Tenofovir demonstrates cytotoxic effects in HK-2 cells, with IC50 values of 9.21 μM at 48 hours and 2.77 μM at 72 hours in MTT assays. It lowers ATP levels, increases oxidative stress and protein carbonylation, and induces apoptosis through mitochondrial damage in these cells [1]. Tenofovir combined with M48U1, each formulated in 0.25% HEC, inhibits replication of both R5-tropic HIV-1BaL and X4-tropic HIV-1IIIb in activated PBMCs, including several laboratory and patient-derived HIV-1 strains. This combination exhibits synergistic antiretroviral effects against R5-tropic HIV-1BaL infection and is non-toxic to PBMCs [2].
体内研究
Tenofovir Disoproxil Fumarate administered at doses of 20, 50, 140, or 300 mg/kg shows dose-dependent effectiveness in preventing vaginal HIV transmission in BLT humanized mice, significantly reducing HIV transmission at 50, 140, and 300 mg/kg [3].
Tenofovir Disoproxil Fumarate (0.5, 1.5, or 5.0 mg/kg/day, pO.) leads to a dose-dependent reduction in serum viremia in woodchucks with chronic WHV infection and is safe and effective in this model [4].
体外研究
Tenofovir demonstrates cytotoxic effects in HK-2 cells, with IC50 values of 9.21 μM at 48 hours and 2.77 μM at 72 hours in MTT assays. It lowers ATP levels, increases oxidative stress and protein carbonylation, and induces apoptosis through mitochondrial damage in these cells [1].
Tenofovir combined with M48U1, each formulated in 0.25% HEC, inhibits replication of both R5-tropic HIV-1BaL and X4-tropic HIV-1IIIb in activated PBMCs, including several laboratory and patient-derived HIV-1 strains. This combination exhibits synergistic antiretroviral effects against R5-tropic HIV-1BaL infection and is non-toxic to PBMCs [2].
Tenofovir hydrate/替诺福韦水合物 细胞实验
Cell Line
Concentration
Treated Time
Description
References
MΦ cells
5-600 µg/mL
5 days
Evaluate the cell viability of Tenofovir, AuNPs, and AuNP-TNF in MΦ cells, showing that the viability of AuNP-TNF-treated cells was significantly higher than those treated with free TNF.
J Nanobiotechnology. 2023 Jan 19;21(1):19.
PBMCs
5-600 µg/mL
5 days
Evaluate the cell viability of Tenofovir, AuNPs, and AuNP-TNF in PBMCs, showing that the viability of AuNP-TNF-treated cells was significantly higher than those treated with free TNF.
J Nanobiotechnology. 2023 Jan 19;21(1):19.
TZM-bl cells
5-600 µg/mL
48 h
Evaluate the cell viability of Tenofovir, AuNPs, and AuNP-TNF in TZM-bl cells, showing that the viability of AuNP-TNF-treated cells was significantly higher than those treated with free TNF.
J Nanobiotechnology. 2023 Jan 19;21(1):19.
CD4+ T cells
10 μM
12 h
To stop ongoing HIV-1 infection, the results showed that Tenofovir effectively suppressed viral replication.
Nat Immunol. 2024 Mar;25(3):462-470.
MΦ cells
5-600 µg/mL
5 days
Assess cell viability, results showed that AuNP-TNF had significantly higher cell viability than free TNF.
J Nanobiotechnology. 2023 Jan 19;21(1):19.
PBMCs
5-600 µg/mL
5 days
Assess cell viability, results showed that AuNP-TNF had significantly higher cell viability than free TNF.
J Nanobiotechnology. 2023 Jan 19;21(1):19.
TZM-bl cells
5-600 µg/mL
48 h
Assess cell viability, results showed that AuNP-TNF had significantly higher cell viability than free TNF.
J Nanobiotechnology. 2023 Jan 19;21(1):19.
NL4.3-ΔNef-eGFP infected CD4+ T cells
10 μM
12 h
To inhibit viral replication and prevent ongoing infection. The results showed that Tenofovir successfully inhibited viral replication, and no ongoing infection was observed in the experiment.
Nat Immunol. 2024 Mar;25(3):462-470.
CD4+ T cells
10 μM
18 h
To inhibit viral replication and prevent viral persistence in cells. The results showed that Tenofovir successfully inhibited viral replication, and no ongoing infection was observed in the experiment.
Nat Immunol. 2024 Mar;25(3):462-470.
Tenofovir hydrate/替诺福韦水合物 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
MISTRG-6-15 mouse model
Oral
1 g/kg
Not specified
Suppress HIV-1 replication
J Clin Invest. 2022 Dec 15;132(24):e162694
BALB/c mice
Healthy mice
Intravenous injection
5 mg/kg
Single injection, observed for 7 days
Evaluate the biodistribution of Cy5.5-AuNPs in BALB/c mice, showing that Cy5.5-AuNPs mainly accumulated in the liver and lungs, and gradually decreased within 7 days.
J Nanobiotechnology. 2023 Jan 19;21(1):19.
Mice
Chronic unpredictable mild stress (CUMS) model
Gastric administration
30 mg/kg
Once daily for 2 weeks
Tenofovir significantly reversed the chronic stress-induced negative emotional behaviors, including increased center time% in the open field test, increased open arms time% and open arms entries% in the elevated plus maze test, increased recognition index in the novel object recognition test, increased sucrose preference% in the sucrose preference test, and decreased immobility time% in both the forced swimming and tail suspension tests.
J Neuroinflammation. 2023 Feb 15;20(1):37
Mice
BLT humanized mouse model
Oral
1560 mg/kg
Once daily for five weeks
Tenofovir was used to suppress HIV infection, and ART successfully suppressed the virus to below the limit of detection
AIDS. 2023 Mar 15;37(4):571-577
Mice
Pregnant mice
Oral gavage
100 mg/kg
Once daily for 5 days
Tenofovir treatment reduced red blood cell counts, bone marrow cellularity, splenic HSCs, and erythroid progenitor numbers in pregnant mice, and decreased HSC division rates.
Science. 2024 Nov 8;386(6722):eado6836
Mice
HIV infection model
Oral
5.35mg
Once daily for 42 days
To evaluate the effect of antiretroviral therapy on HIV-infected mice
Front Immunol. 2022 Nov 25;13:1047277
Rhesus macaques
SIV infection model
Intravenous infusion
0.1 mg/kg
Weekly for 3 or 10 weeks
To evaluate the latency reversal effect of AZD5582 in SIV-infected rhesus macaques, results showed that AZD5582 induced SIV-RNA expression.
Nature. 2020 Feb;578(7793):160-165.
Hu-NSG-Tg (IL-15) mice
HIV infection model
Intraperitoneal injection
500 µg/mouse
Twice a week for 2 weeks
To evaluate the antiviral effect of Bi-Ab32/16 in an HIV-infected mouse model. Results showed that Bi-Ab32/16 treatment led to a significant decline in NK cell numbers and was negatively correlated with the time to viral rebound, indicating potential adverse effects on NK cell dynamics.
Commun Biol. 2025 Feb 14;8(1):236.
Mice
HIV-1 infection model
Oral
1,560 mg/kg
Daily until the end of the study
To suppress HIV-1 replication, the results showed that Tenofovir effectively reduced viral load.
Nat Immunol. 2024 Mar;25(3):462-470.
Mice
BLT mouse model
Oral
80 mg/kg
Daily
Evaluate the antiviral efficacy of Tenofovir in HIV-infected mice
Mol Ther. 2024 Apr 3;32(4):1000-1015
Mice
HIV-1 infection model
Oral
90 mg/kg
Daily for 7 weeks
Suppress HIV-1 viral replication
Cell Rep Med. 2023 Sep 19;4(9):101178.
Mice
Chronic unpredictable mild stress (CUMS) model
Gastric administration
30 mg/kg
Once daily for 2 weeks
Tenofovir significantly reversed chronic stress-induced negative emotional behaviors, including reduced anxiety- and depressive-like behaviors, and improved microglial morphological activation and biological immuno-inflammation.
J Neuroinflammation. 2023 Feb 15;20(1):37
NSG mice
BLT humanized mouse model
Oral
1,560mg/kg
Continuous administration
Evaluate the impact of Gal-9 on HIV persistence
AIDS. 2023 Mar 15;37(4):571-577
Mice
Pregnant and non-pregnant mice
Oral gavage
100 mg/kg
Daily for 5 days
In non-pregnant female mice, reverse transcriptase inhibitors had little or no effect on blood cell counts, or bone marrow or spleen hematopoiesis. In pregnant mice, reverse transcriptase inhibitors reduced red blood cell counts, bone marrow cellularity and the frequency of HSCs and LSK cells in the spleen. The absolute number of CD71+Ter119+ erythroid progenitors declined in the spleens of pregnant mice treated with reverse transcriptase inhibitors.
Science. 2024 Nov 8;386(6722):eado6836
Humanized DRAGA mice
HIV infection model
Oral
5.35mg
Once daily for 42 days
Evaluate the therapeutic effect of antiretroviral therapy on HIV infection
Front Immunol. 2022 Nov 25;13:1047277
Hu-NSG-Tg (IL-15) mice
HIV infection model
Oral
131 mg/kg
From 6 to 9 weeks post-infection (WPI)
To evaluate the therapeutic effect of Tenofovir in an HIV infection model
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