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Anti-HIV-1 activity, protease inhibition and safety profile of extracts prepared from Rhus parviflora.

Modi M - BMC Complement Altern Med (2013)

Bottom Line: Both the extracts did not disturb the integrity of monolayer formed by intestinal epithelial Caco-2 cells.The extracts when tested up to 100 μg/ml did not significantly reduce the viability of L. plantarum, L. fermentum, L. rhamnosus and L. casei.The studies reported herein showed in vitro anti-HIV activity and preliminary safety profile of the extracts prepared from the leaves of R. parviflora.

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ABSTRACT

Background: In the present study, extracts prepared from the leaves of Rhus parviflora Roxb. (Anacardiaceae) were evaluated for their anti-HIV activity, which have been traditionally used for the treatment of neurological disorders such as anxiety, insomnia and epilepsy.

Methods: Aqueous and 50% ethanolic extracts prepared from leaves of the plant were tested for their cytotoxicity and anti-HIV property using reporter gene based assays as well as human peripheral blood lymphocytes (PBLs). Further these extracts were evaluated for their ability to inhibit HIV-1 reverse transcriptase (RT) and protease activity. Safety profile of the extracts was determined on viability of Lactobacillus sp., secretion of pro-inflammatory cytokines by vaginal keratinocytes and transepithelial resistance.

Results: Both aqueous (IC50 = 15 μg/ml) and 50% ethanolic (IC50 = 26 μg/ml) extracts prepared from leaves of R. parviflora showed anti-HIV activity in TZM-bl cells wherein the virus was treated with the extracts prior to infection. Further, both the extracts also inhibited virus load in HIV infected CEM-GFP cells and human PBLs. The anti-HIV activity is mediated through inhibition of HIV-1 protease activity. Both the extracts did not disturb the integrity of monolayer formed by intestinal epithelial Caco-2 cells. The extracts when tested up to 100 μg/ml did not significantly reduce the viability of L. plantarum, L. fermentum, L. rhamnosus and L. casei. The extracts (100 μg/ml) did not reveal any cytotoxic effect on vaginal keratinocytes (Vk2/E6E7). Levels of pro-inflammatory cytokines secreted by Vk2/E6E7 cells treated with both the plant extracts were within the non-inflammatory range.

Conclusions: The studies reported herein showed in vitro anti-HIV activity and preliminary safety profile of the extracts prepared from the leaves of R. parviflora.

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Inhibitory effect of the extracts prepared from leaves of R. parviflora on HIV-1 protease activity. Inhibition of HIV-1 protease by 50% ethanolic and aqueous extracts prepared from leaves of R. parviflora was determined by a commercial kit. Experiments were performed using both positive (HIV-1 protease with pepstatin treatment) as well as negative controls (HIV-1 protease without treatment). Data is expressed as percent inhibition of HIV-1 protease activity determined by dividing the difference in fluorescent intensity of experimental and negative control by negative control followed by multiplication with 100. Data is represented as mean ± SE of three independent experiments. Statistical significance between the extract treated groups as compared to untreated enzyme control group is presented by asterisk (*p < 0.001).
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Figure 3: Inhibitory effect of the extracts prepared from leaves of R. parviflora on HIV-1 protease activity. Inhibition of HIV-1 protease by 50% ethanolic and aqueous extracts prepared from leaves of R. parviflora was determined by a commercial kit. Experiments were performed using both positive (HIV-1 protease with pepstatin treatment) as well as negative controls (HIV-1 protease without treatment). Data is expressed as percent inhibition of HIV-1 protease activity determined by dividing the difference in fluorescent intensity of experimental and negative control by negative control followed by multiplication with 100. Data is represented as mean ± SE of three independent experiments. Statistical significance between the extract treated groups as compared to untreated enzyme control group is presented by asterisk (*p < 0.001).

Mentions: HIV-1 protease is another important enzyme of the HIV life cycle acting at post-entry level. Protease influences the viral components to associate with host cell membrane which then buds off as immature virions. Protease activity continues after detachment from the host cell to ensure maturation into a fully infectious virion. The 50% ethanolic and aqueous leaves extracts of R. parviflora were evaluated for their effect on HIV-1 protease activity. Both these extracts inhibited HIV-1 protease activity in a dose dependent manner when tested at 10, 20 and 50 μg/ml. A maximum inhibition of >65% was shown by both the extracts at 50 μg/ml (Figure 3). Hence, HIV-1 protease inhibition is one of the mode by which the extracts prepared from leaves of R. parviflora inhibited HIV infection. However, a higher degree of inhibition of HIV-1 infection by these extracts might be attributed to the presence of several phytochemicals that could work through interference at other steps of virus life cycle.


Anti-HIV-1 activity, protease inhibition and safety profile of extracts prepared from Rhus parviflora.

Modi M - BMC Complement Altern Med (2013)

Inhibitory effect of the extracts prepared from leaves of R. parviflora on HIV-1 protease activity. Inhibition of HIV-1 protease by 50% ethanolic and aqueous extracts prepared from leaves of R. parviflora was determined by a commercial kit. Experiments were performed using both positive (HIV-1 protease with pepstatin treatment) as well as negative controls (HIV-1 protease without treatment). Data is expressed as percent inhibition of HIV-1 protease activity determined by dividing the difference in fluorescent intensity of experimental and negative control by negative control followed by multiplication with 100. Data is represented as mean ± SE of three independent experiments. Statistical significance between the extract treated groups as compared to untreated enzyme control group is presented by asterisk (*p < 0.001).
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC3716979&req=5

Figure 3: Inhibitory effect of the extracts prepared from leaves of R. parviflora on HIV-1 protease activity. Inhibition of HIV-1 protease by 50% ethanolic and aqueous extracts prepared from leaves of R. parviflora was determined by a commercial kit. Experiments were performed using both positive (HIV-1 protease with pepstatin treatment) as well as negative controls (HIV-1 protease without treatment). Data is expressed as percent inhibition of HIV-1 protease activity determined by dividing the difference in fluorescent intensity of experimental and negative control by negative control followed by multiplication with 100. Data is represented as mean ± SE of three independent experiments. Statistical significance between the extract treated groups as compared to untreated enzyme control group is presented by asterisk (*p < 0.001).
Mentions: HIV-1 protease is another important enzyme of the HIV life cycle acting at post-entry level. Protease influences the viral components to associate with host cell membrane which then buds off as immature virions. Protease activity continues after detachment from the host cell to ensure maturation into a fully infectious virion. The 50% ethanolic and aqueous leaves extracts of R. parviflora were evaluated for their effect on HIV-1 protease activity. Both these extracts inhibited HIV-1 protease activity in a dose dependent manner when tested at 10, 20 and 50 μg/ml. A maximum inhibition of >65% was shown by both the extracts at 50 μg/ml (Figure 3). Hence, HIV-1 protease inhibition is one of the mode by which the extracts prepared from leaves of R. parviflora inhibited HIV infection. However, a higher degree of inhibition of HIV-1 infection by these extracts might be attributed to the presence of several phytochemicals that could work through interference at other steps of virus life cycle.

Bottom Line: Both the extracts did not disturb the integrity of monolayer formed by intestinal epithelial Caco-2 cells.The extracts when tested up to 100 μg/ml did not significantly reduce the viability of L. plantarum, L. fermentum, L. rhamnosus and L. casei.The studies reported herein showed in vitro anti-HIV activity and preliminary safety profile of the extracts prepared from the leaves of R. parviflora.

View Article: PubMed Central - HTML - PubMed

ABSTRACT

Background: In the present study, extracts prepared from the leaves of Rhus parviflora Roxb. (Anacardiaceae) were evaluated for their anti-HIV activity, which have been traditionally used for the treatment of neurological disorders such as anxiety, insomnia and epilepsy.

Methods: Aqueous and 50% ethanolic extracts prepared from leaves of the plant were tested for their cytotoxicity and anti-HIV property using reporter gene based assays as well as human peripheral blood lymphocytes (PBLs). Further these extracts were evaluated for their ability to inhibit HIV-1 reverse transcriptase (RT) and protease activity. Safety profile of the extracts was determined on viability of Lactobacillus sp., secretion of pro-inflammatory cytokines by vaginal keratinocytes and transepithelial resistance.

Results: Both aqueous (IC50 = 15 μg/ml) and 50% ethanolic (IC50 = 26 μg/ml) extracts prepared from leaves of R. parviflora showed anti-HIV activity in TZM-bl cells wherein the virus was treated with the extracts prior to infection. Further, both the extracts also inhibited virus load in HIV infected CEM-GFP cells and human PBLs. The anti-HIV activity is mediated through inhibition of HIV-1 protease activity. Both the extracts did not disturb the integrity of monolayer formed by intestinal epithelial Caco-2 cells. The extracts when tested up to 100 μg/ml did not significantly reduce the viability of L. plantarum, L. fermentum, L. rhamnosus and L. casei. The extracts (100 μg/ml) did not reveal any cytotoxic effect on vaginal keratinocytes (Vk2/E6E7). Levels of pro-inflammatory cytokines secreted by Vk2/E6E7 cells treated with both the plant extracts were within the non-inflammatory range.

Conclusions: The studies reported herein showed in vitro anti-HIV activity and preliminary safety profile of the extracts prepared from the leaves of R. parviflora.

Show MeSH
Related in: MedlinePlus