| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Additional Infomation |
Therapeutic Uses
Traditional Chinese Medicine Exploring Treatments Candida albicans is one of the most common fungal pathogens in humans. The emergence of resistance to azole antifungal drugs has raised the question of combination therapy to optimize treatment efficacy. This study aimed to evaluate the in vitro synergistic effect of pseudolarial acid B (PAB) and fluconazole (FLC) against clinically isolated Candida albicans. The in vitro antifungal activity of PAB (a diterpenic acid from P. albicans) alone and in combination with FLC against 22 FLC-resistant (FLC-R) and 12 FLC-sensitive (FLC-S) Candida albicans strains was evaluated using the checkerboard microdilution method and time-kill assay. Synergistic effects were observed in all 22 (100%) FLC-R strains, determined by the partial inhibition concentration index (FICI) (range 0.02 to 0.13) and the Bliss independence (BI) model. Of the 12 FLC-S strains, 2 (17%) showed synergistic effects using the FICI model (values ranging from 0.25 to 0.5), while 3 (18%) showed synergistic effects using the BI model. For the FLC-R strains, the synergistic FLC and PAB concentrations ranged from 0.06 to 4 μg mL⁻¹ and 0.5 to 4 μg mL⁻¹, respectively. For the FLC-S strains, the concentrations ranged from 1 to 8 μg mL⁻¹ and 0.5 to 4 μg mL⁻¹, respectively. The results of the BI model were consistent with those of the FICI model, but no antagonistic activity was observed in any of the tested strains. The interaction between PAB and FLC was confirmed using time-kill assays against the selected strains. Fluconazole and PAB showed good synergistic effects against azole-resistant Candida albicans isolates. Exploring treatments for candidiasis is an opportunistic infection common in HIV-infected individuals. Approximately 90% of patients with HIV/AIDS develop oral and/oropharyngeal candidiasis at different stages. Triazole antifungals, such as fluconazole and itraconazole, are considered the first-line drugs for the treatment and prevention of candidiasis due to their relatively low side effects and high efficacy against mucosal infections. However, long-term exposure to azole drugs can lead to drug resistance, which poses a challenge for both clinicians and patients. In Traditional Chinese Medicine (TCM), over 300 herbs have been identified as having "bactericidal" properties, some of which have been used clinically as antifungal drugs for many years. Crude extracts of many TCM herbs have shown antifungal activity in in vitro experiments, including peony bark, larch bark, galangal, coptis, clove, cinnamon, anemarrhena, phellodendron bark, cassia twig, and gallnut. Identified effective anti-Candida components include berberine, palmatine, allicin, larchic acid A and B, magnolol, and magnolol and galangin. Therefore, TCM provides a rich selection for treating refractory candidiasis, a common ailment in HIV/AIDS patients. However, further screening of the effective extracts and investigation of their antifungal mechanisms are still needed. Importantly, the safety of these compounds must be fully demonstrated before clinical application. |
| Molecular Formula |
C23H28O8
|
|---|---|
| Molecular Weight |
432.46
|
| Exact Mass |
432.178
|
| CAS # |
82508-31-4
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| PubChem CID |
6475943
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| Appearance |
White to off-white solid powder
|
| Density |
1.3±0.1 g/cm3
|
| Boiling Point |
613.8±55.0 °C at 760 mmHg
|
| Melting Point |
166°C
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| Flash Point |
208.8±25.0 °C
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| Vapour Pressure |
0.0±3.8 mmHg at 25°C
|
| Index of Refraction |
1.565
|
| LogP |
2.78
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
7
|
| Heavy Atom Count |
31
|
| Complexity |
913
|
| Defined Atom Stereocenter Count |
4
|
| SMILES |
C/C(=C\C=C\[C@@]1([C@@H]2CC[C@@]3([C@@]2(CCC(=CC3)C(=O)OC)OC(=O)C)C(=O)O1)C)/C(=O)O
|
| InChi Key |
VDGOFNMYZYBUDT-YDRCMHEVSA-N
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| InChi Code |
InChI=1S/C23H28O8/c1-14(18(25)26)6-5-10-21(3)17-9-12-22(20(28)31-21)11-7-16(19(27)29-4)8-13-23(17,22)30-15(2)24/h5-7,10,17H,8-9,11-13H2,1-4H3,(H,25,26)/b10-5+,14-6+/t17-,21+,22+,23-/m0/s1
|
| Chemical Name |
(2E,4E)-5-[(1R,7S,8S,9R)-7-acetyloxy-4-methoxycarbonyl-9-methyl-11-oxo-10-oxatricyclo[6.3.2.01,7]tridec-3-en-9-yl]-2-methylpenta-2,4-dienoic acid
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| Synonyms |
Pseudolaric Acid B (-)-Pseudolaric acid B Pseudolaric Acid-B
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~115.62 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.78 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 25.0 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.81 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 20.8 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.81 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3124 mL | 11.5618 mL | 23.1235 mL | |
| 5 mM | 0.4625 mL | 2.3124 mL | 4.6247 mL | |
| 10 mM | 0.2312 mL | 1.1562 mL | 2.3124 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.