| Description | Dihydrocyclosporin A (Dihydrocyclosporin-A) is closely related co-metabolite of cyclosporin A. Dihydrocyclosporin A significantly inhibits promastigotes and intracellular amastigotes. |
| In vitro | Dihydrocyclosporin A was able to inhibit the proliferation of L. donovani promastigotes (IC50: 21.24 μM and 12.14 μM at 24 h and 48 h, respectively) and intracellular amastigotes (IC50: 5.23 μM and 4.84 μM at 24 and 48 h, respectively) in vitro. Dihydrocyclosporin A caused several alterations in the morphology and ultrastructure of L. donovani, especially in the mitochondria. However, Dihydrocyclosporin A showed high cytotoxicity towards cells of the mouse macrophage cell line RAW264.7, with CC50 values of 7.98 μM (24 h) and 6.65 μM (48 h).[2]. |
| Target activity | Intracellular amastigotes:4.84 μM(48 h,L. donovani), Intracellular amastigotes:5.23 μM(24 h,L. donovani), Promastigotes:12.14(48 h,L. donovani), Promastigotes:21.24 μM(24 h,L. donovani) |
| Synonyms | Dihydrocyclosporin-A, 二氢环孢菌素A |
| molecular weight | 1204.63 |
| Molecular formula | C62H113N11O12 |
| CAS | 59865-15-5 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 60 mg/mL (49.81 mM) |
| References | 1. Sanglier JJ, et al. Isolation of (4R)-4-[(E)-2-butenyl]-4-methyl-L-threonine, the characteristic structural element of cyclosporins, from a blocked mutant of Tolypocladium inflatum. J Antibiot (Tokyo). 1990 Jun;43(6):707-14. 2. Zheng ZW, et al. Evaluation of in vitro antileishmanial efficacy of cyclosporin A and its non-immunosuppressive derivative, dihydrocyclosporin A. Parasit Vectors. 2020 Feb 21;13(1):94. 3. Chappell LH, et al. Dosage, timing, and route of administration of cyclosporin A and nonimmunosuppressive derivatives of dihydrocyclosporin A and cyclosporin C against Schistosoma mansoni in vivo and in vitro. 4. Chappell LH, et al. Dosage, timing, and route of administration of cyclosporin A and nonimmunosuppressive derivatives of dihydrocyclosporin A and cyclosporin C against Schistosoma mansoni in vivo and in vitro. Antimicrob Agents Chemother. 1987 Oct;31(10):1567-71. |