• Title/Summary/Keyword: Anti-HIV agent(s)

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Identification of anti-HIV and anti-Reverse Transcriptase activity from Tetracera scandens

  • Kwon, Hyeok-Sang;Park, Jung-Ae;Kim, Joo-Hwan;You, Ji-Chang
    • BMB Reports
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    • v.45 no.3
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    • pp.165-170
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    • 2012
  • We report here that an ethanol extract of Tetracera scandens, a Vietnamese medicinal plant, has anti-HIV activity and possesses strong inhibitory activity against HIV-1 reverse transcriptase (RTase). Using a MT-4 cell-based assay, we found that the T. scandens extract inhibited effectively HIV virus replication with an $IC_{50}$ value in the range of 2.0-2.5 ${\mu}g$/ml while the cellular toxicity value (CC50) was more than 40-50 ${\mu}g$/ml concentration, thus yielding a minimum specificity index of 20-fold. Moreover, the anti-HIV efficacy of the T. scandens extract was determined to be due, in part, to its potent inhibitory activity against HIV-1 RTase activity in vitro. The inhibitory activity against the RTase was further confirmed by probing viral cDNA production, an intermediate of viral reverse transcription, in virus-infected cells using quantitative DNA-PCR analysis. Thus, these results suggest that T. scandens can be a useful source for the isolation and development of new anti-HIV-1 inhibitor(s).

A Spirulina maxima-derived peptide inhibits HIV-1 infection in a human T cell line MT4

  • Jang, In-Seung;Park, Sun Joo
    • Fisheries and Aquatic Sciences
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    • v.19 no.9
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    • pp.37.1-37.5
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    • 2016
  • Human immunodeficiency virus (HIV) is the causative agent of acquired immune deficiency syndrome (AIDS). Anti-HIV agents targeting various steps in HIV life cycle have been developed; however, so far, no effective drugs have been found. We show here that a peptide isolated from Spirulina maxima (SM-peptide) inhibits HIV-1 infection in a human T cell line MT4. SM-peptide inhibited $HIV-1_{IIIB}$-induced cell lysis with a half-maximal inhibitory concentration ($IC_{50}$) of 0.691 mM, while its 50 % cytotoxic concentration ($CC_{50}$) was greater than 1.457 mM. Furthermore, the SM-peptide inhibited the HIV-1 reverse transcriptase activity and p24 antigen production. This suggests that SM-peptide is a novel candidate peptide, which may be developed as a therapeutic agent for acquired immunodeficiency syndrome patients.

Inhibitory effects of Korean plant resources on human immunodeficiency virus type 1 protease activity

  • Park, Jong-Cheol
    • Advances in Traditional Medicine
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    • v.3 no.1
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    • pp.1-7
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    • 2003
  • Some Korean plants were found to inhibit HIV-1 protease activity. The extracts of Acanthopanax koreanum (stem bark), Berchemia berchemiaefolia (stem), Berchemia berchemiaefolia (bark), Distylium racemosum (leaves), Distylium racemosum (stem), Lindera erythrocarpa (leaves), Physalis alkekengi var. francheti (root), Platycarya strobilacea (stem), Rodiola rosea (root), Rosa davurica (stem), Syringa dilatata (leaves), Viburnum awabuki (stem) and Viburnum awabuki (leaves) showed significant inhibitory effect against HIV-1 protease. Camelliatannin H from Camellia japonica and uvaol from Cratagus pinatrifida were potent active inhibitors of HIV-1 protease with $IC_{50}$ values of $0.9\;{\mu}M$ and $5.5\;{\mu}M$, respectively. The cure and prevention of AIDS have been a global challenge since it was discovered in the ealy 1980s. However, the development of anti-HIV agent that can effectively treat or prevent this disease are still demanded.

Anti-HIV-1 Viral Activity of Glycyrrhizin (감초탕(甘草湯)의 Human Immunodeficiency Virus-1 억제능(抑制能)에 관(關)한 연구(硏究))

  • Lee, Tae-kyun;Moon, Jun-Joon
    • The Journal of Dong Guk Oriental Medicine
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    • v.1
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    • pp.209-236
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    • 1992
  • The microculture XTT antiviral assay method is used to quantitate HIV-1 induced cytopathic effects as modulated by test substances. This relatively simple assay facilitated the safe and rapid determination of in vitro antiviral activity of selected chemicals as well as direct cytotoxicity. This experiment also confirmed that this system measures infection and subsequent viral replication in target cells and XTT formazan formations correlated with the accumulation of extracellular virions, as measured by quantitative HIV-1 induced syncytium foramtion. The present results with Glycyrrhizin using this in vitro culture system demonstrated that effective dose, EC50(the concentration at which increases XTT formazan production in infected cultures to 50% of that in untreated, uninfected controls) was 250ml. As comparison, AZT was included in this experiment and demonstrated that EC50 AZT of was 0.05g/ml, approximately 5,000 times more potent than Glycyrrhizin based on EC50 ratio's alone. However, this potency is limited by severe cytotoxicity of AZT, while Glycyrrhizin is approximately 16 times less toxic(IC50 of Glycyrrhizin 800 and AZT 51 g/ml). While AZT's anti-HIV-1 viral activity is mediated by inhibition of reverse transcriptase of the virus, Glycyrrhizin faild to demonstrate any inhibitory activity against reverse transcriptase. Further study is necessary in order to understand the precise mechanisms of Glycyrrhizin action against HIV-1 viruses. Althouth Glycyrrhizin is less effective antiviral agent than AZT, much less toxicity of Glycyrrhizin is desirable in terms of chronic treatment. Combination treatment of AZT and Glycyrrhizin may be therapeutically beneficial. Clinical effectiveness of two drug combination therapy for AIDS patient is unknown at this time. However, this experimental investigation presents the scientific rational basis for such therapeutic approach.

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A Novel Approach for Sericin-Conjugated Silver Nanoparticle Synthesis and Their Potential as Microbicide Candidates

  • Lv, Xiaowen;Wang, Huanru;Su, Airong;Chu, Ying
    • Journal of Microbiology and Biotechnology
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    • v.28 no.8
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    • pp.1367-1375
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    • 2018
  • Silver nanoparticles have been widely applied for biomedical areas owing to their potent antiviral and antibacterial activities. Synthesis of silver nanoparticles using biomacromolecules is more efficient, environment-friendly, and cost-saving compared with the traditional approach. In this paper, a novel approach was developed to establish a reaction system with $Ag^+-BH4^--sericin$ to synthesize silver nanoparticles conjugated to sericin (AgNPs-Sericin). Sericin could be as a good dispersant and stabilizing agent, which is able to modify nanoscaled AgNPs, the average diameter of which was only $3.78{\pm}1.14nm$ prepared in a 0.3 mg/ml sericin solution. The characterizations of the AgNPs-Sericin were determined by FTIR, thermogravimetry, and XRD analyses. The results showed that the synthesized AgNPs conjugated with sericin as organic phase. Via SAED and XRD analysis, we showed that these AgNPs formed polycrystalline powder with a face-centered cubic structure of bulk metals. Moreover, we investigated the antiviral and antibacterial activities of AgNPs-Sericin, and the results showed that AgNPs-Sericin exhibited potent anti-HIV-1 activity against CCR5-tropic and CXCR4-tropic strains, but no significant cytotoxicity was found toward human genital epithelial cells compared with free silver ions, which are accepted as a commonly used potent antimicrobial agent. Moreover, its antibacterial activity was determined via flow cytometry. The results showed that AgNPs-Sericin could suppress gram-negative (E. coli) and gram-positive (S. aureus) bacteria, but more was potent for the gram-negative one. We concluded that our AgNPs-Sericin could be a potential candidate as a microbicide or antimicrobial agent to prevent sexually transmitted infections.

Changing Patterns of Communicable Diseases in Korea (우리나라 전염성 질환의 변화 양상)

  • Lim, Hyun-Sul
    • Journal of Preventive Medicine and Public Health
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    • v.38 no.2
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    • pp.117-124
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    • 2005
  • Before twentieth centuries and during early twentieth centuries, communicable diseases were the major cause of morbidity and mortality in Korea. But reliable data are not available. After 1975, the overall morbidity and mortality from communicable diseases, rapidly declined. Recently many new pathogenic microbes were recognized: L. monocytogenes, Hantaan virus, Y. pseudotuberculosis, P. multocida, L. pneumophilia, Human immunodeficiency virus (HIV), G. seoi, H. capsulatum, C. burnetii, V. cholerae O139, C. parvum, F. tularensis, E. coli O157:H7, B. burgdorferi, S. Typhimurium DT104, Rotavirus, hepatitis C virus and so on. Since the first HIV infection recognized in 1985, the reported cases of infection and deaths from HIV/AIDS have been steady increased each year. Legionnaire's disease, E. coli O157:H7 colitis, listeriosis and crytosporidiasis have been occurring just sporadically among immunocompromized cases. Many re-emerging communicable diseases were occurred in Korea: leptospirosis, malaria, endemic typhus, cholera, tsutsugamushi disease, salmonellosis, hepatitis A, shigellosis, mumps, measles, acute hemorrhagic conjunctivitis, brucellosis and so on. Leptospirosis and tsutsugamushi diseases have been noticed as major public health problems since 1980s. The malaria that had been virtually disappeared for a decade has reappeared from 1993 with striking increase of patients in recent 3-4 years. The distributions of salmonella and shigella serotypes have been changed a lot in recent few decades. Furthermore rapid emergence of antibiotic-resistant bacterial strains induces more difficult and complex problems in control of communicable diseases. We must recognize on the importance of environment and ecosystem conservation and careful prescription of anti-microbial agent in order to prevent communicable diseases.

Pharmacokinetic analysis for the development of new potent anti-HIV-1 agents, the KR-V series (새로운 항HIV-1제, KR-V series의 개발을 위한 약물동태연구)

  • Lee, Young-mi;Kim, Jin-suk;Han, Sang-seop;Shin, Ho-chul
    • Korean Journal of Veterinary Research
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    • v.40 no.3
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    • pp.471-478
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    • 2000
  • The pharmacokinetic properties of KR-V compounds, recently developed as new anti-HIV agents, were studied after i.v. and p.o. administration in rats. The concentrations of the KR-V series were determined in rat plasma using an high-performance liquid chromatography (HPLC)-UV detection system. Of the 19 KR-V compounds investigated in the present study, only KR-V 3, 10, 14, 16 and 18-1 showed oral bioavailability. The plasma concentration-time data could be adequately described by an one-compartment open model. In the i.v. kinetic study (10mg/kg), the CLt of KR-V 3, 10, 14 and 16 (>4L/hr/kg) were significantly higher than that of KR-V 18-1 (1.1 L/hr/kg). The AUC of KR-V 18-1 was greater ($8.97{\mu}g{\cdot}hr/ml$) than that of the other compounds, but the Vd (0.58 L/kg) was lower. In the p.o. kinetic study (50mg/kg), although the t-1/2 of KR-V 18-1 was shorter than that of the other compounds, the AUC ($3.659{\mu}g{\cdot}hr/ml)$ and $C_{max}(1.891{\mu}g/ml$) were markedly higher. In a seperated in vitro experiment, only KR-V 18-1, of the 5 compounds with bioavailibility, exhibits potent activity against HIV-1 mutant strains. Therefore, KR-V 18-1 is expected to become a new potent anti-AIDS drug candidate/lead compound.

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