• Title/Summary/Keyword: active ingredients

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Mechanism of $Ca^{2+}$ -activated $Cl^-$ Channel Activation by Ginsenosides in Xenopus Oocytes

  • Park, Seok;Jung, Se-Yeon;Park, Seong-Hwan;Ko, Sung-Ryong;Hyewon Rhim;Park, Chul-Seung;Nah, Seung-Yeol
    • Journal of Ginseng Research
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    • v.24 no.4
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    • pp.168-175
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    • 2000
  • Relatively little is known about the signaling mechanism of ginseng saponins (ginsenosides), active ingredients of ginseng, in non-neuronal cells. Here, we describe that ginsenosides utilize a common pathway of receptor-mediated signaling pathway in Xenopus oocytes: increase in intracellular $Ca^{2+}$ concentration via phospholipase C (PLC) and $Ca^{2+}$ mobilization. Ginsenosides induced a marked and robust artivation of $Ca^{2+}$-activated Cl- channels in Xenopus oocytes. The effect of ginsenosides was completely reversible, in a dose-dependent manner with EC$_{50}$ of 4.4 $\mu\textrm{g}$/mi, and specifically blocked by niflumic acid, an inhibitor of $Ca^{2+}$-activated Cl- channel. Intracellular injection of BAPIA abolished the effect of ginsenosides. Intracellular injection of GTP${\gamma}$S also abolished the effect of ginsenosides. The effect of gin senosides on $Ca^{2+}$-activated Cl- currents was greatly reduced by the intracellular injection of heparin, an IP$_3$ receptorantagonist or the pretreatment of PLC inhibitor. These results indicate that ginsenosides activate endogenous $Ca^{2+}$-activated Cl- channels via the activation of PLC and the release of $Ca^{2+}$ from the IP$_3$-sensitive intracellular store following the initial interaction with membrane component(s) from extracellular side. This signaling pathway of ginsenosides may be one of the action mechanisms for the pharmacological effects of ginseng.ts of ginseng.

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Development of Chitosan Coated Solid Lipid Nano-particles Containing 7-Dehydrocholesterol (7-디하이드로콜레스테롤을 함유한 키토산 코팅 처리 Solid Lipid Nano-particle의 개발에 관한 연구)

  • Lee Geun-Soo;Kim Tae-Hoon;Lee Chun-Il;Pyo Hyeong-Bae;Choe Tae-Boo
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.31 no.2 s.51
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    • pp.141-146
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    • 2005
  • Unstable cosmetic active ingredients could rapidly break down in chemical and photochemical process. Therefore, it has become a very important issue to encapsulate active ingredient for the stabilization. 7-Dehydrocholesterol (7-DHC), a precursor of vitamin $D_3$, has been shown to increase levels of protein and mRNA for heat shock protein in normal human epidermal keratinocytes. However, topical dermal application of 7-DHC is restricted due to its poor solubility and chemical unstability. In this study, 7-DHC was incorporated into nano-emulsion (NE), solid lipid nano-particle (SLN), and chitosan coated solid lipid nano-particle (CASLN), respectively. In order to prepare NE and SLN dispersion, high-pressure homogenization at temperature above the melting point of lipid was used Hydrogenated lecithin and polysorbate 60 were used as stabilizer for NE and SLN. CASLN was prepared by high speed homogenizing after adding chitosan solution to the SLN dispersion and showed positively charged particle properties. Decomposition rate of 7-DHC in NE, SLN and CASLN was studied as a function of time at different temperature. Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) studies were performed to characterize state of lipid modification. It appeared that CASLN is the most effective to stabilize 7-DHC and may be used for a useful topical dermal delivery system.

Putative multiple reaction monitoring strategy for the comparative pharmacokinetics of postoral administration Renshen-Yuanzhi compatibility through liquid chromatography-tandem mass spectrometry

  • Sun, Yufei;Feng, Guifang;Zheng, Yan;Liu, Shu;Zhang, Yan;Pi, Zifeng;Song, Fengrui;Liu, Zhiqiang
    • Journal of Ginseng Research
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    • v.44 no.1
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    • pp.105-114
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    • 2020
  • Background: Exploring the pharmacokinetic (PK) changes of various active components of single herbs and their combinations is necessary to elucidate the compatibility mechanism. However, the lack of chemical standards and low concentrations of multiple active ingredients in the biological matrix restrict PK studies. Methods: A putative multiple reaction monitoring strategy based on liquid chromatography coupled with mass spectrometry (LC-MS) was developed to extend the PK scopes of quantification without resorting to the use of chemical standards. First, the compounds studied, including components with available reference standard (ARS) and components lacking reference standard (LRS), were preclassified to several groups according to their chemical structures. Herb decoctions were then subjected to ultrahigh-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry analysis with appropriate collision energy (CE) in MS2 mode. Finally, multiple reaction monitoring transitions transformed from MS2 of ultrahigh-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry were used for ultrahigh-performance liquid chromatography coupled with triple quadrupole mass spectrometry to obtain the mass responses of LRS components. LRS components quantification was further performed by developing an assistive group-dependent semiquantitative method. Results: The developed method was exemplified by the comparative PK process of single herbs Radix Ginseng (RG), Radix Polygala (RP), and their combinations (RG-RP). Significant changes in PK parameters were observed before and after combination. Conclusion: Results indicated that Traditional Chinese Medicine combinations can produce synergistic effects and diminish possible toxic effects, thereby reflecting the advantages of compatibility. The proposed strategy can solve the quantitative problem of LRS and extend the scopes of PK studies.

Functional Characterization of the Extracts from Nipa Palm, Molokhia, and Finger Root for Cosmetic Ingredients (니파팜, 몰로키아, 핑거루트 추출물의 화장품 소재로서의 기능적 특성 분석)

  • Jun, Yue Jin;Lee, Sohyun;Heo, Sojeong;Jin, Byung Suk
    • Journal of the Korean Applied Science and Technology
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    • v.36 no.3
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    • pp.821-829
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    • 2019
  • This study was conducted to evaluate the applicability of the extracts from nipa palm, molokhia, and finger root in functional cosmetics as a natural active ingredient. The extracts were obtained through the processes of heating under reflux with ethanol, filtration, concentration, and freeze-drying. UV absorption and blocking effects of the extracts were examined by using the UV-vis spectrophotometer equipped with an integrating sphere. Antioxidant activity and its stability between the extracts were compared using the 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assay. Also, total polyphenol content in the extracts was determined quantitatively using the Folin-Ciocalteu reagent, with gallic acid as the standard. Antibacterial activity of the extracts was investigated by the disc diffusion test against Staphylococcus aureus (gram-positive) and Escherichia coli (gram-negative). Finally, collagenase inhibitor assay was performed to examine the anti-wrinkle effect of the extracts. From the results of this study, the extract of nipa palm showed the potential for use in cosmetics as an antioxidant and anti-wrinkle agent, and the extract of finger root as a sunscreen and antibacterial agent.

Protective Effects of Traditional Korean Medicine Preparations, Herbs, and Active Compounds on the Blood-brain Barrier in Ischemic Stroke Models (허혈성 뇌졸중 모델에서 혈액-뇌 장벽에 보호효과를 나타내는 한약처방, 한약재 및 활성화합물)

  • Shin, Su Bin;Jang, Seok Ju;Lee, Na Gyeong;Choi, Byung Tae;Shin, Hwa Kyoung
    • Journal of Life Science
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    • v.32 no.7
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    • pp.550-566
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    • 2022
  • Stroke is among the leading causes of death and long-term physical and cognitive disabilities worldwide, affecting an estimated 15 million people annually. The pathophysiological process of stroke is complicated by multiple and coordinated events. The breakdown of the blood-brain barrier (BBB) in people with stroke can significantly contribute to the development of ischemic brain injury. Therefore, BBB disruption is recognized as a hallmark of stroke; thus, it is important to develop novel therapeutic strategies that can protect against BBB dysfunction in ischemic stroke. Traditional medicines are composed of natural products, which represent a promising source of new ingredients for the development of conventional medicines. Indeed, several studies have shown the effectiveness of Korean medicine on stroke, highlighting the value of Korean medicinal treatment for ischemic stroke. This review summarizes the current information and underlying mechanisms regarding the ameliorating effects of the formula, decoction, herbs, and active components of traditional Korean medicine on cerebral ischemia-induced BBB disruption. These traditional medicines were shown to have protective effects on the BBB in many cellular and animal ischemia models of stroke, and experiments in various animal species, such as mice and rats. In addition, they showed brain-protective effects by protecting the BBB through the regulation of tight junction proteins and matrix metalloproteinase-9, reducing edema, neuroinflammation, and neuronal cell death. We hope that this review will help promote further investigation into the neuroprotective effects of traditional Korean medicines and stimulate the performance of clinical trials on Korean herbal medicine-derived drugs in patients with stroke.

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.

Comparative Evaluation of Biological Activities and Active Compounds of Some Invasive Alien Plants (주요 생태계 교란 외래식물의 생리활성 비교 평가 및 유효성분)

  • So Jin Kim;Min Gun Kim;Kyung-Hwan Boo;Chang Sook Kim
    • Korean Journal of Plant Resources
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    • v.36 no.4
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    • pp.264-274
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    • 2023
  • To evaluate functional biomaterials of 5 invasive alien plants, total polyphenol and flavonoid contents, antioxidant activity, anti-inflammatory activity, and antibacterial effect were measured. The total polyphenol and flavonoid contents of the extracts were in the order of Rumex acetosella L. > Hypochaeris radicata L. ≥ Lactuca scariola L. > Humulus japonicus Siebold & Zucc. ≥ Solanum viarum Dunal. The DPPH and ABTS radical scavenging activities of the extract were the highest in R. acetosella and correlated well with the total polyphenol contents. In RAW 264.7 cells stimulated with lipopolysaccharide (LPS), nitric oxide (NO) and prostaglandin E2 (PGE2) production inhibitory effect of the extracts (100 ㎍ SE/mL) were 20~60% and 10~70%, respectively, showing the highest inhibitory effect in R. acetocella. The extracts of R. acetosella, H. japonicus and S. viarum showed antibacterial activity against food poisoning-causing microorganisms such as Bacillus subtilis, Escherichia coli, Vibrio parahaemolyticus and Vibrio vulnificus. Furthermore, the H. japonicus extract was found to have effective antibacterial activity against oral microorganisms such as Enterococcus faecalis, Lacticaseibacillus casei, Rothia dentocariosa, Staphylococcus epidermidis and Streptococcus mutans, and its major active ingredients were predicted to be pentadecylic acid, palmitic acid and clionasterol. These results suggest that alien plants have potential as biomaterials with antioxidant, anti-inflammation and antibacterial effects.

The Application of Entomopathogenic Fungi Metarhizium anisopliae, Beauveria bassiana, and Trichoderma harzianum for Coptotermes curvignathus and Cryptotermes cynocephalus Termite Control in Indonesia

  • Niken SUBEKTI;Ari SUSILOWATI;Elizabeth Novi KUSUMANINGRUM;Anita FADHILA;Sania SALSABILA;Citra Anisah ZAHRA;Nasiha Al SABRINA;Ikhsan GUSWENRIVO;Yayan SANJAYA;Cepi KURNIAWAN;Apri Heri ISWANTO;Mia MIRANTI
    • Journal of the Korean Wood Science and Technology
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    • v.52 no.3
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    • pp.262-275
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    • 2024
  • In Indonesia, Coptotermes curvignathus Holmgren and Cryptotermes cyanocephalus Light termite attacks can damage wood and causing losses of 8.7 trillion rupiah per year. Wood treatment and soil barrier are very important to protect structures and their components from termite infestation. The application of synthetic chemicals that pose risks to the environment and human health. The growing movement to replace these chemicals with new termiticides that are safe for the environment in place of persistent organic pollutants. Efficacy performance in entomopathogenic fungi spores such as that produce decanoic acid, hexadecanoic acid, palmitic acid, and octadecadienoic acid are potential compounds that provide for ecofriendly termite control. Entomopathogenic fungal spores from Metarhizium anisopliae, Trichoderma harzianum, and Beauveria bassiana, as the active ingredient were formulated with nanocellulose was added as an inert ingredient to which helped to deliver the active ingredients on controlling the target pest, and enhance the utility ability of the product fungi to control termites. The mortality of these termites successively entomopathogenic fungi was the main cause of death. The higher concentrations being associated with of nanocellulose used affect increased the number of termites mortality. M. anisopliae paired with 60% nanocellulose concentrate was the best percentage for yielded the greatest C. curvignathus and C. cynocephalus termite control. In the field testing, M. anisopliae provided better, it showed the finest result of termite control rather than B. bassiana and T. harzianum. The results of the research indicate that entomopathogenic fungi can be used for Pest Control Management as the subterranean termite and drywood termite control.

Effects of Compositions of Saponin Fraction from Korean Red Ginseng in the Relaxation of Rabbit and Rat Corpus Cavernosum (토끼와 흰쥐 음경해면체 이완작용에 미치는 홍삼사포닌 분획별 효과)

  • Choi Young Deuk;Park Jin Ah;Choi Hyung Ki;Nam Ki Yeul
    • Journal of Ginseng Research
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    • v.23 no.1 s.53
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    • pp.13-20
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    • 1999
  • We previously reported that Korean red ginseng (KRG) has a relaxation effect on the smooth muscles of corpus cavernosum via nitric oxide (NO) pathway and calcium and potassium channels. However, it is suggested that the active ingredients of KRG might be different depending on the sources of preparation, and there might be differences in actions for different compositions. We first investigated the composition of KRG saponins according to the extractions of the various sources of KRG, then with these extractions the relaxation effects were evaluated in vitro and hemodynamical in vivo using New Zealand white rabbit and rat corpus cavernosum. The total compositions of ginsenoside $(G-Rb_1,\;-Rb_2,\;-Rc,\;-Rd,\;G-Re,\;-Rf,\;-Rg_1)$ in fractionated KRG saponin designated as TS-1, TS-2, TS-3 were $41\%,\;40\%,\;and\;62\%,$ respectively, and the ratios of PD saponin and PT saponin (PD/PT) were 1,55, 1.72, 2.25, and 2.61, the values of which were statistically significant. In vitro studies using the rabbit corpus cavernosal muscle strips, the KRG saponin relaxed cavernosal strips in a dose-dependent manner, and same results were observed in in vivo studies, that KRG saponin increased the intracavernosal pressure in the rat. There was difference in the efficacy according to fractionation techniques. The differences in the total contents of ginsenosides did not affect relaxation, rather PT saponin content was statistically related to the degree of cavernosal relaxation, and this action presumed to be mediated by NO pathway and calcium and potassium channels. In conclusion, KRG exerts relaxation which is a key step in erection via combination of effects on NO system or calcium and potassium channels. The efficacy of this action is different to the sources of ginseng, which is affected by the different composition of ginsenosides $(G-Rb_1,\;-Rb_2,\;-Rc,\;-Rd,\;G-Re,\;-Rf,\;-Rg_1).$ Thus the further studies on the active ingredients such as minor ginsenosides and non-saponin components of red ginseng with maximum potency should be sought.

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