• Title/Summary/Keyword: Pharmacological effects

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General Pharmacology of AS2-006A, A New Wound Healing Agent (창상치료후보물질 AS2-006A의 일반약리연구)

  • 정혜진;조민경;손문호;강건욱;최성희;김혜정;이애경;박형근;주상섭
    • Toxicological Research
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    • v.16 no.3
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    • pp.211-219
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    • 2000
  • The therapeutic effect of AS2-006A, a derivative of asiaticoside, has been studied and is being developed as a new wound-healing agent. In the present study, the general pharmacological effects on 1) central nervous system, 2) autonomic nervous system, 3) respiratory system, 4) gastrointestinal system. 5) cardiovascular system. and 6) urinary system were assessed in experimental animals and in in vitro models. 1. In vivo animal study: External applications of the 1 % gel ointment of AS2-006A to rats at the doses of 200. 600 or 2000 mg/kg body weight showed no observable pharmacological effects. The effects on the central nervous system were assessed by observation of behavior, hexobarbital-induced sleeping time, pentetrazole-induced convulsion assay, body temperature measurements, and observations on spontaneous activity and catalepsy. The gel ointment exhibited no effects on the cardiovascular system (i.e. blood pressure and heart rate), renal physiology (i.e. urine volume and electrolytes excretion) and gas-trointestinal physiology (i.e. intestinal charcoal propulsion and gastric mucosal irritation). 2. In vitro experiments: The effects of AS2-006A on the physiology of smooth and cardiac muscles were assessed. Muscle contractions were isotonically and isometrically measured in organ chambers using a physiograph. Cumulative additions of AS2-006A (10$^{-9}$ -10$^{-5}$ M) induced no changes in the tension of isolated guinea pig ileum and tracheal muscles. AS2-006A only slightly increased contractility of rat atrial and papillary muscles at 10$^{-2}$ M, which was not statistically different from control. These data showed that the gel ointment of AS2-006A could be externally applied as a wound-healing agent with no potential side effects.

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Radioprotective Potential of Panax ginseng: Current Status and Future Prospectives (고려인삼의 방사선 방어효과에 대한 연구현황과 전망)

  • Nam, Ki-Yeul;Park, Jong-Dae;Choi, Jae-Eul
    • Korean Journal of Medicinal Crop Science
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    • v.19 no.4
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    • pp.287-299
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    • 2011
  • Pharmacological effects of Panax ginseng have been demonstrated in cardiovascular system, endocrine secretion and immune system, together with antitumor, anti-stress and anti-oxidant activities. Modern scientific data show protective effect of ginseng against bone marrow cell death, increased survival rate of experimental animals, recovery of hematopoietic injury, immunopotentiation, reduction of damaged intestinal epithelial cells, inhibition of mutagenesis and effective protection against testicular damages, caused by radiation exposure. And also, ginseng acts in indirect fashion to protect radical processes by inhibition of initiation of free radical processes and thus reduces the radiation damages. The research has made much progress, but still insufficient to fully uncover the action mechanism of ginseng components on the molecule level. This review provides the usefulness of natural product, showing no toxic effects, as an radioprotective agent. Furthermore, the further clinical trials on radioprotection of ginseng need to be highly done to clarify its scientific application. The effective components of ginseng has been known as ginsenosides. Considering that each of these ginsenosides has pharmacological effect, it seems likely that non-saponin components might have radioprotective effects superior to those of ginsenosides, suggesting its active ingredients to be non-saponin series. These results also show that the combined effects of saponin and non-saponin components play an important role in the radioprotective effects of ginseng.

Similarities and Distinctions in the Effects of Metformin and Carbon Monoxide in Immunometabolism

  • Park, Jeongmin;Joe, Yeonsoo;Ryter, Stefan W.;Surh, Young-Joon;Chung, Hun Taeg
    • Molecules and Cells
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    • v.42 no.4
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    • pp.292-300
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    • 2019
  • Immunometabolism, defined as the interaction of metabolic pathways with the immune system, influences the pathogenesis of metabolic diseases. Metformin and carbon monoxide (CO) are two pharmacological agents known to ameliorate metabolic disorders. There are notable similarities and differences in the reported effects of metformin and CO on immunometabolism. Metformin, an anti-diabetes drug, has positive effects on metabolism and can exert anti-inflammatory and anti-cancer effects via adenosine monophosphate-activated protein kinase (AMPK)-dependent and AMPK-independent mechanisms. CO, an endogenous product of heme oxygenase-1 (HO-1), can exert anti-inflammatory and antioxidant effects at low concentration. CO can confer cytoprotection in metabolic disorders and cancer via selective activation of the protein kinase R-like endoplasmic reticulum (ER) kinase (PERK) pathway. Both metformin and CO can induce mitochondrial stress to produce a mild elevation of mitochondrial ROS (mtROS) by distinct mechanisms. Metformin inhibits complex I of the mitochondrial electron transport chain (ETC), while CO inhibits ETC complex IV. Both metformin and CO can differentially induce several protein factors, including fibroblast growth factor 21 (FGF21) and sestrin2 (SESN2), which maintain metabolic homeostasis; nuclear factor erythroid 2-related factor 2 (Nrf2), a master regulator of the antioxidant response; and REDD1, which exhibits an anticancer effect. However, metformin and CO regulate these effects via different pathways. Metformin stimulates p53- and AMPK-dependent pathways whereas CO can selectively trigger the PERK-dependent signaling pathway. Although further studies are needed to identify the mechanistic differences between metformin and CO, pharmacological application of these agents may represent useful strategies to ameliorate metabolic diseases associated with altered immunometabolism.

Anti-Oral Microbial Effect of Ethanol Extract of Angelica gigas Nakai

  • Soon-Jeong Jeong
    • Journal of dental hygiene science
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    • v.24 no.1
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    • pp.54-61
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    • 2024
  • Background: The Korean name for Angelica gigas Nakai (AGN) is Cham-dang-gui, which grows naturally or is cultivated, and its dried roots are used in traditional herbal medicines. The AGN root exert various pharmacological effects. Despite the various pharmacological effects of the AGN root, there are no reports on its anti-oral microbial effects. The purpose of this study was to reveal the anti-oral microbial effect and the microbial and biochemical changes in oral microorganisms according to the concentration of the ethanol extract of AGN (EAGN) root, and to confirm the possibility of using EAGN as a plant-derived functional substance for controlling oral infectious microorganisms. Methods: Disk diffusion test, growth measurement, biofilm formation assay, and measurements of acid production and buffering capacity were performed to confirm the antibacterial effect of EAGN. Results: EAGN showed anti-oral bacterial effects against Streptococcus mutans and Aggregatibacter actinomycetemcomitans at all concentrations, with S. mutans showing a more susceptible effect at concentrations above 5.0 mg/ml and A. actinomycetemcomitans at 3.75 mg/ml. EAGN treatment significantly reduced A. actinomycetemcomitans growth at all concentrations tested. Biofilm formation was significantly reduced at concentrations above 3.75 mg/ml for S. mutans and 2.5 mg/ml for A. actinomycetemcomitans. Acid production in S. mutans and A. actinomycetemcomitans was significantly increased by treatment with EAGN, and the buffering capacities of S. mutans and A. actinomycetemcomitans increased from an EAGN concentration of 3.75 mg/ml and above. Conclusion: EAGN showed anti-oral bacterial effects against both S. mutans and A. actinomycetemcomitans at concentrations above 3.75 mg/ml, which were thought to be related to the inhibition of their growth and biofilm formation. Therefore, EAGN can be used as a safe functional substance derived from medicinal plants owing to its antibacterial effects against S. mutans and A. actinomycetemcomitans.

Research in the antioxidant of Phellinus linteus mycelia

  • Nakamura, Tomoyuki;Akiyama, Yukihito;Matsugo, Seiichi;Shibata, Keiji;Kawagishi, Hirokazu
    • Journal of Photoscience
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    • v.9 no.2
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    • pp.421-423
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    • 2002
  • Phellinus linteus mycelia have many pharmacological effects, although their pharmacological efficacy principles have not been known yet. In the course of screening for biological activity of the extracts of Phellinus linteus mycelia, we found strong antioxidative activity in some fraction of water-insoluble. Therefore, we tried to isolate the active principle(s) from the extract. The isolation of the active compound was guided by superoxide anion radical scavenging activity. As a result, caffeic acid was isolated as an active compound. The IC$\_$50/ of the compound was 3.05 $\mu$g/ml (16.9$\mu$M).

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Identification of a Potential Anticancer Target of Danshensu by Inverse Docking

  • Chen, Shao-Jun;Ren, Ji-Long
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.1
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    • pp.111-116
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    • 2014
  • Objective: To study potential targets of Danshensu via dual inverse docking. Method: PharmMapper and idTarget servers were used as tools, and the results were checked with the molecular docking program autodock vina in PyRx 0.8. Result: The disease-related target HRas was rated top, with a pharmacophore model matching well the molecular features of Danshensu. In addition, docking results indicated that the complex was also matched in terms of structure, H-bonds, and hydrophobicity. Conclusion: Dual inverse docking indicates that HRas may be a potential anticancer target of Danshensu. This approach can provide useful information for studying pharmacological effects of agents of interest.

General Pharmacology of Aspalatone (Aspalatone의 일반약리작용)

  • 이은방;조성익;천선아;장혜옥
    • Biomolecules & Therapeutics
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    • v.8 no.1
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    • pp.99-106
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    • 2000
  • Aspalatone [3-(2-methyl-4proponyl)]-2-acetyloxybenzoate, CAS 147249-33-0) is a compound having an antithrombotic action. General pharmacological properties of aspalatone were studied. Aspalatone had no effect on central nervous system and no anticonvulsant effect up to 1200 mg/kg p.o. However, the compound has hypothermic and analgesic effect. When administered intravenously in rabbits, aspalatone did not affect blood pressure, heat rate and respiration rate and depth, and it did not inhibit transient hypotensive effect of acetylcholine. The compound did not affect isolated guinea-pig ileum and tracheal strip at a concentration of 1${\times}$$10^{-4}$, and did not inhibit histamine-induced contraction of guinea-pig ileum. It also did not affect isolated rat stomach fundus and estrogenated rat uterus at 1${\times}$$10^{-4}$, and did not inhibit contraction produced by acetylcholine or oxytocin. The pupil size and intestinal propulsion were not influenced at a large dose of was shown. The compound showed a slight increase in urine volume and led to decreased excretion of potassium in urine of rats. The results suggest that aspalatone may have no considerable adverse effects in general pharmacological aspect.

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Metabolism of Ginsenosides to Bioactive Compounds by Intestinal Microflora and Its Industrial Application

  • Kim, Dong-Hyun
    • Journal of Ginseng Research
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    • v.33 no.3
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    • pp.165-176
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    • 2009
  • Korean ginseng, which contains ginsenosides and polysaccharides as its main constituents, is orally administered to humans. Ginsenosides and polysaccharides are not easily absorbed by the body through the intestines due to their hydrophilicity. Therefore, these constituents which include ginsenosides Rb1, Rb2, and Rc, inevitably come into contact with intestinal microflora in the alimentary tract and can be metabolized by intestinal microflora. Since most of the metabolites such as compound K and protopanaxatriol are nonpolar compared to the parental components, these metabolites are easily absorbed from the gastrointestinal tract. The absorbed metabolites may express pharmacological actions, such as antitumor, antidiabetic, anti-inflammatory, anti-allergic, and neuroprotective effects. However, the activities that metabolize these constituents to bioactive compounds differ significantly between individuals because all individuals possess characteristic indigenous strains of intestinal bacteria. Recently, ginseng has been fermented with enzymes or microbes to develop ginsengs that contain these metabolites. However, before using these enzymes and probiotics, their safety and biotransforming activity should be assessed. Intestinal microflora play an important role in the pharmacological action of orally administered ginseng.

General Pharmacology of the Active Ingredients of New Antibiotic Bead (CJ-40003) (골수염 치료제인 항생제비드(CJ-40003) 유효성분의 일반약리작용)

  • 김영훈;최재묵;온윤성;연규정;이윤하;김제학;이영수
    • Biomolecules & Therapeutics
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    • v.7 no.1
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    • pp.97-104
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    • 1999
  • A new antibiotic bead, CJ-40003 is a combination of three antibiotics, tobramycin, vancomycin and cefazolin embedded in bone cement, for the treatment of osteomyelitis. To evaluate the general pharmacological properties of CJ-40003, the effects of its active ingredients were investigated in mice, rats, dogs and isolated guinea pig ileum. The combination of three antibiotics (CA) did not affect general behavior, central nervous system, smooth muscles, gastrointestinal system, cardiovascular and respiratory system and water and electrolytes excretion when administered intravenously at the doses of 0.3, 1 and 3 mg/kg, respectively, into experimental animals. The CA had no effect on the contractile response of the isolated guinea pig ileum to various spasmogen at concentrations of 1, 3 and 10 $\mu\textrm{g}$/ml, respectively. In conclusion, the active ingredients of CJ-40003 showed no pharmacological effect in these studies.

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Novel zinc sources as antimicrobial growth promoters for monogastric animals: a review

  • Lei, Xin Jian;Liu, Zhang Zhuang;Park, Jae Hong;Kim, In Ho
    • Journal of Animal Science and Technology
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    • v.64 no.2
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    • pp.187-196
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    • 2022
  • The essentiality of zinc for animals has been recognized over 80 years. Zinc is an essential trace element that is a component of many enzymes and is associated with the various hormones. Apart from the nutritional function, zinc has antimicrobial property and often be supplemented in diets in the quantities greater than which is required to meet the nutritional requirement, especially for weaning pigs. This review will focus on the application of pharmacological zinc and its mechanisms which may be responsible for the effects of zinc on performance and health of monogastric animals. Various novel sources of zinc in non-ruminant animal production will also be discussed. These should assist in more precisely formulating feed to maximize the production performance and to maintain the health condition of monogastric animals.