Gramicidin S  (Synonyms: Gramicidin soviet)

Gramicidin S (Gramicidin soviet) is a cationic cyclic peptide antibiotic that selectively targets bacterial cell membranes and has anticancer activity. Gramicidin S also exerts antibacterial activity by destroying membrane integrity and interfering with membrane protein function. Gramicidin S inserts into the phospholipid bilayer through hydrophobic amino acid residues, specifically binds to negatively charged membrane lipids and disrupts membrane structure, thereby inhibiting cell division and cell wall synthesis, and ultimately causing bacterial death. Gramicidin S also inhibits ion channels, with IC₅₀s of 41 μM, 24 μM, and 3 μM for Na⁺/K⁺-ATPase, tobacco leaf plasma membrane Mg²⁺/K⁺-ATPase, and rat heart plasma membrane Ca²⁺-ATPase, respectively^[1][2][3].

In the membrane protein localization experiment, Gramicidin S (1 μM; 10 min) causes the localization disorder of the peripheral membrane proteins MinD, DivIVA and PlsX of Bacillus subtilis, among which PlsX completely lost its membrane binding ability^[1].
In the cell viability experiment, Gramicidin S (1 μM; 30 min) significantly reduces the viability of Escherichia coli (E. coli) cells, causing about 70% cell death by destroying the cell membrane integrity and inducing lipid phase separation^[1].
Gramicidin S has nematicidal activity with IC₅₀=0.08 μM (Bursaphelenchus lignicolus) and inhibits Escherichia coli with IC₅₀=3.5 μM^[1].
Gramicidin S (1 μg/mL, 2 μg/mL; 9 h) can induce fluid lipid domains independently of the MreB cytoskeleton, leading to the delocalization of peripheral membrane proteins (such as MurG involved in cell wall synthesis)^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Gramicidin S (20-200 μg/mouse/day; intraperitoneal injection; daily; 21 days) significantly inhibits tumor growth in ICR mice subcutaneously implanted with Sarcoma 180 (S180), with a 60% inhibition rate observed in the high-dose group (200 μg/mouse/day) after 21 days without significant body weight loss^[3].
Gramicidin S (20-50 μg/mouse/day; intraperitoneal injection; daily; 16 days) shows a 60% tumor inhibition rate in BALB/c mice subcutaneously implanted with Meth A fibrosarcoma at the high dose (50 μg/mouse/day) after 16 days, while low-dose treatment exhibits weaker inhibition^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

1141.45

C₆₀H₉₂N₁₂O₁₀

113-73-5

Solid

White to off-white

cyclo(Val-Orn-Leu-D-Phe-Pro)2

cyclo(VOLDFP)2

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Mogi T, et al. Gramicidin S and polymyxins: the revival of cationic cyclic peptide antibiotics. Cell Mol Life Sci. 2009 Dec;66(23):3821-6.  [Content Brief]

  [2]. Wenzel M, et al. The Multifaceted Antibacterial Mechanisms of the Pioneering Peptide Antibiotics Tyrocidine and Gramicidin S. mBio. 2018 Oct 9;9(5):e00802-18.  [Content Brief]

  [3]. Okamoto K, et al. Inhibitory effect of gramicidin S on the growth of murine tumor cells in vitro and in vivo. Oncology. 1984;41(1):43-8.  [Content Brief]