2015
DOI: 10.1097/cad.0000000000000210
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N-Farnesyloxy-norcantharimide and N-farnesyl-norcantharimide inhibit the progression of leukemia and increase survival days in a syngeneic mouse leukemia model

Abstract: This study investigated the anticancer effects of two newly synthesized norcantharidin analogs, N-farnesyloxy-norcantharimide (NOC15) and N-farnesyl-norcantharimide (NC15), in L1210 cells and in a syngeneic mouse leukemia model (L1210 cell line plus DBA/2 mice). We found that the half-maximal inhibitory concentration (IC50) of NOC15 and NC15 on L1210 cells is 1.56 and 2.62 μmol/l, respectively, and that the IC50 of NOC15 and NC15 on human normal lymphoblast is 207.9 and 2569 μmol/l, respectively. In cell cycle… Show more

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Cited by 6 publications
(6 citation statements)
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“…Tail vein injection was performed with 1 × 10 6 cells/mouse. Through the detection of the number of white blood cells (WBC) in peripheral blood (PB) as well as the leukemia cell infiltration, whether mouse models of leukemia were successfully established was detected (Chang et al, , Trifirò et al, ). The mice models were randomly assigned into the model group, negative control (NC) group, HOTAIR mimics group (transfected with HOTAIR mimics, a nucleic acid sequence enhancing the expression of HOTAIR; Ji, Wuerkenbieke, He, & Ding, ), small interfering RNA (siRNA) HOTAIR group (transfected with siRNA targeting HOTAIR, a nucleic acid sequence reducing the expression of HOTAIR), xav‐939 (the Wnt/β‐catenin signaling pathway inhibitor) group, and HOTAIR mimics + xav‐939 group, with a normal group (10 mice with tail vein injection of 0.1 ml normal saline) acting as the control.…”
Section: Methodsmentioning
confidence: 99%
“…Tail vein injection was performed with 1 × 10 6 cells/mouse. Through the detection of the number of white blood cells (WBC) in peripheral blood (PB) as well as the leukemia cell infiltration, whether mouse models of leukemia were successfully established was detected (Chang et al, , Trifirò et al, ). The mice models were randomly assigned into the model group, negative control (NC) group, HOTAIR mimics group (transfected with HOTAIR mimics, a nucleic acid sequence enhancing the expression of HOTAIR; Ji, Wuerkenbieke, He, & Ding, ), small interfering RNA (siRNA) HOTAIR group (transfected with siRNA targeting HOTAIR, a nucleic acid sequence reducing the expression of HOTAIR), xav‐939 (the Wnt/β‐catenin signaling pathway inhibitor) group, and HOTAIR mimics + xav‐939 group, with a normal group (10 mice with tail vein injection of 0.1 ml normal saline) acting as the control.…”
Section: Methodsmentioning
confidence: 99%
“…NOC15 was obtained as a colorless liquid; the details of the 1 H and 13 C NMR spectra have been described in a previous report. The molecular weight for C 23 H 33 NO 4 calculated using LC-MS (ESI + , m/z ) is 387.24, found for 410.21 [M+Na] + 26 , 27 .…”
Section: Methodsmentioning
confidence: 99%
“…N -Farnesyloxy-norcantharimide (NOC15, C 23 H 33 NO 4 ), which is a newly synthesized NCTD derivative with the N -farnesyloxy group, has high anticancer activity toward hepatocellular carcinoma, bladder carcinoma, colorectal adenocarcinoma, and acute promyelocytic leukemia 26 . NOC15 also has anticancer efficacy in a syngeneic mouse leukemia model by increasing the survival of mice and decreasing the tumor weight 27 . However, the anticancer mechanism of NOC15 is not clear.…”
Section: Introductionmentioning
confidence: 99%
“…[ 17 ] Both NOC15 and NC15 have higher anticancer activities against hepatocellular carcinoma, bladder carcinoma, colorectal adenocarcinoma, and acute promyelocytic leukemia than NCTD, [ 17 ] and can increase the survival days of mice, decrease the tumor weight, and retard the decrease in the weight of the spleen in a syngeneic mouse leukemia model. [ 18 ]…”
Section: Introductionmentioning
confidence: 99%