• Title/Summary/Keyword: active pharmaceutical ingredients

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Effects of Ginsenosides on $GABA_A$ Receptor Channels Expressed in Xenopus Oocytes

  • Choi, Se-Eun;Choi, Seok;Lee, Jun-Ho;Paul J.Whiting;Lee, Sang-Mok;Nah, Seung-Yeol
    • Archives of Pharmacal Research
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    • v.26 no.1
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    • pp.28-33
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    • 2003
  • Ginsenosides, major active ingredients of Panax ginseng, are known to regulate excitatory ligand-gated ion channel activity such as nicotinic acetylcholine and NMDA receptor channel activity. However, it is not known whether ginsenosides affect inhibitory ligand-gated ion channel activity. We investigated the effect of ginsenosides on human recombinant $GABA_A$ receptor (${\alpha}_1{\beta}_1{\gamma}_{2s}$) channel activity expressed in Xenopus oocytes using a two-electrode voltage-clamp technique. Among the eight individual ginsenosides examined, namely, $Rb_1$, $Rb_2$, Rc, Rd, Re, Rf, $Rg_1$ and $Rg_2$, we found that Rc most potently enhanced the GABA-induced inward peak current ($I_{GABA}$). Ginsenoside Rc alone induced an inward membrane current in certain batches of oocytes expressing the $GABA_A$ receptor. The effect of ginsenoside Rc on $I_{GABA}$ was both dose-dependent and reversible. The half-stimulatory concentration ($EC_{50}$) of ginsenoside Rc was 53.2$\pm$12.3 $\mu$M. Both bicuculline, a $GABA_A$ receptor antagonist, and picrotoxin, a $GABA_A$ channel blocker, blocked the stimulatory effect of ginsenoside Rc on $I_{GABA}$. Niflumic acid (NFA) and 4,4'-diisothiocyanostilbene-2,2'-disulfonic acid (DIDS), both $CI^{-1}$ channel blockers, attenuated the effect of ginsenoside Rc on I$I_{GABA}$. This study suggests that ginsenosides regulated $GABA_A$ receptor expressed in Xenopus oocytes and implies that this regulation might be one of the pharmacological actions of Panax ginseng.

Effect of Lignan Components from Schizandra chinensis on Beta-amyloid Aggregation Inhibition and Dissociation (오미자 리그난 화합물의 베타-아밀로이드간 결합 억제 및 해리 효과)

  • Yu, Ho Jin;Yoon, Mi So;Kim, Do Yoon;Won, Kyung-Jong;Kim, Bokyung;Jang, Sang-Hee;Lee, Hwan Myung
    • YAKHAK HOEJI
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    • v.56 no.5
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    • pp.293-298
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    • 2012
  • The present study tested the effect of Schizandra chinensis lignan compounds, Gomisin A and Schizandrin, on the aggregation and dissociation of beta-amyloid $(A{\beta})_{1-42}$ to explore a possible therapeutic target for Alzheimer's disease. Gomisin A significantly inhibited the $A{\beta}_{1-42}$ aggregation in a dose dependent manner, but did not induced the dissociation of aggregated $A{\beta}_{1-42}$. On the other hand, Schizandrin significantly suppressed the aggregation and dissociation of $A{\beta}_{1-42}$. These results suggest that Gomisin A and Schizandrin, which are known as biologically active ingredients from Schizandra chinensis, may be potentially useful target molecules to develop a drug for the prevention or treatment of Alzheimer's disease.

Hair Growth-promoting Effect of Resina Pini and Its Main Constituent, Abietic Acid, in Mouse Model of Alopecia (탈모마우스모델에서의 송지추출물 및 그 성분인 아비에트산의 모발성장효과)

  • Park, Gunhyuk;Kim, Yong-ung
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.42 no.3
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    • pp.203-209
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    • 2016
  • Recently, increased attention has been directed toward medicinal extracts and their active ingredients as potential new drug candidates for androgenic alopecia. Resina Pini (RP), a resinous exudation obtained from Pinus sp. (Pinaceae), has been used as a traditional medicine for the treatment of infection, pain related to dental caries, and periodontal disease. Previously, we suggested that RP and its main constituent, abietic acid (abieta-7,13-dien-18-oic acid; AA), may play important roles against androgenic alopecia as $5{\alpha}$-reductase inhibitors. However, to date, there is no evidence that AA has hair growth-promoting effects in vivo. In this study, we found that 10 ~ 300 mg/kg RP and 3 ~ 30 mg/kg AA significantly promoted hair growth in a C3H/HeN mouse model of alopecia. To our knowledge, this is the first report of the hair growth-promoting effects of RP and AA in vivo. From these results, RP and its main constituent AA can promote hair growth in mouse by inhibiting $5{\alpha}$-reductase activity and may be effective alternative therapies for androgenic alopecia.

Anti-melanogenic effects of Hordeum vulgare L. barely sprout extract in murine B16F10 melanoma cells

  • Choi, Jeong-Hwa;Jung, Jong-Gi;Kim, Jung-Eun;Bang, Mi-Ae
    • Journal of Nutrition and Health
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    • v.52 no.2
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    • pp.168-175
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    • 2019
  • Purpose: Barely sprout is a well-known oriental herbal medicine with a wide range of health benefits. Recent studies have provided scientific evidence of its therapeutic effects with expanded application. This study investigated anti-melanogenic effect of barley sprout water extract (BSE) in murine melanocyte B16F10. Methods: Various concentrations (0, 50, 125, and $250{\mu}g/mL$) of BSE and arbutin (150 ppm) were applied to B16F10 stimulated with or without alpha-melanocyte stimulating hormone (100 nM) for 72 hours. The whitening potency of BSE was determined altered cellular melanin contents. Activity and expression of tyrosinase and microphthalmia-associated transcription factor (MITF) were also assayed. Results: Experimental results revealed that treatment with BSE reduced cellular melanin production by approximately 40% compared to the control. Molecular findings supported that suppressed activity and expression of tyrosinase and MITF proteins by BSE were associated with declined cellular melanogenesis. Furthermore, anti-melanogenic effect of BSE ($250{\mu}g/mL$) was similar to that of arbutin, a commonly used whitening agent. Lastly, polyphenols including p-coumaric, ferulic, and vanillic acids were identified in BSE using HPLC analyses. They might be potential active ingredients showing such melanogenesis-reducing effect. Conclusion: BSE was evident to possess favorable anti-melanogenic potency in an in vitro model. As a natural food sourced material, BSE could be an effective depigmentation agent with potential application in pharmaceutical and cosmetic industries.

Analysis of Influencing Factors on the Outpatient Prescription of Antipsychotic Drugs in the Elderly Patients (노인환자의 항정신병 약물 원외처방 내역에 미친 영향 요인 분석)

  • Dong, Jae Yong;Lee, Hyun Ji;Lee, Tae Hoon;Kim, Yujeong
    • Korean Journal of Clinical Pharmacy
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    • v.31 no.4
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    • pp.268-277
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    • 2021
  • Background: Most antipsychotic drugs studies have been mainly conducted on side effects, randomized clinical trials, utilization rates, and trends. But there have been few studies on the influencing factors in elderly patients. The purpose of this study was to analyze the influencing factors on the outpatient prescription of antipsychotic drugs in the elderly patients. Methods: Active ingredients of antipsychotic drugs in Korea were selected according to the Korean Pharmaceutical Information Center (KPIC)'s classification. Data source was Korean Health Insurance Review and Assessment Service (HIRA) claims data in 2020 and target patient group was the elderly patient group. We extracted patients who have been prescribed one or more antipsychotic drugs and visited only one medical institution. Data were analyzed using descriptive statistics, chi-square, t-test, negative binomial regression. Results: A number of outpatients were 245,197 and prescriptions were 1,379,092. Most characteristics of patients were 75-85 year's old, female, health insurance type, no disease (dementia, schizophrenia), atypical drugs, cci score (>2) and characteristics of medical institution were neurology in specialty, rural region, general hospitals. Results of regression showed that patient's characteristics and medical center characteristics had significant effect on the outpatient prescription of antipsychotic drugs in the elderly patients. Conclusion: This study suggests that national policy of antipsychotic drugs in the elderly patients, with the consideration of the patients' and medical institutions' characteristics, is needed.

Ethanol-pretreated Drying of (+)-dihydromyricetin for Removal of Residual Solvents (잔류 용매 제거를 위한 (+)-dihydromyricetin의 에탄올 전처리 건조)

  • Lee, Hee-Gun;Kim, Jin-Hyun
    • Korean Chemical Engineering Research
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    • v.60 no.2
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    • pp.237-242
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    • 2022
  • In this study, a drying method that can effectively remove residual solvent from (+)-dihydromyricetin was developed. Residual acetone concentration was efficiently removed below ICH-specified value (5,000 ppm) by simple rotary evaporation with ethanol pretreatment. In addition, the residual ethanol met the ICH-specified value (5,000 ppm) by simple rotary evaporation through the addition of water, and the residual moisture also met the specified value (<4%) for active pharmaceutical ingredients. At all the drying temperature (35, 45, and 55 ℃), a large amount of the residual solvent was initially removed during the drying, and the drying efficiency increased when increasing the drying temperature. Removal of residual solvent by ethanol pretreatment was shown to be related to high vapor pressure of acetone-ethanol mixture and hydrogen bonding between acetone and ethanol.

Effects of Activated Carbon on the Reduction of Benzo(a)pyrene in Artemisia argyi Extract

  • Lee, Sung-Hoon
    • Journal of People, Plants, and Environment
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    • v.23 no.5
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    • pp.537-544
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    • 2020
  • Background and objective: Artemisia argyi has a long history as an effective treatment for various diseases. The detection of environmental pollutant benzo(a)pyrene, a known human carcinogen, in the leaves of Artemisia argyi is cause for concern. For medicinal plant extracts, both a reduction of benzo(a)pyrene as well as the maintained effectiveness of the compound are important. Therefore, in this study, we propose an optimized process for the addition and filtration of activated carbon to reduce benzo(a)pyrene and change the contents of the indicating substance(jaceosidine and eupatilin). Methods: Artemisia argyi EtOH extract containing 36 ppb of benzo(a)pyrene was added to 0.1, 0.5, 1.0, and 1.5% (w/w) of activated carbon for 120 min and filtered using an activated carbon filter 1, 2, 3, and 5 times respectively. The content of benzo(a)pyrene and indicating substances in Artemisia argyi extract were then measured with high performance liquid chromatography (fluorescence and UV detectors). Results: As the amounts of activated carbon powder and filtering cycles increased, the content of benzo(a)pyrene in the Artemisia argyi extract decreased. However, when activated carbon powder 1.5% was added to the extract, and when the activated carbon filter was filtered five times, the results were reduced by 15% and 30~40% respectively. The optimal extraction condition for reducing benzo(a)pyrene was adding 1.5% of activated carbon powder. This resulted in reducing benzo(a)pyrene by 83% and indicating substances by about 4%. Conclusions: Here we present a process for reducing benzo(a)pyrene in Artemisia argyi extract using activated carbon to reduce toxicity and minimize the loss of active ingredients. This approach has potential application within a manufacturing process of various medicinal plant extracts.

Study on Optimization of Liquid Fermentation Medium and Antitumor Activity of the Mycelium on Phyllopora lonicerae

  • Min Liu;Lu Liu;Guoli Zhang;Guangyuan Wang;Ranran Hou;Yinghao Zhang;Xuemei Tian
    • Journal of Microbiology and Biotechnology
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    • v.34 no.9
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    • pp.1898-1911
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    • 2024
  • Phylloporia lonicerae is an annual fungus that specifically parasitizes living Lonicera plants, offering significant potential for developing new resource food and medicine. However, wild resources and mycelium production of this fungus is limited, and its anti-tumor active ingredients and mechanisms remain unclear, hampering the development of this fungus. Thus, we optimized the fermentation medium of P. lonicerae and studied the anti-tumor activity of its mycelium. The results indicated that the optimum fermentation medium consisted of 2% sucrose, 0.2% peptone, 0.1% KH2PO4, 0.05% MgSO4·7H2O, 0.16% Lonicera japonica petals, 0.18% P fungal elicitor, and 0.21% L. japonica stem. The biomass reached 7.82 ± 0.41 g/l after 15 days of cultivation in the optimized medium, a 142% increase compared with the potato dextrose broth medium, with a 64% reduction in cultivation time. The intracellular alcohol extract had a higher inhibitory effect on A549 and Eca-109 cells than the intracellular water extract, with half-maximal inhibitory concentration values of 2.42 and 2.92 mg/ml, respectively. Graded extraction of the alcohol extract yielded petroleum ether phase, chloroform phase, ethyl acetate phase, and n-butanol phase. Among them, the petroleum ether phase exhibited a better effect than the positive control, with a half-maximal inhibitory concentration of 113.3 ㎍/ml. Flow cytometry analysis indicated that petroleum ether components could induce apoptosis of Eca-109 cells, suggesting that this extracted component can be utilized as an anticancer agent in functional foods. This study offers valuable technical support and a theoretical foundation for promoting the comprehensive development and efficient utilization of P. lonicerae.

Dammarane-type triterpene oligoglycosides from the leaves and stems of Panax notoginseng and their antiinflammatory activities

  • Li, Juan;Wang, Ru-Feng;Zhou, Yue;Hu, Hai-Jun;Yang, Ying-Bo;Yang, Li;Wang, Zheng-Tao
    • Journal of Ginseng Research
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    • v.43 no.3
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    • pp.377-384
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    • 2019
  • Background: Inflammation is widespread in the clinical pathology and closely associated to the progress of many diseases. Triterpenoid saponins as a key group of active ingredients in Panax notoginseng (Burk.) F.H. Chen were demonstrated to show antiinflammatory effects. However, the chemical structures of saponins in the leaves and stems of Panax notoginseng (PNLS) are still not fully clear. Herein, the isolation, purification and further evaluation of the antiinflammatory activity of dammarane-type triterpenoid saponins from PNLS were conducted. Methods: Silica gel and reversed-phase C8 column chromatography were used. Furthermore, preparative HPLC was used as a final purification technique to obtain minor saponins with high purities. MS, NMR experiments, and chemical methods were used in the structural identifications. The antiinflammatory activities of the isolated saponins were assessed by measuring the nitric oxide production in RAW 264.7 cells stimulated by lipopolysaccharides. Real-time reverse transcription polymerase chain reaction was used to measure the gene expressions of inflammation-related gene. Results: Eight new minor dammarane-type triterpene oligoglycosides, namely notoginsenosides LK1-LK8 (1-8) were obtained from PNLS, along with seven known ones. Among the isolated saponins, gypenoside IX significantly suppressed the nitric oxide production and inflammatory cytokines including tumor necrosis $factor-{\alpha}$, interleukin 10, interferon-inducible protein 10 and $interleukin-1{\beta}$. Conclusion: The eight saponins may enrich and expand the chemical library of saponins in Panax genus. Moreover, it is reported for the first time that gypenoside IX showed moderate antiinflammatory activity.

Cell Protective Effects of Enzymatic Hydrolysates of Citrus Peel Pectin (귤피 펙틴 유래 효소적 가수분해물의 세포 보호 효과)

  • Kwon, Soon Woo;Ko, Hyun Ju;Bae, Jun Tae;Kim, Jin Hwa;Lee, Geun Soo;Pyo, Hyeong Bae
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.42 no.1
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    • pp.75-85
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    • 2016
  • Pectin, a naturally occurring polysaccharide, has in recent years attracted considerable attention. Its benefits are increasingly appreciated by scientists and consumers due to its safety and usefulness. The chemistry and gel-forming characteristics of pectin have enabled to be used in pharmaceutical industry, health promotion and treatment. Yet, it has been rarely used in cosmetics because of its incompatibility with many cosmetic ingredients, including alcohols, and unstable viscosity of pectin gels under various pH and salt conditions. However, low-molecular-weight pectin oligomers have excellent biological activities, and depolymerization of pectin to produce cosmetic ingredients would be very useful. In this study, we attempted the development of cosmetic ingredients using pectin with an excellent effect on human skin. We developed a bio-conversion process that uses enzymatic hydrolysis to produce pectin hydrolysates containing mainly low-molecular-weight pectin oligomers. Gel permeation chromatography was used to determined the ratio of hydrolysis. The molecular weight of the pectin hydrolysates obtained varied between 200 and 2,700 Da. The two newly developed low-molecular-weight pectin hydrolysates, LMPH A and B, had higher anti-oxidative activities than pectin or D-galacturonic. Exposure to UVB radiation induces apoptotic cell death in epidermal cells. Annexin V binding and propidium iodide uptake were measured by flow cytometry to evaluate UVB-induced cell death in HaCaT cells. Both LMPH A and B reduced UVB-induced cell death and increased cell proliferation by 22% and 30% at 0.5% concentration respectively, while pectin had no significant activity. In conclusion, this study suggests that the newly developed low-molecular-weight pectin hydrolysates can be used as safe and biologically active cosmetic ingredients.