• 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.

• Bulletin of the Korean Chemical Society
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• v.33 no.8
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• pp.2574-2580
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• 2012

The discovery that threosyl phosphonate nucleoside (PMDTA, $EC_{50}=2.53{\mu}M$) is a potent anti-HIV agent has led to the synthesis and biological evaluation of 5'-deoxy versions of threosyl phosphonate nucleosides. In the present study, (E)-3'-phosphonoalkenyl and 3'-phosphonoalkyl nucleoside analogues 13, 16, 20 and 23 were synthesized from acetol and tested for anti-HIV activity and cytotoxicity. The adenine analogue 16 was found to exhibit moderate in vitro anti-HIV-1 activity ($EC_{50}=22.2{\mu}M$).

• Archives of Pharmacal Research
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• v.25 no.4
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• pp.441-445
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• 2002

Three naphthalene glycosides (1-3), four flavonoids (4-7), and two galloyl glycosides (8-9) were isolated from the stem-bark of Juglans mandshurica (Juglandaceae). Their structures were determined by chemical and spectral means, including to 2D-NMR (COSY, HMQC, and HMBC) experiments. Amongst the isolated compounds, taxifolin (4) showed the most potent HIV-induced cytopethic activity against MT-4 cells with complete inhibitory concentration ($IC_{100}$) value of $25{\;}{\mu\textrm{g}}/ml$ and maximum cytotoxic concentration ($CC_{100}$) value of above $100{\;}{\mu\textrm{g}}/ml$. However, naphthalene glycosides (1-3), flavonoids (5-7)), and galloyl tannins (8-9) were inactive against anti-HIV-1 activity.

• Archives of Pharmacal Research
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• v.20 no.5
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• pp.425-431
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• 1997

To examine components of Ganoderma lucidum for anti-human immunodeficiency virus (HIV) activity, the aqueous extracts of its basidiocarps were separated into high-molecular-weight (HMF) and low-molecular-weight (LMF) fractions. These fractions were used in XTT [2,3-bis (2-methoxy-4-nitro-5-sulfophenyl)-5-[(phenylamino) carbonyl]-2H-tetrazolium hydroxide] antiviral assay which can quantitatively measure cytopathic effects of HIV-1 on CEM, human T lymphoblastoid cell line. The CEM cell line added with serial diluted HMF or LMF was cultured in the absence or presence of HIV-1. The results showed that the LMF of the aqueous extract strongly inhibited cytopathic effect of the target cell induced by HIV-1. When two-fold serially diluted LMF ranging from $40.97{\mu}g/ml$4 to 125.00 .mu.g/ml was added to the virus-free culture system, no toxicity on the target cells was detected in all the concentrations tested. However, when it was added to the HIV-infected culture system, the viabilities of the target cell reached a plateau recovering its viabilities to 71.7% and 82.5% in experiment-1 and -2 at 15.60 .mu.g/ml, respectively. The cell viabilities were then gradually decreased but maintained at more than 50% above 31.20 .mu.g/ml concentration. On the contrary, HMF did not prevent any HIV-induced cytopathic effect at any concentrations tested on this cell line. From these results, negligible toxicities were observed by both HMF and LMF of G. luciolum, and recovery of cell viability in HIV infected target cell was induced only by LMF of the carpophores.

• YAKHAK HOEJI
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• v.58 no.5
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• pp.349-356
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• 2014

With the advent of highly active anti-retroviral therapy (HAART), the perceptions of HIV therapy have changed from treating acute and terminal diseases to managing complex chronic diseases. Due to needs for specialists with professional knowledge on anti-retroviral therapies, pharmacists have been recognized as established and integral members in HIV multi-disciplinary care teams. Nevertheless, the roles of Korean pharmacists for HIV/AIDS therapy were highly limited. According to the transition of '2+4'-year pharmacy school curricula in Korea, it is necessary for pharmacy students to possess improved knowledge about and proper attitudes toward HIV/AIDS as future pharmacists. However, there have been little studies regarding the assessment of HIV/AIDS knowledge, attitudes, and risk perceptions of pharmacy students in Korea. Thus, this study was to examine Korean pharmacy students' knowledge levels, attitudes, and risk perceptions about HIV/AIDS and compare them according to pharmacy educational systems. The self-reported questionnaire was utilized to collect data. Total 238 students responded to the survey questionnaires. Most pharmacy students who participated in this study knew that the main transmission routes of HIV were unprotected sex, unscreened blood, occupational exposure, and intravenous drug use. However, they did not properly know post exposure prophylaxis for HIV. The pharmacy students under '2+4'-year curricula were more competent with treatment, care, counseling for HIV patients than those under 4-year curricula. Most pharmacy students thought that all healthcare students and professionals should receive mandatory HIV testings. The results from this study may contribute to developing new educational programs about HIV/AIDS. Additionally, further studies regarding the changes of Korean pharmacy students' attitudes and risk perceptions will need to be performed after they participate in these kinds of the programs.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1994.11a
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• pp.61-67
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• 1994

One fundamental problem in developing an AIDS vaccine is antigenic variation of HIV. Despite a substantial induced immune response in gp120-immunized monkeys and humans, high titers of V3-directed type specific neutralizing antibodies may not be sufficient to neutralize continuously emerging new isolates. Several studies analyzing anti-gp120 antibodies in HIV-infected individuals have clearly indicated that most broadly neutralizing antibodies are directed to conformation-dependent epitopes. Therefore, it seems important to evaluate the potential efficacy of candidate gp120 vaccines at inducing such antibodies, that might be potentially protective against multiple HIV strains. One concern in the development of any recombinant protein as a vaccine is its stability when mixed with an adjuvant. This could be a particularly important factor for recombinant gp120, given the conformational nature of its major, broadly neutralizing, epitopes. We hypothesized that gp120 complexed with recombinant CD4 could stabilize the conformation-dependent epitopes and effectively deliver these epitopes to the immune system. In this study, a soluble gp120-CD4 complex in Syntex Adjuvant Formulation was tested in mice to analyze the anti-gp120 antibody response. With the aim of defining the fine specificity and neutalizing activities of the immune response, 17Mabs were generated and characterized. The studies indicate that the gp120-CD4 complex elicits neutralizing anti-gp120 antibodies, most of which are directed to the conformation dependent epitopes.

• Bulletin of the Korean Chemical Society
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• v.34 no.3
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• pp.868-874
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• 2013

Efficient synthetic route to novel 2'-spirocyclopropanoid 4'-deoxythreosyl phosphonic acid nucleosides was described from 1,4-dihydroxy-2-butene. Cyclopropane moiety was prepared via ester enolate alkylation using (2-chloroethyl)dimethylsulfonium iodide. Synthesized nucleoside analogues 16, 19, 23 and 26 were tested for anti-HIV activity as well as cytotoxicity. However, none of them showed any anti-HIV activity or cytotoxicity up to 100 ${\mu}M$.

• BMB Reports
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• v.55 no.12
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• pp.639-644
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• 2022

Serine-arginine-rich splicing factors (SRSFs) are members of RNA processing proteins in the serine-arginine-rich (SR) family that could regulate the alternative splicing of the human immunodeficiency virus-1 (HIV-1). Whether SRSF9 has any effect on HIV-1 regulation requires elucidation. Here, we report for the first time the effects and mechanisms of SRSF9 on HIV-1 regulation. The overexpression of SRSF9 inhibits viral production and infectivity in both HEK293T and MT-4 cells. Deletion analysis of SRSF9 determined that the RNA regulation motif domain of SRSF9 is important for anti-HIV-1 effects. Furthermore, overexpression of SRSF9 increases multiple spliced forms of viral mRNA, such as Vpr mRNA. These data suggest that SRSF9 overexpression inhibits HIV-1 production by inducing the imbalanced HIV-1 mRNA splicing that could be exploited further for a novel HIV-1 therapeutic molecule.

• Archives of Pharmacal Research
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• v.22 no.1
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• pp.75-77
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• 1999

Two diterpenoid compounds, agastanol (1) and agastaquinone (2), were isolated from the roots of Agastache rugosa (Labiatae). Compound 1 and 2 showed significant inhibitory effects against human immunodeficiency virus type 1 (HIV-1) protease activity with $IC_{50}$ values of 360 and $87{\mu}M$, respectively.

• Bulletin of the Korean Chemical Society
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• v.35 no.9
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• pp.2743-2748
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• 2014

Novel 4'-trifluoromethyl-5'-norcarbocyclic purine phosphonic acid analogs were efficiently synthesized from commercially available 1,3-dihydroxy cyclopentane (5). Trifluoromethylation was successfully performed by using the Ruppert-Prakash reaction. The purine nucleosidic bases were efficiently coupled by using the Mitsunobu reaction. The synthesized adenosine phosphonic acids analogs 13 and 16 were screened for antiviral activity against human immunodeficiency virus-1 (HIV-1). Adenine derivative 13 exhibited significant anti-HIV-1 activity.