Novel macrolide compounds with antibiotic and antneoplastic properties
A compound and composition technology, applied in the field of new macrolide compounds with antibacterial and antitumor activities, can solve the problems of the existence and application of WBI-3001 that have not been recorded
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Embodiment 1
[0030] Example 1. Preparation and isolation of WBI-3001 from the culture broth of pathogenic bacteria burgdorferi
[0031] Primary cultures of P. burgdorferi were maintained for 14 days before secondary cultures were performed. Primary cultures of the inoculum (Inocula) were prepared by adding one loop of culture to 50 ml of Tryptic Soy Broth (TSB) in a 100 ml Erlenmeyer flask. Cultures were shaken at 120 rpm on an Eberbach gyrorotary shaker for 24 hours at 25°C. Bacterial fermentation was started by adding 100 ml of this bacterial culture to 900 ml of TSB in a 2000 ml flask. Flasks were incubated in the dark at 25°C on an Eberbach rotary shaker. After 96 hours, the culture was immediately subjected to centrifugation (12,000хg, 20 minutes, 4°C) to isolate bacterial cells. Xenobacterium burgdorferi was inoculated into twenty liters of medium. The inoculated medium was incubated at 37°C for 3 days. Then, the medium was triturated and extracted three times with 20 L of ethyl...
example 2
[0032] Example 2. Identification of WBI-3001
[0033] NMR spectra were obtained on a Bruker WM600 spectrometer using C5D5N5. Low resolution MS was obtained by a HP 5985B gc / ms system operating at 7OeV using a direct probe. CIMS spectra were obtained by the same equipment as above using isobutane. High resolution MS was obtained with a Kratos MS80 device. HPLC and UV analyzes were performed with a Waters 2695 equipped with a Waters 996 PDA detector.
[0034] 1 H NMR (C5D5N) (600Hz) δ0.87 (dd, 6H, J = 7.2Hz), 1.42 (mult., 1H), 1.83 (mult., 2H), 1.92 (mult., 2H), 2.21 (mult. ,1H),2.35(mult.,1H),2.94(dd,1H,J=16Hz,J=3Hz),3.21(dd,1H,J=16Hz,J=13Hz),3.41(mult.,1H), 4.40(mult.,1H),4.66(mult.,1H),4.72(dd.,1H,J=16Hz,J=3Hz),4.88(d,1H,J=6Hz),5.02(dd,1H,J =6Hz, J=3Hz), 6.62(d, 1H, J=7Hz), 6.97(d, 1H, J=8Hz), 7.35(t, 1H, J=8Hz), 8.78(d, 1H, J=9Hz ).
[0035] 13 C NMR (C5D5N) (600Hz) δ21.76 (C-1), 23.41 (C-1'), 24.70 (C-8), 24.94 (C-2), 25.91 (C-7), 30.10 (C- 6), 39.93(C-3), 45.53(C...
example 3
[0038] Example 3. WBI-3001 as an antibacterial agent
[0039] The following experiments were performed, which showed the antibacterial properties of WBI-3001. To determine the minimum inhibitory concentration (MIC) of WBI-3001, a standard dilution method was used. Tests were performed at 35°C and MICs were determined after 24 hours of incubation.
[0040] Table 1 shows the MICs determined for the inhibition of each microorganism by these compounds. It was concluded that WBI-3001 isolated from Xenorhabdus has potent antibacterial properties, especially against some antibiotic-resistant Staphylococcus strains.
[0041] Table 1: MICs of WBI-3001 and erythromycin in tryptic soybean broth at time points of 24hr and 48hr (note: the unit of MIC value is μg / ml).
[0042] bacterial sample WBI-3001 Erythromycin Escherichia coli 4 1 Staphylococcus epidermidis 8 0.25 Staphylococcus aureus MSRA* (S.aureus MSRA) 4 >32 Enterococcus faecalis 32 >32 ...
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