In Vitro Anti-hepatitis B Virus Activity of 2′,3′-Dideoxyguanosine

Zhang, Pinghu; Zhai, Shuo; Chang, Jinhong; Guo, Ju‐Tao

doi:10.1007/s12250-018-0065-7

Cited by 3 publications

(7 citation statements)

References 35 publications

(77 reference statements)

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“…Then they were respectively loaded onD101, DM301, X-5 and AB-8 resins. Next, they were eluted with distilled water 25%, 50% and 75% ethanol and the eluent were collected for anti-HSV-1 experiments [16].…”

Section: Antiviral Experimentsmentioning

confidence: 99%

The Efficacy of an Empowerment Program for End-Stage Renal Disease Patients Treated with Hemodialysis

Bayoumy¹

2017

JOJNHC

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Background: In recent years, many literatures have pointed out that the fruit of Prunus cerasifera Ehrhar f. has anti-oxidation effect. Based on the anti-oxidation principle of traditional Chinese medicine in antiviral aspect the antiviral effect of the fruit was studied herein and the problem of the toxicity of the fruit has not been systematically investigated yet. To clarify the toxic effects of the fruit and its material basis, the toxicity test of the fruit was carried out. Methods:The fruit was percolated with water and the percolated liquid was concentrated to collect the concentrated liquid. Viral infection model in vitro was used to evaluate the antiviral effects of different viruses in vitro. CPE was observed under a microscope to determine the inhibitory effects of different viruses. The best type of macro-porous resin was determined by the method of macro-porous resin adsorption. The types of active ingredients were determined by physical and chemical identification, and their contents were determined by UV. By intragastric administration the long-term toxicity of percolating juice of the fruit to rats was observed including the nature severity, dose-toxicity relationship, time-toxicity relationship, main target organs, toxicity reversible degree, delayed toxicity, etc.Results: showed that percolation solution of the fruit had obvious inhibitory effect on HSV-1 virus, and the TI value was 109.22. The inhibition effect of 60% ethanol precipitation on HSV-1 was the best, and the TI value was 148.84. D101 macro-porous resin presented an excellent separation effect at the volume of the first column eluted by 25% ethanol and TI value was 200.85. Chemical polyphenols were determined by physical and chemical identification and the content was 18.15 mg/g. Comparison of each dose group of percolation of the fruit and blank group there were not abnormalities in appearance signs, behavioral activities, body weight, food intake, hematological examination, serum biochemistry, organ quality and organ coefficient; Morphological examination of organs such as heart, liver, spleen, lung, kidney, ovary, testis, etc. didn't show pathological changes related to medication; Reversible observation showed that the fruit did not cause delayed toxicity to rats. There was not statistically significant difference in the above indicators. Conclusion:Polyphenols from 25% alcohol elution site of percolation of the fruit may have good anti-HSV-1 activity. The large dose of percolation of the fruit and long-term use don't have obvious toxicity which provides a basis for clinical application.

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Section: Antiviral Experimentsmentioning

confidence: 99%

The Efficacy of an Empowerment Program for End-Stage Renal Disease Patients Treated with Hemodialysis

Bayoumy¹

2017

JOJNHC

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“…[24,25] However, prolonged administration of the nucleoside drugs may result in the evolution of drug-resistant mutants of hepatitis B virus. [24][25][26][27] Various research groups have reported the frequency of HBV drug resistance-associated mutations (RAM) from different populations across the world based on public sequence databases. [28] Thus, there is a continuing need to develop wide range of nucleoside analogues with increased therapeutic indices and drug resistant barriers.…”

Section: Introductionmentioning

confidence: 99%

“…Similarly, 2′,3′‐dideoxyguanosine ( 8 ) exhibited potent antiviral effects on human and animal hepadnaviruses and found to be highly effective against 3‐TC and adefovir resistant mutants (Figure 1). [24] …”

Section: Introductionmentioning

confidence: 99%

“…Chronic hepatitis B virus (HBV) remains a serious health hazard affecting almost 250 million people worldwide [24] . Food and Drug Administration (FDA) have approved five nucleos(t)ide analogues for anti‐HBV therapy, i. e ., lamivudine (3TC), telbivudine (LdT), adefovir (ADV), tenofovir (TDF) and entecavir (ETV) [24] . The nucleos(t)ide analogues inhibit DNA replication by chain termination of viral DNA or RNA elongation [24,25] .…”

Section: Introductionmentioning

confidence: 99%

“…Similarly, 2',3'-dideoxyguanosine (8) exhibited potent antiviral effects on human and animal hepadnaviruses and found to be highly effective against 3-TC and adefovir resistant mutants (Figure 1). [24] Herein, we report the synthesis of novel 1,2,3-triazole linked hexopyranosyl mono/double-headed pyrimidine nucleosides 15 a-b and 20 a-b from D-glucose via click chemistry. The synthesized nucleosides were examined for their anti hepatitis B virus activity on HepG2.2.15 cell line.…”

Section: Introductionmentioning

confidence: 99%

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Synthesis of 1,2,3‐Triazole‐Linked Hexopyranosylpyrimidine Nucleosides and Their Application as Hepatitis B Viral DNA, HBsAg and HBeAg Suppressants

et al. 2023

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A series of novel 1,2,3‐triazole‐linked hexopyranosyl mono/double‐headed pyrimidine nucleosides from D‐glucose was synthesized by Cu(I)‐mediated [3+2] cycloaddition reactions (CuAAC) of mono/diazido 2,6‐anhydro‐glucoheptitol and propynylated pyrimidines in good yields. It was observed that all the four synthesized pyrimidine nucleosides were found to be non‐cytotoxic upto 500 μM concentration. The 1,2,3‐triazole‐linked hexopyranosyl mono/double‐headed pyrimidine nucleosides have shown significant suppression of Hepatitis B surface antigen (HBsAg) and Hepatitis B e‐antigen (HBeAg). Amongst all the synthesized compounds, nucleoside dimer 1‐[1‐(6′‐deoxy‐6′‐(4‐(1‐methyluracil)‐1,2,3‐triazol‐1‐yl)‐β‐D‐glucopyranosyl methyl)‐1,2,3‐triazol‐4‐yl]methyl‐uracil was found to be more effective against HBeAg. In the suppression of viral DNA level, all the four synthesized nucleoside analogues were comparable to known drug Entecavir (ETV) with IC50 value in the range of 8.39 μM–18.58 μM and are two folds significant as compared to control.

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Advancing beyond reverse transcriptase inhibitors: The new era of hepatitis B polymerase inhibitors

Ranga

Gupta

Yadav

et al. 2023

European Journal of Medicinal Chemistry

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In Vitro Anti-hepatitis B Virus Activity of 2′,3′-Dideoxyguanosine

Cited by 3 publications

References 35 publications

The Efficacy of an Empowerment Program for End-Stage Renal Disease Patients Treated with Hemodialysis

The Efficacy of an Empowerment Program for End-Stage Renal Disease Patients Treated with Hemodialysis

Synthesis of 1,2,3‐Triazole‐Linked Hexopyranosylpyrimidine Nucleosides and Their Application as Hepatitis B Viral DNA, HBsAg and HBeAg Suppressants

Advancing beyond reverse transcriptase inhibitors: The new era of hepatitis B polymerase inhibitors

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