AVX 13616 shows the potent in vivo antibacterial activity of Avexa’s lead antibacterial candidate; particularly against drug-resistant Staphylococcus pathogens. IC50 value: 2-4 ug ml (MICs) Target: antibacterial agent AVX13616 was as active as mupirocin i
(E)-Ajoene is a disulfide that has been found inA. sativumand has diverse biological activities.1,2,3,4It is active against Gram-positive and Gram-negative bacteria (MICs = 10-250 and 150->500 μg/ml, respectively) and fungi (MICs = 15-50 μg/ml).1(E)-Ajoene inhibits proliferation of a variety of cancer cells, including MDA-MB-231 breast, HeLa cervical, and WHCO1 esophageal cancer cells (IC50s = 18.6, 61, and 39.2 μM, respectively).2It also inhibits human glutathione reductase andT. cruzitrypanothione reductase when used at a concentration of 200 μM.3(E)-Ajoene (25 mg/kg) is neuroprotective in a gerbil model of ischemia-reperfusion injury, reducing reactive astrocytosis and microgliosis in the hippocampal CA1 region.4 1.Yoshida, H., Iwata, N., Katsuzaki, H., et al.Antimicrobial activity of a compound isolated from an oil-macerated garlic extractBiosci. Biotechnol. Biochem.62(5)1014-1017(1998) 2.Kaschula, C.H., Hunter, R., Hassan, H.T., et al.Anti-proliferation activity of synthetic ajoene analogues on cancer cell-linesAnticancer Agents Med. Chem.11(3)260-266(2011) 3.Gallwitz, H., Bonse, S., Martinez-Cruz, A., et al.Ajoene is an inhibitor and subversive substrate of human glutathione reductase and Trypanosoma cruzi trypanothione reductase: Crystallographic, kinetic, and spectroscopic studiesJ. Med. Chem.42(3)364-372(1999) 4.Yoo, D.Y., Kim, W., Nam, S.M., et al.Neuroprotective effects of Z-ajoene, an organosulfur compound derived from oil-macerated garlic, in the gerbil hippocampal CA1 region after transient forebrain ischemiaFood Chem. Toxicol.721-7(2014)
3-hydroxy Myristic acid methyl ester is a hydroxylated fatty acid methyl ester that has been found in E. camaldulensis and E. torelliana extracts. [1] It is active against M. tuberculosis (MIC = 49.5 μg ml) and is non-cytotoxic to Vero cells (IC50 = >100 μM). 3-hydroxy Myristic acid methyl ester is also a volatile compound that contributes to the aroma of red wild strawberries (F. pentaphylla) but is not present in cultivated strawberries (Fragaria x ananassa).[2] Reference:[1]. Lawal, T.O., Adeniyi, B.A., Adegoke, A.O., et al. In vitro susceptibility of Mycobacterium tuberculosis to extracts of Eucalyptus camaldulensis and Eucalyptus torelliana and isolated compounds. Pharm. Biol. 50(1), 92-98 (2012).[2]. Duan, W., Sun, P., Chen, L., et al. Comparative analysis of fruit volatiles and related gene expression between the wild strawberry Fragaria pentaphylla and cultivated Fragaria × ananassa. Eur. Food Res. Technol. 244(1), 57-72 (2018).
Mcl-1 inhibitor 6 is a potent, orally active chemical compound that selectively inhibits the myeloid cell leukemia 1 (Mcl-1) protein, with a high affinity (K d = 0.23 nM) and binding activity (K i = 0.02 μM). This compound exhibits exceptional selectivity over other members of the Bcl-2 family, including Bcl-2, Bcl2A1, Bcl-xL, and Bcl-w (K d >10 μM). Notably, Mcl-1 inhibitor 6 demonstrates strong antitumor activity.
Calmodulin antagonist-1 (W-7) is a calmodulin (CaM) antagonist that effectively inhibits calmodulin-activated Ca 2+ -phosphodiesterase (PDE) with an IC 50 of 28 μM. This compound also competitively inhibits trypsin-treated Ca 2+ -PDE with respect to cyclic GMP, exhibiting an IC 50 of 375 μM and a K i value of 300 μM.
1,2-Dilinoleoyl-3-oleoyl-rac-glycerol, a triacylglycerol, comprises linoleic acid at the sn-1 and sn-2 positions and oleic acid at the sn-3 position. This compound is present in the oils of ostrich and emu, and the fat body of male B. lapidarius bumblebees. It demonstrates efficacy in reducing scald development in Delicious apples, showing a 3% w v reduction when applied immediately after harvest and evaluated after six months of storage.
1,2-Dilinoleoyl-3-palmitoyl-rac-glycerol is a triacylglycerol featuring linoleic acid at the sn-1 and sn-2 positions and palmitic acid at the sn-3 position. Present in various vegetable oils such as poppy seed, hazelnut, maize, and olive, this compound (3% w v) effectively reduces scald development in Delicious apples when applied right after harvest, with results observed after six months of storage.
1-Isothiocyanato-6-(methylsulfenyl)-hexane, identified in wasabi (W. japonica), exhibits multifaceted biological activities. This isothiocyanate compound demonstrates antibacterial properties by inhibiting B. subtilis growth in an agar diffusion assay at 25 µmol disc, and antifungal effectiveness against T. mentagrophytes with a minimum inhibitory concentration (MIC) of 25 µg ml. Additionally, it acts as a repellent in the blue mussel (M. edulis) assay and shows antifouling capabilities on polyvinyl chloride (PVC) plates at a concentration of 50 µmol cm^2, underscoring its potential in biotechnological applications.