Application of 3,4-split-ring cycloartane type tetracyclic triterpenoid compound or pharmaceutically acceptable salt thereof in preparation of anti-cancer drugs
A technology of cycloartenane and tetracyclic triterpenes, which is applied in the field of preparing anticancer drugs and can solve the problems of incomplete biological activity research and the like
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Embodiment 1
[0068] The in vitro anticancer activity assay experiment of 3,4-splitting cycloartane-type tetracyclic triterpenes is as follows:
[0069] 1. Experimental operation
[0070] (1) Cell culture and passage
[0071] The cancer cell lines involved in this example include: human liver cancer cell line Huh7, human liver cancer cell line HepG2, human non-small cell lung cancer cell line A549, human breast cancer cell line MCF-7, human triple negative breast cancer cell line MDA- MB-231, human colon cancer cell line SW480, human pancreatic cancer cell line PANC-1, human prostate cancer cell line PC3, human cervical cancer cell line Hela, and human kidney cancer cell line 786-O. All cell lines were provided by the Systems Biology Laboratory, Department of Biology, Southern University of Science and Technology.
[0072] MCF-7, SW480, PC3, PANC-1, 786-O cells were cultured in RPMI-1640 medium containing 10% FBS (fetal bovine serum), 100 U / mL penicillin, and 100 U / mL streptomycin, Place...
Embodiment 2
[0108] Study on the structure-activity relationship of 3,4-cleaved cycloartane-type compounds with phenylacrylic acid substituents:
[0109] The compound core numbers are as follows:
[0110]
[0111] According to the data results in Table 2, compare 10 belts of 1GJ-5I5A, 2GJ-5I5B, 3GJ-5J9A, 4GJ-5J8C2, 5GJ-5J6A, 6GJ-5K6A, 7GJ-5H8A, 8GJ-5K10A, 11GJ-5L11C and 12GJ-5J10E1 IC of 3,4-Split Cycloartane Type Compounds with Phenyl Acrylic Acid Substituent 50 The structure-activity relationship can be concluded as follows:
[0112] After the C-2 carboxyl group is changed into an ester group, the activity decreases by about 1 times;
[0113] After the C-4 carbon-carbon double bond becomes a single bond, the activity decreases by 1-2 times;
[0114] The cis-trans isomerization of the C-2' carbon-carbon double bond, the activity of the trans structure is 1-2 times higher than that of the cis structure;
[0115] The cis-trans isomerization of the C-24 carbon-carbon double bond, the ...
Embodiment 3
[0121] Study on the structure-activity relationship of 3,4-splitting cycloartane-type compounds without phenylacrylic acid substituents:
[0122] In this example, the structure-activity relationship of 3,4-splitting cycloartane-type tetracyclic triterpenes XI, XII, XIII, XIV, XV, and XVI without the substitution of phenylacrylic acid was studied. According to the method described in Example 1, these five compounds of XII-XVI act on human breast cancer cell MCF7, and the curve between cell viability and drug concentration is as follows Figure 23 Shown, wherein the IC of compound XII 50 IC of compound XIII was 44.70 μM 50 was 42.21 μM, and the IC of the other three compounds 50 >100μM, lower activity. and with IC 50 Compared to Compound XI at 19.96 μM, an activity versus structure relationship can be drawn.
[0123] The compound core numbers are as follows:
[0124]
[0125] Summarized as follows:
[0126] After the C-2 carboxyl group is changed to an ester group, the...
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