• 제목/요약/키워드: Anti-HIV activity

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Friend Anemia Virus에 감염된 BALB/c 생쥐를 이용한 항AIDS약물의 생체내 약효검색 (In Vivo Screening Method for the Anti-AIDS Drugs in the BALB/c Mice Inoculated by Anemia Strain of Friend Virus)

  • 안형수;염윤기;장영수
    • 약학회지
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    • 제39권6호
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    • pp.622-630
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    • 1995
  • Inoculation of Friend anemia virus, which was a Kind of retro virus such as HIV, results splenomegaly, anemia, the increase of WBC counts and reverse transcriptase activity in serum. These results were due to the inhibition of the differentiation of erythroid progenitor cell by the FVA at the spleen. Using these as index of antiviral effects, we pursued the establishment of in vivo screening method for the new anti-ADS drugs. Among zidovudine, didanosine and zalcitabine, which were already approved as anti-AIDS drugs, treatment of zidovudine for 18 days in BALB/c mice inoculated with Friend anemia virus resulted the most potent inhibitory effects on the splenomegaly, the increase of WBC counts and reverse transcriptase activity, but did not recovered the anemia due to the tomcity of zidovudhie itself on the bone marrow. The antiviral effects of zidovudine was reduced in case of zidovudine treatment 7 days after Friend anemia virus inoculation. These results suggested that the sooner treatment of zidovudine would be better improved when the virus was inoculated. Human recombinant interferon itself .alpha. did not showed the antiviral activity against Friend anemia virus and did not also affected the antiviral activity of zidovudine. These results suggested that Friend anemia virus would be used as a tool in vivo screening method for the Lobster of reverse transcriptase.

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Pseudo type HIV-1 Particles Carrying CD4

  • Park, Seung-Won;Kim, Tai-Gyu;You, Ji-Chang;Schubert, Manfred;Paik, Soon-Young
    • 대한바이러스학회지
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    • 제30권1호
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    • pp.83-99
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    • 2000
  • A defective HIV-1 helper virus DNA, pHyPC, was assembled by deleting the RNA packaging signal, env, nef and the 3'LTR sequences. HIV-1 like virus particles that carry the HIV-1 receptor, CD4 were generated by co expression of pHyPC and plasmid DNAs encoding different chimeric CD4 proteins. The CD4 particles, sharing the CD4 ectodomain, precisely fused to different membrane anchors. CD4(+) particles specifically bound to HIV-1 Env expressing cells, but any signs of infection into these cells were not detected. Binding was only partially blocked by either polyclonal anti-CD4 antibodies or by high concentrations of soluble CD4. Surprisingly, CD4(+) particles also adsorbed to HeLa, CHO, NIH3T3 and COS-7 cells in the absence of HIV-1 Env expression. Adsorption was comparable in strength and speed to the highly specific CD4-Env interaction. CD4(-) particles exhibited only background levels of binding. Cell binding was CD4. dependent, but it was independent of the cell type from which the CD4(+) particles originated. Interestingly, CD4-dependent/Env-independent binding was only found when CD4 was present on virus particles. This suggests that the micro-environment of CD4 on virus particles uniquely expose this new cell binding activity. Its high affinity could explain in part why infection of Env(+) cells by CD4(+) particles was not detected. Further experiments will be required to evaluate whether this strong membrane interaction could represent one step in the multiple-step viral entry process.

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

  • 이영미;김진석;한상섭;신호철
    • 대한수의학회지
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    • 제40권3호
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    • pp.471-478
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    • 2000
  • 새로운 항HIV 후보물질인 19개의 KR-V 경구제제의 생체이용률을 평가하기 위해 랫드에서 정맥 및 경구투여후 약물동태를 연구하였다. 혈장내 KR-V 화합물들의 검출은 HPLC-UVD 법을 이용하여 분석하였다. 19개 KR-V series 중 KR-V 3, 10, 14, 16 및 18-1만이 랫드에서 경구로 흡수되어 생체이용성을 나타내었다. 10mg/kg의 정맥투여후 약물 통태 연구에 있어서는 5개물질, KR-V3, 10, 14, 16 및 18-1의 소실 반감기는 서로 비슷하였으나 KR-V 3, 10, 14 및 16의 총청소율($CL_{total}$, >4L/hr/kg)은 KR-V 18-1(1.1L/hr/kg) 보다 유의성있게 높았다. KR-V 3, 10, 14 및 16에 비해 KR-V3 18-1이 혈중곡선하면적(AUC, $8.97{\mu}g{\cdot}hr/ml$)은 크고 겉보기분포용적(Vd, 0.58L/kg)은 적었다. 50mg/kg의 경구투여후 약물동태 연구에 있어서는 KR-V 18-1의 반감기가 다른 4개의 물질에 비해 비록 짧았지만 경구 AUC($3.659{\mu}g{\cdot}hr/ml$), 최고혈중농도($C_{max}$, $1.891{\mu}g/ml$) 는 현저히 높았다. 또한 별도의 in virus 실험결과 생체이용률을 나타낸 이들 5개의 물질들 중 KR-V 18-1만이 HIV-1 돌연변이종(mutants)에 대한 억제효과를 나타내었다. 따라서 KR-V 18-1이 항에이즈(AIDS)제의 새로운 후보물질 혹은 선도물질로서 가능성이 기대되었다.

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New Triterpenoids from the Fruits of Schisandra wilsoniana and Their Biological Activities

  • Gao, Xue-Mei;Li, Yun-Qi;Shu, Li-Dan;Shen, Yan-Qiong;Yang, Li-Ying;Yang, Liu-Meng;Zheng, Yong-Tang;Sun, Han-Dong;Xiao, Wei-Lie;Hu, Qiu-Fen
    • Bulletin of the Korean Chemical Society
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    • 제34권3호
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    • pp.827-830
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    • 2013
  • Investigation of an organic extract of the fruits Schisandra wilsoniana led to the isolation of two new highly oxygenated nortriterpenoids, named schilancidilactones V-W (1-2). Their structures were elucidated by spectroscopic evidence. Compounds 1-2 feature a double bond between C-7 and C-8 compared with related known nortriterpenoids isolated from the genus Schisandra. Compounds 1 and 2 were tested for their anti-HIV-1 activities and cytotoxicity. The results revealed that compounds 1 and 2 showed moderate anti-HIV-1 activities with $EC_{50}$ 3.05 and 2.87 ${\mu}g/mL$, respectively, and compound 1 showed high cytotoxicity against KB and MDA-MB-231 cell with $IC_{50}$ values of 3.18 and 5.22 ${\mu}M$, respectively.

Interaction of HIV-1 Core p24 Antigen with Human Monocytic Cell Line THP1 Results in TNF-${\alpha}$ Dependent Secretion of Matrix Metalloproteinase-9

  • Sung, Ji-Hye;Yoo, Seung-Hee;Park, Hae-Kyung;Chong, Young-Hae
    • 대한미생물학회지
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    • 제35권1호
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    • pp.9-18
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    • 2000
  • Immunological mechanisms involving the release of inflammatory factors by HIV-1 infected microglia in the brain have been implicated in the pathogenesis of HIV dementia (HIVD). Since the regulation of matrix metalloproteinases (MMPs) activity can be influenced by variety of inflammatory mediators, this study was undertaken to look for a correlation between the MMP-9 release and the production of TNF-${\alpha}$ in response to HIV-1 p24 in the human monocyte cell line THP-1 as a model for microglia. First, it was shown that HIV-l core p24 antigen induced THP-1 to secrete MMP-9 in a dose response manner while it elicited a little effect on MMP-2 release in human astroglial cell line T98G. Next, it was found that p24 induced THP-1 to secrete TNF-${\alpha}$ without prior differentiation into macrophages by phorbol myristate acetate (PMA) treatment. Furthermore, anti-TNF-${\alpha}$ neutralizing antibodies significantly blocked p24-induced MMP-9 release in a dose dependent manner. Our data indicate that p24 antigen induces monocytic MMP-9 release by triggering up-regulation of TNF-${\alpha}$ secretion.

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An Efficient Synthesis of 4'-Vinylated Carbocyclic Nucleoside Analogues via Two Directional Ring-closing Metathesis

  • Li, Hua;Hong, Joon-Hee
    • Bulletin of the Korean Chemical Society
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    • 제29권5호
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    • pp.993-997
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    • 2008
  • Two directional ring-closing metathesis (RCM) was applied successfully to the synthesis of 4'-vinylated carbocyclic nucleoside analogues from the trivinyl intermediate 12, which was readily made using a sequential Claisen rearrangement and ring-closing metathesis (RCM) starting from Weinreb amide 5. An antiviral evaluation of the synthesized compounds against various viruses such as HIV, HSV-1, HSV-2 and HCMV revealed that the guanine analogue 20 have moderate anti-HIV activity in the MT-4 cell line ($EC_{50}$ = 10.2 $\mu$ M).

Immunostimulatory Activity of Syneilesis palmata Leaves through Macrophage Activation and Macrophage Autophagy

  • Jeong Won Choi;Hyeok Jin Choi;Gwang Hyeon Ryu;Seung Woo Im;Jae Won Lee;Jin Boo Jeong
    • 한국자원식물학회:학술대회논문집
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    • 한국자원식물학회 2023년도 임시총회 및 춘계학술대회
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    • pp.44-44
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    • 2023
  • Syneilesis palmata (SP) has been used as a traditional medicinal plant and vegetable. SP was reported to exert pharmacological activities such as anti-inflammation, anti-cancer, and anti-HIV. However, there are no studies on the immunostimulatory activity of SP. Thus, in this study, we report that S. palmata leaves (SPL) induce the activation of macrophages. An increase in both secretions of immunostimulatory mediators and phagocytotic activity was observed in SPL-treated RAW264.7 cells. However, this was reversed by inhibition of TLR2/4. In addition, the p38 inhibition reduced the SPL-mediated secretion of immunostimulatory mediators, and the SPL-mediated p38 activation was blocked by the TLR2/4 inhibition. SPL augmented both p62/SQSTM1 and LC3-II. TLR2/4 inhibition blocked the SPL-mediated increase of p62/SQSTM1 and LC3-II. These findings indicate that SPL may activate macrophages through TLR2/4-dependent p38 activation and activate autophagy through TLR2/4 stimulation.

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인신매매와 관련된 국제경제, HIV, 그리고 비인간적 문제들에 대한 담론: 네팔여성들에 대한 사례제시를 중심으로 (A discussion on the issues of human trafficking and global economy, HIV, and inhumanity: A case study of Nepal women)

  • 장덕형
    • 시큐리티연구
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    • 제46호
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    • pp.171-187
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    • 2016
  • 인신매매는 오늘날 지구촌에서 급속히 발전하는 지하산업이자 범죄 행위이다. 세계 일부 기업들의 해외 법인은 종종 이러한 성매매 산업에 참여하여 인신매매에 필요한 비용을 지불하는 등 범죄조직의 운영 및 수익에 관여할 뿐만 아니라 지하경제의 투자자금 생성에 깊은 관련이 있다. 이는 불법적 경제의 조성에 인신매매를 통한 성매매가 심각한 위험이라는 것을 반증한다. 또한 전 세계 윤락녀의 56% 정도가 HIV 혹은 AIDS를 가지고 있으며 성매매는 AIDS 감염의 원인이 되고 있는 등 수많은 사람들이 성매매 산업과 접촉하면서 매일 HIV와 다른 질병에 감염되어 확산되고 있어 성매매를 위한 인신매매가 가져오는 보건의 문제 역시 심각한 문제로 인식되고 있다. 그러나 이러한 성매매를 위한 인신매매가 내포하고 있는 심각한 문제는 다양하지만, 일부 국가에서 보이는 바와 같이 정부와 정책 결정자들에게 성매매는 관심 밖의 문제로 외면당하고 학문적 논의에서도 미진한 부분이 되고 있다. 따라서 성매매를 위한 인신매매와 관련된 경제적인 파장과 보건 및 질병에 관한 연구가 매우 필요하다. 이에 따라 이 연구는 성매매를 위한 인신매매와 관련된 선행연구들을 분석하고, 네팔에서의 성매매의 실상을 파악하기 위한 인신매매에 대한 사례분석을 제시하고자 한다. 그리고 이 연구의 결론과 논의부분에서는 세계 여러 나라는 성 매매 산업을 감축하기 위한 정책과 국제사회의 공조가 필요한 부분 등의 정책적 부분에 대한 내용을 논의하고 있다.

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Neuronal injury in AIDS dementia: Potential treatment with NMDA open-channel blockers and nitric oxide-related species

  • Lipton, Stuart A.
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 1996년도 춘계학술대회
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    • pp.19-29
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    • 1996
  • The neurological manifestations of AIDS include dementia, encountered even in the absence of opportunistic superinfection or malignancy. The AIDS Dementia Complex appears to be associated with several neuropathological abnormalities, including astrogliosis and neuronal injury or loss. How can HIV-1 result in neuronal damage if neurons themselves are only rarely, if ever, infected by the vitus\ulcorner In vitro experiments from several different laboratiories have lent support to the existence of HIV- and immune-related toxins. In one recently defined pathway to neuronal injury, HIV-infected macrophages/microglia as well as macrophages activated by HIV-1 envelope protein gp120 appear to secrete excitants/neurotoxins. These substances may include arachidonic acid, platelet-activating factor, free radicals (NO - and O$_2$), glutamate, quinolinate, cysteine, cytokines (TNF-${\alpha}$, IL1-B, IL-6), and as yet unidentified factors emanating from stimulated macrophages and possibly reactive astrocytes. A final common pathway for newonal suscepubility appears to be operative, similar to that observed in stroke, trauma, epilepsy, and several neurodegenerative diseases, including Huntington's disease, Parkinson's disease, and amyotrophic lateral sclerosis. This mechanism involves excessive activation of N-methyl-D-aspartate (NMDA) receptor-operated channels, with resultant excessive influx of Ca$\^$2+/ leading to neuronal damage, and thus offers hope for future pharmacological intervention. This chapter reviews two clinically-tolerated NMDA antagonists, memantine and nitroglycerin; (ⅰ) Memantine is an open-channel blocker of the NMDA-associated ion channel and a close congener of the anti-viral and anti-parkinsonian drug amantadine. Memantine blocks the effects of escalating levels of excitotoxins to a greater degree than lower (piysiological) levels of these excitatory amino acids, thus sparing to some extent normal neuronal function. (ⅱ) Niuoglycerin acts at a redox modulatory site of the NMDA receptor/complex to downregulate its activity. The neuroprotective action of nitroglycerin at this site is mediated by n chemical species related to nitric oxide, but in a higher oxidation state, resulting in transfer of an NO group to a critical cysteine on the NMDA receptor. Because of the clinical safety of these drugs, they have the potential for trials in humans. As the structural basis for redox modulation is further elucidated, it may become possible to design even better redox reactive reagents of chinical value. To this end, redox modulatory sites of NMDA receptors have begun to be characterized at a molecular level using site-directed mutagenesis of recombinant subunits (NMDAR1, NMDAR2A-D). Two types of redox modulation can be distinguished. The first type gives rise to a persistent change in the functional activity of the receptor, and we have identified two cysteine residues on the NMDARI subunit (#744 and #798) that are responsible for this action. A second site, presumably also a cysteine(s) because <1 mM N-ethylmaleimide can block its effect in native neurons, underlies the other, more transient redox action. It appears to be at this, as yet unidentified, site on the NMDA receptor that the NO group acts, at least in recombinant receptors.

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