Plasmodium

With IC50s of 0.88±0.59 and 1.23±0.64 nM, respectively, artemisone inhibits 3D7 and K1 P. falciparum[1].

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The anti-SARS-CoV-2 activity of Artemisone was evaluated in vitro using African green monkey kidney Vero E6 cells. The half-cytotoxic concentration (CC50) was greater than 200 µM. The half-maximal effective concentration (EC50) against SARS-CoV-2 was 49.64 ± 1.85 µM, resulting in a suboptimal selective index. [2]

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The anti-SARS-CoV-2 activity of Artemisone was evaluated in vitro using African green monkey kidney Vero E6 cells. The half-cytotoxic concentration (CC50) was greater than 200 µM. The half-maximal effective concentration (EC50) against SARS-CoV-2 was 49.64 ± 1.85 µM, resulting in a suboptimal selective index. [2]

Artemisone has an effective ED50 of 9.62 mg/kg when administered subcutaneously and 11.67 mg/kg when administered orally in the P. berghei NY susceptible strain.
When used with other antimalarials, artemisone (3, 1, 0.3, and 0.1 mg/kg, s.c.) has a greater effect against the chloroquine-resistant line P. yoelii NS.[1]

Cytotoxicity and Antiviral Assay: Cytotoxicity was evaluated in Vero E6 cells using a cell counting kit. For the antiviral assay, cells were seeded overnight, pretreated with a gradient of diluted experimental compounds for 1 hour, and then infected with SARS-CoV-2 at a low multiplicity of infection. After incubation, the inoculum was removed, cells were washed, and fresh drug-containing medium was added. At 24 hours post-infection, total RNA was extracted from the supernatant and quantitative real-time PCR was performed to quantify the virus yield. [2]
Immunofluorescence Assay (IFA): Vero E6 cells were inoculated, pretreated with compounds, and infected with virus similar to the antiviral assay. At 24 hours post-infection, cells were fixed, permeabilized, and blocked. Cells were then incubated with a primary antibody against the SARS-CoV-2 nucleoprotein, followed by a fluorescently labeled secondary antibody. Nuclei were stained with a dye, and images were obtained using a fluorescence microscope. This study used IFA to demonstrate the dose-dependent inhibition of viral nucleoprotein expression by several artemisinins, but specific IFA results for Artemisone were not shown in the provided figures. [2]

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Cytotoxicity and Antiviral Assay: Cytotoxicity was evaluated in Vero E6 cells using a cell counting kit. For the antiviral assay, cells were seeded overnight, pretreated with a gradient of diluted experimental compounds for 1 hour, and then infected with SARS-CoV-2 at a low multiplicity of infection. After incubation, the inoculum was removed, cells were washed, and fresh drug-containing medium was added. At 24 hours post-infection, total RNA was extracted from the supernatant and quantitative real-time PCR was performed to quantify the virus yield. [2]
Immunofluorescence Assay (IFA): Vero E6 cells were inoculated, pretreated with compounds, and infected with virus similar to the antiviral assay. At 24 hours post-infection, cells were fixed, permeabilized, and blocked. Cells were then incubated with a primary antibody against the SARS-CoV-2 nucleoprotein, followed by a fluorescently labeled secondary antibody. Nuclei were stained with a dye, and images were obtained using a fluorescence microscope. This study used IFA to demonstrate the dose-dependent inhibition of viral nucleoprotein expression by several artemisinins, but specific IFA results for Artemisone were not shown in the provided figures. [2]

[1]. Antimalarial efficacy and drug interactions of the novel semi-synthetic endoperoxide artemisone in vitro and in vivo. J Antimicrob Chemother. 2007 Apr;59(4):658-65.

[2]. Anti-SARS-CoV-2 Potential of Artemisinins In Vitro. ACS Infect. Dis. 2020 Jul.

Artemisone is being studied in the clinical trial NCT00936767 (Artemisone for the treatment of uncomplicated malignant malaria in western Cambodia). Artemisone is an approved drug derived from Artemisone. This study systematically evaluated its potential against SARS-CoV-2 in vitro when used in combination with other Artemisone-based drugs. [2] The text also mentions that, based on previous studies (not this study), Artemisone has been shown to be an effective inhibitor of human cytomegalovirus and has shown synergistic antiviral activity when used in combination with other drugs. [2] Artemisone is an approved drug derived from Artemisone. This study systematically evaluated its potential against SARS-CoV-2 in vitro when used in combination with other Artemisone-based drugs. [2] The text also mentions that, based on previous studies (not this study), Artemisone has been shown to be an effective inhibitor of human cytomegalovirus and has shown synergistic antiviral activity when used in combination with other drugs. [2]

C19H31NO6S

401.51754

401.187

C, 56.84; H, 7.78; N, 3.49; O, 23.91; S, 7.98

255730-18-8

11531457

White to off-white solid powder

2.595

0

7

1

27

696

8

C[C@@H]1CC[C@H]2[C@@H](C)[C@H](N3CCS(=O)(=O)CC3)O[C@H]4[C@@]25[C@H]1C[C@](C)(CO4)OO5

FDMUNKXWYMSZIR-NQWKWHCYSA-N

InChI=1S/C19H31NO6S/c1-12-4-5-15-13(2)16(20-8-10-27(21,22)11-9-20)23-17-19(15)14(12)6-7-18(3,24-17)25-26-19/h12-17H,4-11H2,1-3H3/t12-,13-,14+,15+,16-,17-,18-,19-/m1/s1

4-((3R,5aS,6R,8aS,9R,10R,12R,12aR)-3,6,9-Trimethyldecahydro-12H-3,12-epoxypyrano(4,3-j)(1,2)benzodioxepin-10-yl)thiomorpholine-1,1-dione

Artemifone; Artemisone; BAY-44-9585; BAY44-9585; BAY 44-9585; BAY-449585; BAY 449585; BAY449585.

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~130 mg/mL (~323.77 mM)

Solubility in Formulation 1: ≥ 2.17 mg/mL (5.40 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 21.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 2.17 mg/mL (5.40 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 21.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.17 mg/mL (5.40 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 21.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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Solubility in Formulation 4: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2.17 mg/mL (5.40 mM)

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 (Please use freshly prepared in vivo formulations for optimal results.)