scholarly journals In vitro anti-HIV activity of ethanol extract from gandarusa (Justicia gendarussa Burm. f) leaves

Author(s):  
Ni Putu Ermi Hikmawanti ◽  
Prihartini Widiyanti ◽  
Bambang Prajogo EW

Anti retroviral drugs for HIV has problems with uncomfortable side effects and that endanger the lives of HIV sufferers. Several herbs have been empirically proven to have an effect on HIV eradication through inhibition of reverse transcriptase. One of such antiviral herbs is Justicia gendarussa (J. gendarussa). The aim of research is to evaluate anti-HIV activity of 70% fractionated-ethanol extract (with releasing alkaloids) and 70% ethanol extract (without releasing alkaloids) of J. gendarussa leaves on in vitro HIV-infected of MOLT-4 cells. The effect of the extracts in inhibiting viral replication and fusion process on acute HIV infection was identi- fied through syncytia formation assay. Effect of the extracts on HIV p24 antigen was evaluated using HIV-1 p24 ELISA kit. It was found that 70% fractionated-ethanol extract and 70% ethanol extract of J. gendarussa leaves significantly inhibited of HIV replication by inhibition of syncytia formation, where the 50% effective concen- tration (EC50) values of the 70% fractionated-ethanol extract and 70% ethanol extract are 70.5 μg/mL and 228.7 μg/mL, respec- tively. Both of the extracts were also significantly inhibited HIV replication by decreasing HIV p24 antigen level where the EC 50 values of the 70% fractionated-ethanol extract and 70% ethanol extract are 88.8 μg/mL and 540.7 μg/mL, respectively. Moreover, it was found that 70% fractionated-ethanol extract of J. gendarussa leaves has anti-HIV activity since its EC50 values less than 100 μg/mL. It was concluded that J. gendarussa could be potentially developed into a phytopharmaceutical product due to its anti-HIV activity.

Planta Medica ◽  
2017 ◽  
Vol 83 (17) ◽  
pp. 1368-1373 ◽  
Author(s):  
Miao Dong ◽  
Li-Qiu Quan ◽  
Wei-Feng Dai ◽  
Shi-Li Yan ◽  
Chin-Ho Chen ◽  
...  

AbstractThree new compounds (1 – 3), including a sesterterpenoid, aspterpenacid C (1), with an unusual 5/3/7/6/5 pentacyclic skeleton, together with seven known ones (4 – 10), were isolated from the ethanol extract of the traditional Chinese medicinal plant Swertia bimaculata. Their structures were elucidated on the basis of the methods of spectroscopic NMR, MS, and computational chemistry. The structure of 1 was further confirmed by single-crystal X-ray diffraction analysis. Compounds 1 – 10 were tested for activities on the inhibition of nitric oxide production and HIV-1 replication in vitro. Compound 1 exhibited moderate activity in inhibiting nitric oxide production (IC50 = 16.1 µM) and HIV-1 replication (EC50 = 1.35 µM).


1998 ◽  
Vol 42 (5) ◽  
pp. 1200-1206 ◽  
Author(s):  
Satoshi Kubota ◽  
Shubhra Shetty ◽  
Huizhong Zhang ◽  
Shigehisa Kitahara ◽  
Roger J. Pomerantz

ABSTRACT The anti-human immunodeficiency virus type I (anti-HIV-1) effects of γ-glutamylcysteine ethyl ester (γ-GCE; TEI-2306) were examined in vitro. In initial studies using a vigorously HIV-1-producing human T-lymphocytic cell line, γ-GCE displayed a novel biphasic repressive effect on chronic HIV-1 infection that was unlike that of other glutathione prodrugs or other reported antioxidants. In high doses, up to a concentration of 2.5 mM, at which neither glutathione (GSH) nor another GSH precursor has shown inhibitory effects, γ-GCE potently inhibited the production of HIV-1 by a selective cytopathic effect against infected cells, while the viability and growth of uninfected cells were unaffected at the same γ-GCE concentrations. At lower concentrations (200 to 400 μM), γ-GCE significantly repressed the virus production from chronically HIV-1-expressing cells without affecting their viability. The discrepancy of the thresholds of the toxic doses between infected and uninfected cells was found to be more than 10-fold. Relatively high doses of γ-GCE, utilized in acute HIV-1 infection of T-lymphocytic cells, entirely blocked the propagation of HIV-1 and rescued the cells from HIV-1-induced cell death. Furthermore, γ-GCE at such concentrations was found to directly inhibit the infectivity of HIV-1 within 4 h. Repressive effects of γ-GCE on acute HIV-1 infection in human primary human peripheral blood mononuclear cells were also demonstrated. Here, the anti-HIV-1 strategy utilizing γ-GCE is removal of both HIV-1-producing cells and free infectious HIV-1 in vitro, in place of specific immunoclearance in vivo, which might lead to an arrest or slowing of viral propagation in HIV-1-infected individuals.


1996 ◽  
Vol 7 (4) ◽  
pp. 179-183 ◽  
Author(s):  
M.D. Wigg ◽  
A.A. Al-Jabri ◽  
S.S. Costa ◽  
E. Race ◽  
B. Bodo ◽  
...  

Aqueous (PA1) and methanolic extracts (PA2a–d; PA3) from the tropical tree Persea americana Mill. (Lauraceae), were evaluated for their cellular toxicity and anti-HIV-1 activity both in virustatic and virucidal assays. With the exception of PA3 and PA2d, all extracts showed anti-HIV-1 activity at concentrations which were not toxic for the H9 indicator cells. From the methanol insoluble extract (PA2) four different fractions (PA2a–d) were obtained using reverse-phase column chromatography, and two of the fractions (b and c) showed detectable virucidal effect. One fraction (PA2a) showed virustatic effects inhibiting HIV syncytium formation and viral p24 antigen formation at concentrations which were not toxic for the indicator cells. The results demonstrate for the first time that extracts from P. americana leaves have moderate anti-HIV-1 activity in vitro.


2020 ◽  
Vol 18 ◽  
Author(s):  
Maryam-Sadat Yadavar-Nikravesh ◽  
Alireza Milani ◽  
Rouhollah Vahabpour ◽  
Mehdi Khoobi ◽  
Haleh Bakhshandeh ◽  
...  

Background: HIV-1 TAT protein is essential for regulation of viral genome transcription. The first exon of TAT protein has a fundamental role in stimulation of the extrinsic and intrinsic apoptosis pathways but its anti-HIV activity is not clear yet. Methods: In the current study, we firstly cloned the first exon of TATcoding sequence in pET-24a expression vector and then protein expression was done in the Rosetta expression host. Next, the expressed TAT protein was purified by Ni-NTA column under native conditions. After that, the protein yield was determined by Bradford kit and NanoDrop spectrophotometry. Finally, the cytotoxicity effect and anti-Scr-HIV-1 activity of the recombinant TAT protein alone and along with Tenofovir drug were assessed by MTT and ELISA, respectively. Results: The recombinant TAT protein was successfully generated in E. coli as confirmed by 13.5% SDS-PAGE and western blotting. The protein yield was ~150-200 µg/ml. In addition, the recombinant TAT protein at a certain dose with low toxicity could suppress Scr-HIV replication in the infected HeLa cells (~30%) that was comparable with a low toxic dose of Tenofovir drug (~40%). It was interesting that the recombinant TAT protein could enhance anti-HIV potency of Tenofovir drug up to 66%. Conclusion: Generally, combination of TAT protein and Tenofovir drug could significantly inhibit HIV-1 replication. It will be required to determine their mechanism of action in the next studies.


1994 ◽  
Vol 36 (3) ◽  
pp. 287-292 ◽  
Author(s):  
Jorge Simão do Rosário Casseb ◽  
Adele Caterino-de-Araujo

Several cases of primary HIV-1 infection are not identified, either because the diagnosis is not suspected or because they test negative for HIV-1 antibody. This work presents an uncommon case of primary HIV-1 infection in an young parenteral drug abuser man, who presented symptoms of acute hepatitis. During the initial acute phase the serum sample of the patient tested negative for the presence of antibodies against several viruses, including HIV-1. Nevertheless, the diagnosis of primary HIV-1 infection was suspected by using an alternative method for"in vitro" induced antibody production (IVIAP), and confirmed by p24 antigen serum positivity and seroconversion in serial plasma samples of the patient. The authors suggest the use of the IVIAP and others complementary assays to help the diagnosis of acute HIV-1 infection in persons at high risk conditions.


1997 ◽  
Vol 8 (5) ◽  
pp. 307-310 ◽  
Author(s):  
H Ichimura ◽  
J M Dwyer ◽  
H Tsuchie ◽  
M A Detorio ◽  
M M Hossain ◽  
...  

The inhibitory effect of CD8+ T-cells from HIV-infected or HIVseronegative individuals on HIV replication in the naturally-infected CD4+ T-cells in vitro was examined. Not only autologous CD8+ T-cells from HIV-infected individuals but also allogeneic CD8+ T-cells from HIV-seronegative individuals prevented or delayed HIV replication, even in transwell cocultures using a semipermeable 0.45 micron filter. The level of the inhibitory effect of allogeneic CD8+ Tcells from the HIV-seronegative individuals on the HIV replication was varied among CD4+ T-cells obtained from HIV-infected individuals used. The results suggested that CD8+ T-cells from HIV-seronegative individuals as well as HIVinfected individuals could produce some cytokine(s) which suppress HIV replication in vitro . The sensitivity to the cytokine(s) might be variable among HIV strains, depending on differences in the nucleotide sequence of different HIV-1 strains. Further studies of control of HIV replication by CD8+ anti-HIV cytokine(s) should provide new strategies for the therapy of HIV infection.


2010 ◽  
Vol 7 (4) ◽  
pp. 427-432 ◽  
Author(s):  
Mamdooh Ghoneum ◽  
Magda Shaheen

We examined thein vitroanti-human immunodeficiency virus (HIV) activity of MRN-100, an iron-based compound derived from bivalent and tervalent ferrates. MRN-100 action against HIV-1 (SF strain) was tested in primary cultures of peripheral blood mononuclear cells (MNC) by analyzing p24 antigen production and percent survival of MNC infected with HIV. MRN-100 at a concentration of 10% (v/v) inhibited HIV-1 replication in 11 out of 14 samples (79%). The percentage of suppression of p24 antigen was −12.3 to 100% at 10 days post-treatment. MRN-100 also exhibited a significant protective effect in the survival of HIV-1-infected MNC. MNC survival post-treatment was dose dependent, 70.4% ± 8.4, 83.6% ± 10.7 and 90% ± 11.4, at concentrations 2.5, 5 and 10% (v/v), respectively, as compared with 53% ± 4 for HIV-1-infected MNC without treatment. The effect was detected as early as 4 days and continued up to 11 days. Treatment with MRN-100 caused no significant change in proliferative response of MNC alone or cocultured with different mitogens: PHA and Con-A (activators of T cell function) and PWM (activator of CD4+T cell-dependent B cells). We concluded that MRN-100 possesses anti-HIV activityin vitroand without an increase in lymphocyte proliferation, MRN-100 may be a useful agent for treating patients with acquired immunodeficiency syndrome.


2011 ◽  
Vol 8 (7) ◽  
pp. 602-605
Author(s):  
Ning Huang ◽  
Qin Wang ◽  
Liu-Meng Yang ◽  
Hui Xu ◽  
Yong-Tang Zheng

2008 ◽  
Vol 52 (6) ◽  
pp. 2111-2119 ◽  
Author(s):  
Hirotomo Nakata ◽  
Seth M. Steinberg ◽  
Yasuhiro Koh ◽  
Kenji Maeda ◽  
Yoshikazu Takaoka ◽  
...  

ABSTRACT Aplaviroc (AVC), an experimental CCR5 inhibitor, potently blocks in vitro the infection of R5-tropic human immunodeficiency virus type 1 (R5-HIV-1) at subnanomolar 50% inhibitory concentrations. Although maraviroc is presently clinically available, further studies are required to determine the role of CCR5 inhibitors in combinations with other drugs. Here we determined anti-HIV-1 activity using combinations of AVC with various anti-HIV-1 agents, including four U.S. Food and Drug Administration-approved drugs, two CCR5 inhibitors (TAK779 and SCH-C) and two CXCR4 inhibitors (AMD3100 and TE14011). Combination effects were defined as synergistic or antagonistic when the activity of drug A combined with B was statistically greater or less, respectively, than the additive effects of drugs A and A combined and drugs B and B combined by using the Combo method, described in this paper, which provides (i) a flexible choice of interaction models and (ii) the use of nonparametric statistical methods. Synergistic effects against R5-HIV-1Ba-L and a 50:50 mixture of R5-HIV-1Ba-L and X4-HIV-1ERS104pre (HIV-1Ba-L/104pre) were seen when AVC was combined with zidovudine, nevirapine, indinavir, or enfuvirtide. Mild synergism and additivity were observed when AVC was combined with TAK779 and SCH-C, respectively. We also observed more potent synergism against HIV-1Ba-L/104pre when AVC was combined with AMD3100 or TE14011. The data demonstrate a tendency toward greater synergism with AVC plus either of the two CXCR4 inhibitors compared to the synergism obtained with combinations of AVC and other drugs, suggesting that the development of effective CXCR4 inhibitors may be important for increasing the efficacies of CCR5 inhibitors.


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