• YAKHAK HOEJI
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• v.47 no.1
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• pp.46-51
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• 2003

Baicalein and baicalin are flavonoid compounds isolated from medicinal herb Scutellaria baicalensis Georgi (Labiatae) and have been known to possess antiviral activities. In the present study, we investigated the in vitro effects of baicalein and baicalin on the three distinctive enzymatic activities of the human immunodeficiency virus type-1 (HIV-1) integrase-endonucleolytic, integration, and disintegration activities. Both compounds inhibited the three enzymatic activities in a dose-dependent manner. The 50％ inhibitory concentrations of baicalein and baicalin for endonucleolytic activities of HIV-1 integrase were 4.4$\pm$3.3 and 25.9$\pm$4.0$\mu$M, respectively. In general, baicalein exhibited nearly 6- to 10-fold stronger inhibition than baicalin for the three enzymatic activities. These data demonstrate that baicalein or baicalin can be used as a leading compound to develop anti-AIDS chemotherapeutic agents targeting to the HIV-1 integrase.

• The Korean Journal of Food & Health Convergence
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• v.6 no.4
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• pp.17-19
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• 2020

HIV/AIDS disease still remain a global pandemic and it's management has undergone series of treatment changes and improvement although there is still no permanent cure.Dolutegravir belongs to a group of HIV drugs called integrase inhibitors. Integrase inhibitors block an HIV enzyme called integrase. By blocking integrase, integrase inhibitors prevent HIV from multiplying and can reduce the amount of HIV in the body.Dolutegravir combination based regimen has turned out to be very effective (antiviral) with negligible rare side effects on clients. This drug (Dolutegravir based regimen) combination has successfully increased the appetite for food of all the clients, unlike others and has shown to reduce viral load in the most shortest period ever. It can be deduced that development of resistant mutant virus will be reduced if not eliminated with dolutogravir based regimen.The role of Continuous adherence counseling has shown to improve clients treatment management. It is important to note that the availability of food has direct effect on the economic status or financial weight on the client. Hence the progress that is increase in body mass index (BMI) is a direct impact of the availability of food for the clients.

• Bulletin of the Korean Chemical Society
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• v.27 no.11
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• pp.1888-1890
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• 2006

• Bulletin of the Korean Chemical Society
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• v.32 no.1
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• pp.208-212
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• 2011

In this work, the calculated nuclear quadrupole coupling constants of $^{17}O$ in some styrylquinoline conformers were presented. The calculations were carried out to find the relationships between the charge distribution of styrylquinolines and their pharmaceutical behavior and to explore the differences among the electronic structures of some conformers of these potent HIV IN inhibitors. Furthermore, the HIV IN inhibitory of R1 and R2 rotamers was compared. On the basis of our results: - Charge density on oxygen atoms of carboxyl moiety has a dominant role in the drug activity. - The a conformer in which a divalent hydrogen atom is a link, has more capability in antiviral drug treatment. - The R1 conformer, as a $Mg^{+2}$ chelating agent, is better than R2 conformer and thus it is more inhibitor of HIV IN.

• Bulletin of the Korean Chemical Society
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• v.28 no.9
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• pp.1510-1514
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• 2007

Recently, it has been reported that the inhibition of the strand transfer function of HIV-1 integrase is necessary to obtain significant antiviral activity. Accordingly, several compounds typified by aryl 1,3-diketo acids that can inhibit strand transfer reaction of HIV-1 IN have been identified. In this work, we synthesized new 4- hydroxy-5-azacoumarin-3-carbox(thio)amides (1a-h) and evaluated for the inhibition of HIV-1 IN strand transfer reaction with a brief SAR. Among synthesized, compound 1e was the most potent HIV-1 IN inhibitor with equipotent activity to that of L-708,906. Therefore, the 4-hydroxy-5-azacoumarin ring can be considered as a new scaffold in designing more potent of HIV-1 IN inhibitors for treatment of AIDS.

• Archives of Pharmacal Research
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• v.24 no.4
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• pp.286-291
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• 2001

Seven phenylpropanoid glycosides named acteoside (1), acteoside isomer (2), leucosceptoside A (3), plantainoside C (4), jionoside D (5), martynoside (6), and isomartynoside (7) were isolated from Clerodendron trichotomum. Compounds 1 and 2 showed potent inhibitory activities against HlV-1 integrase with $IC_{20}$ values of 7.8 ${\pm}$ 3.6 and 13.7 ${\pm}$ 6.0${\mu}\textrm{M}$, respectively.