantify the fatty acids, lysophospholipids (LPLs), and phospholipids (PLs) besides LPAs in GEF. Methods: We prepared GEF from white ginseng. We used gas chromatography-mass spectrometry for fatty acid analysis and liquid chromatography-tandem mass spectrometry for PL analysis, and quantified the fatty acids, LPLs, and PLs in GEF using respective standards. We examined the effect of GEF on insulin secretion in INS-1 cells. Results: GEF contains about 7.5% linoleic (C18:2), 2.8% palmitic (C16:0), and 1.5% oleic acids (C18:1). GEF contains about 0.2% LPA C18:2, 0.06% LPA C16:0, and 0.02% LPA C18:1. GEF contains 0.08% lysophosphatidylcholine, 0.03% lysophosphatidylethanolamine, and 0.13% lysophosphatidylinositols. GEF also contains about 1% phosphatidic acid (PA) 16:0-18:2, 0.5% PA 18:2-18:2, and 0.2% PA 16:0-18:1. GEFmediated insulin secretion was not blocked by LPA receptor antagonist. Conclusion: We determined four characteristics of GEF through lipid analysis and insulin secretion. First, GEF contains a large amount of linoleic acid (C18:2), PA 16:0-18:2, and LPA C18:2 compared with other lipids. Second, the main fatty acid component of LPLs and PLs is linoleic acid (C18:2). Third, GEF stimulates insulin secretion not through LPA receptors. Finally, GEF contains bioactive lipids besides LPAs.

TLC, HPTLC FINGERPRINTING AND ACUTE ORAL TOXICITY EVALUATION OF HABB-E-AZARAQI: A NUX-VOMICA-BASED TRADITIONAL UNANI FORMULATION

  • Ara, Shabnam Anjum;Viquar, Uzma;Zakir, Mohammed;Husain, Gulam Mohammed;Naikodi, Mohammed Abdul Rasheed;Urooj, Mohd;Kazmi, Munawwar Husain
    • CELLMED
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    • v.11 no.3
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    • pp.13.1-13.9
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    • 2021
  • Background and Objective: Nux-vomica based traditional Unani formulation, Habb-e-Azaraqi (HAZ) is an important drug used by Unani physicians since several decades. It possesses Muqawwi-i-A'sab (nervine tonic), Muharrik-i-A'sab (nervine stimulant) properties and is an effective treatment option for diseases like Laqwa (facial palsy), Falij (paralysis), Niqris (gout) and Waja'al-Mafasil (arthritis) etc. The aim of the study is to access and provide information of HAZ for its TLC, HPTLC Fingerprinting defining its clear qualitative perspective and acute oral toxicity evaluation for its safety assessment which was not done earlier, thus contributing in the field of research. Materials and Methods: The chief ingredient, nux-vomica was detoxified as per method mentioned in Unani Pharmacopeia before its use in formulation. TLC and HPTLC was developed under four detection system i.e., UV 366nm, UV 254nm, exposure to iodine vapours and after derivatization with anisaldehyde sulphuric acid. Acute toxicity studies were performed as per OECD Guidelines 425 at a limit dose of 2000 mg/kg. Observations were done for signs of toxicity, body weight, and feed consumption at regular intervals followed by haematological and biochemistry evaluation. Results: The generated data proved the authenticity and established the TLC and HPTLC profile of the formulation. Acute toxicity revealed no significant differences in HAZ-treated animals with respect to body weight gain, feed consumption, haematology, clinical biochemistry evaluation. No significant gross pathological observation was noticed in necropsy. Conclusion: Data of the present study is substantial and scientific proof of HAZ in terms of standardization and toxicity study that can be utilize in future research activities.

A study on antioxidant and anti-inflammatory effects of domestic blended essential oils (국내산 블렌딩 정유의 항산화 및 항염 효과 연구)

  • Jung, Sook Heui;Lee, Eun Kyung
    • Journal of the Korean Applied Science and Technology
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    • v.38 no.6
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    • pp.1370-1382
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    • 2021
  • Previous studies have been conducted on domestic materials as a single extract. Research on complex mixtures for maximizing plant characteristics by individual extraction and potential interference with effects is insufficient. Therefore, this study confirmed the GC-MSD according to the extraction of essential oils for Agastache rugosa O. Kuntze(AR), Pinus densiflora Sieb. et Zuccarini(PD), Curcuma longa, Curcuma domestica(CC), Zingiber officinale Roscoe(ZR), Foeniculum vulgare Miller(FV), and Citrus medica L. var. sarcodactylis Swingle(CS). The cytotoxicity, antioxidant, and anti-inflammatory properties of the blending oil were confirmed to confirm its potential as a cosmetic material. As a result of analyzing GC-MSD aroma components, the main components were estragole of AR, à-Pinene for PD, Zingiberene for CC and ZR, Anethole from FV, and D-Limonene for CS. At a concentration of 100 uL/mL with no confirmed cytotoxicity, NO production was inhibited by 70.62%, DPPH radical scavenging activity was 64.03%, and ABTS radical scavenging activity was 89.55%. Through this, blended essential oil suggests the possibility of useful application as a raw material with antioxidant and anti-inflammatory effects in the cosmetic and food industries.

A novel protocol for batch-separating gintonin-enriched, polysaccharide-enriched, and crude ginsenoside-containing fractions from Panax ginseng

  • Rami Lee;Han-Sung Cho;Ji-Hun Kim;Hee-Jung Cho;Sun-Hye Choi;Sung-Hee Hwang;Hyewon Rhim;Ik-Hyun Cho;Man-Hee Rhee;Do-Geun Kim;Hyoung-Chun Kim;Seung-Yeol Nah
    • Journal of Ginseng Research
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    • v.47 no.3
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    • pp.366-375
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    • 2023
  • Background: Ginseng contains three active components: ginsenosides, gintonin, and polysaccharides. After the separation of 1 of the 3 ingredient fractions, other fractions are usually discarded as waste. In this study, we developed a simple and effective method, called the ginpolin protocol, to separate gintonin-enriched fraction (GEF), ginseng polysaccharide fraction (GPF), and crude ginseng saponin fraction (cGSF). Methods: Dried ginseng (1 kg) was extracted using 70% ethanol (EtOH). The extract was water fractionated to obtain a water-insoluble precipitate (GEF). The upper layer after GEF separation was precipitated with 80% EtOH for GPF preparation, and the remaining upper layer was vacuum dried to obtain cGSF. Results: The yields of GEF, GPF, and cGSF were 14.8, 54.2, and 185.3 g, respectively, from 333 g EtOH extract. We quantified the active ingredients of 3 fractions: L-arginine, galacturonic acid, ginsenosides, glucuronic acid, lysophosphatidic acid (LPA), phosphatidic acid (PA), and polyphenols. The order of the LPA, PA, and polyphenol content was GEF > cGSF > GPF. The order of L-arginine and galacturonic acid was GPF >> GEF = cGSF. Interestingly, GEF contained a high amount of ginsenoside Rb1, whereas cGSF contained more ginsenoside Rg1. GEF and cGSF, but not GPF, induced intracellular [Ca2+]i transient with antiplatelet activity. The order of antioxidant activity was GPF > GEF = cGSF. Immunological activities (related to nitric oxide production, phagocytosis, and IL-6 and TNF-α release) were, in order, GPF > GEF = cGSF. The neuroprotective ability (against reactive oxygen species) order was GEF > cGSP > GPF. Conclusion: We developed a novel ginpolin protocol to isolate 3 fractions in batches and determined that each fraction has distinct biological effects.

Physical Properties and Skin Penetration of Niosome Formulations Containing Minoxidil and Diaminopyrimidine Oxide (미녹시딜과 다이아미노피리미딘옥사이드 성분을 함유하는 니오좀 제형의 물성 및 피부투과)

  • Bo Kyung Kim;Won Hyung Kim;Kyung-Sup Yoon
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.49 no.2
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    • pp.127-139
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    • 2023
  • In this study, minoxidil, which is well known as a pharmaceutical raw material, and diaminopyrimidine oxide (DAO), which is a cosmetic raw material, were used as active ingredients to evaluate the physical properties of niosomes and compare the skin penetrations of artificial skin. To prepare niosomes of the size of nanoparticles, a high pressure homogenization method was used, and physical properties were evaluated with a zetasizer. The particle size of the noisome including the active ingredient was measured to be 99 to 123 nm according to HLB, and the zeta potential was measured in the range of -60 to -81 mV. Through DSC (differential scanning colorimetry), it was confirmed that minoxidil, a crystalline component, was uniformly dissolved in an amorphous state in niosomes. In order to confirm and compare skin penetration, it was measured by the in vitro Franz diffusion cell method, and the niosome formulation showed 3.4 times higher penetration for minoxidil and 11.1 times higher penetration for DAO than the control gel formulation. In addition, when comparing the skin penetration of minoxidil niosome and DAO niosome, a similar trend was shown, and the penetration amount of DAO was relatively high. The shapes of the niosome formulations with different HLB values were observed using Cryo-TEM, and it was confirmed that vesicles were formed in all of them and that they were intermediate between SUV (small unilamella vesicle) and LUV (large unilamella vesicle). Through this study, minoxidil, an effective drug for hair loss, and DAO, a cosmetic raw material, can be effectively delivered to the skin by encapsulating them in a noisome formulation.