Lobaplatin (D-19466) is a diastereometric mixture of platinum(II) complexes containing a 1,2-bis(aminomethyl)cyclobutane stable ligand and lactic acid as the leaving group. Its antitumour activity results from the formation of DNA-drug adducts, mainly as GG and AG intra-strand cross-links. Lobaplatin influences the expression of the c-myc gene, which is involved in oncogenesis, apoptosis and cell proliferation[3]. Lobaplatin and paclitaxel inhibited SGC-7901 cell growth in a concentration and timedependent manner, with IC25 values at 48h of 1.97±0.17µg/ml and 1.98±0.19 ng/ml, respectively. Lobaplatin did not affect cyclin D1 and CDK4 protein expression, while cyclin E1 and CDK2 levels were significantly increased, with cyclin B1 amounts markedly decreased (p<0.05). More S phase cells were observed after lobaplatin treatment compared with controls (60.03±1.25 vs. 18.69±0.96%; p<0.05). Lobaplatin and paclitaxel combination did not affect cyclin D1 and CDK4 protein levels (p>0.05); meanwhile, cyclin E1 and CDK2 levels were increased, with reduced cyclin B1 amounts, compared with control values (p<0.05)[4].Lobaplatin inhibited proliferation of human HCC cells in a dose-dependent manner. For the most sensitive SMMC-7721 cells, lobaplatin arrested cell cycle progression in G1 and G2/M phases time-dependently which might be associated with the down-regulation of cyclin B, CDK1, CDC25C, phosphorylated CDK1 (pCDK1), pCDK4, Rb, E2F, and pRb, and the up-regulation of p53, p21, and p27[5].Lobaplatin inhibited the proliferation of human gastric cancer cells and induced apoptosis, which may be associated with the up-regulation of Bax expression, poly(ADP-ribose) polymerase (PARP) cleavage, p53 expression and the reduction of Bcl-2 expression[6].
Lobaplatin/络铂 细胞实验
Cell Line
Concentration
Treated Time
Description
References
SMMC7721 cells
1.536 µg/mL
117.2 hours
To investigate the radiosensitization effect of LBP on SMMC7721 cells, results showed that LBP significantly increased 125I-induced apoptosis.
Cell Death Dis. 2019 Oct 3;10(10):744
HepG2 cells
5.972 µg/mL
117.2 hours
To investigate the radiosensitization effect of LBP on HepG2 cells, results showed that LBP significantly increased 125I-induced apoptosis.
Cell Death Dis. 2019 Oct 3;10(10):744
SOSP-9607
7.94 µg/mL (SOSP-9607-Vector) and 10.04 µg/mL (SOSP-9607-FUBP1)
24 hours
To investigate the effect of FUBP1 overexpression on the sensitivity of SOSP-9607 cells to Lobaplatin. Results showed that FUBP1 overexpression increased the resistance of SOSP-9607 cells to Lobaplatin.
MedComm (2020). 2023 May 9;4(3):e257
MG63
14.95 µg/mL (MG63-Vector) and 28.36 µg/mL (MG63-FUBP1)
24 hours
To investigate the effect of FUBP1 overexpression on the sensitivity of MG63 cells to Lobaplatin. Results showed that FUBP1 overexpression increased the resistance of MG63 cells to Lobaplatin.
MedComm (2020). 2023 May 9;4(3):e257
HCT116 cells
0, 8, 16, 32 μg/ml
8 hours
To investigate the effect of Lobaplatin on the viability of HCT116 cells and its induction of pyroptosis. Results showed that Lobaplatin inhibited cell viability in a dose-dependent manner and induced cell swelling and large bubbles emerging from the plasma membrane, with TEM revealing multiple pores in the membrane.
Cell Death Dis. 2019 Feb 25;10(3):193
HT-29 cells
0, 8, 16, 32 μg/ml
8 hours
To investigate the effect of Lobaplatin on the viability of HT-29 and HCT116 cells and its induction of pyroptosis. Results showed that Lobaplatin inhibited cell viability in a dose-dependent manner and induced cell swelling and large bubbles emerging from the plasma membrane, with TEM revealing multiple pores in the membrane.
Cell Death Dis. 2019 Feb 25;10(3):193
SaOS-2 osteosarcoma cells
10 μg/mL
24 hours
To investigate the effect of rhIL-6 intervention on Lobaplatin resistance, results showed that rhIL-6 pretreatment reduced the sensitivity of osteosarcoma cells to Lobaplatin.
Cancer Cell Int. 2021 Oct 30;21(1):581
MCF-7 cells
5, 10, 50 mg/L
24 hours
To investigate the effect of lobaplatin on MCF-7 cell proliferation and apoptosis. Results showed that lobaplatin significantly reduced cell proliferation and increased cell apoptotic percentage.
Drug Des Devel Ther. 2018 Oct 29;12:3563-3571
Y79 retinoblastoma cells
5, 10, 20, 40 µg/ml
24, 48, 72 hours
To evaluate the inhibitory effect of lobaplatin on Y79 cell proliferation, results showed that lobaplatin significantly inhibited cell proliferation in a dose- and time-dependent manner and induced apoptosis.
Int J Oncol. 2020 Sep;57(3):697-706
Lobaplatin/络铂 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Nude mice
Osteosarcoma xenograft model
Subcutaneous injection
3 mg/kg
Every 3 days for 6 weeks
Evatanepag, as an EP2 receptor agonist, was used to stimulate the arachidonic acid metabolic pathway in FUBP1-silenced osteosarcoma cells to verify that FUBP1 promotes lobaplatin resistance in osteosarcoma cells through PTGES and the arachidonic acid metabolic pathway.
MedComm (2020). 2023 May 9;4(3):e257
Nude mice
Subcutaneous xenograft model
Intraperitoneal injection
3 mg/kg
Every 3 days for 6 weeks
To investigate the effect of FUBP1 on Lobaplatin resistance in vivo. Results showed that FUBP1 overexpression increased tumor resistance to Lobaplatin, while FUBP1 knockdown increased tumor sensitivity to Lobaplatin.
MedComm (2020). 2023 May 9;4(3):e257
BALB/c nude mice
Subcutaneous xenograft tumor model
Intraperitoneal injection
11 mg/kg
Tumor volume was monitored every 3 days, and mice were sacrificed at the end of the experiment
To investigate the inhibitory effect of Lobaplatin on colon cancer xenograft tumors. Results showed that Lobaplatin significantly inhibited tumor growth, and GSDME knockout did not affect the inhibitory effect of Lobaplatin on tumor formation.
Cell Death Dis. 2019 Feb 25;10(3):193
BALB/c nude mice
Y79 retinoblastoma xenograft model
Tail vein injection
750 µg/kg
Every 3 days for 1 or 2 weeks
To evaluate the inhibitory effect of lobaplatin on Y79 xenograft tumors, results showed that lobaplatin significantly inhibited tumor growth and was more effective than carboplatin.
China, Beijing
... 展开 >> Department of Radiation Oncology, National Cancer Center/National Clinical Research Center for Cancer/Cancer Hospital, Chinese Academy of Medical Sciences (CAMS) and Peking Union Medical College (PUMC)
Recruiting
Beijing, Beijing, China, 100021
Contact: Zefen Xiao, MD 收起 <<
IMRT With or Without Concurren... 展开 >>t Chemotherapy for Esophageal Cancer 收起 <<
Phase 3
Recruiting
December 31, 2022
China
... 展开 >> Department of Radiation Oncology, Cancer Hospital, National Cancer Center, Chinese Academy of Medical Sciences (CAMS) and Peking Union Medical College (PUMC)
Recruiting
Beijing, China, 100021
Contact: Xin Wang, MD +861013311583220 beryl_wx2000@163.com 收起 <<
China, Beijing
... 展开 >> Department of Radiation Oncology, Cancer Hospital, National Cancer Center, Chinese Academy of Medical Sciences (CAMS) and Peking Union Medical College (PUMC)
Recruiting
Beijing, Beijing, China, 100021
Contact: Zefen Xiao, MD 收起 <<
China, Beijing
... 展开 >> Department of Radiation Oncology, National Cancer Center/National Clinical Research Center for Cancer/Cancer Hospital, Chinese Academy of Medical Sciences (CAMS) and Peking Union Medical College (PUMC)
Recruiting
Beijing, Beijing, China, 100021
Contact: Zefen Xiao, MD 收起 <<
IMRT With or Without Concurren... 展开 >>t Chemotherapy for Esophageal Cancer 收起 <<
Phase 3
Recruiting
December 31, 2022
China
... 展开 >> Department of Radiation Oncology, Cancer Hospital, National Cancer Center, Chinese Academy of Medical Sciences (CAMS) and Peking Union Medical College (PUMC)
Recruiting
Beijing, China, 100021
Contact: Xin Wang, MD +861013311583220 beryl_wx2000@163.com 收起 <<
China, Beijing
... 展开 >> Department of Radiation Oncology, Cancer Hospital, National Cancer Center, Chinese Academy of Medical Sciences (CAMS) and Peking Union Medical College (PUMC)
Recruiting
Beijing, Beijing, China, 100021
Contact: Zefen Xiao, MD 收起 <<
China, Guangdong
... 展开 >>
Cancer Center Sun Yat-sen University
Recruiting
Guangzhou, Guangdong, China
Contact: Ming Shi, MD 86-2087343582 ext 86-2087343582 shiming@mail.sysu.edu.cn
Contact: Rong Ping Guo, MD 86-2087343117 ext 86-2087343117 guorongp@mail.sysu.edu.cn
Principal Investigator: Ming Shi, MD 收起 <<
China, Guangdong
... 展开 >>
Cancer Center Sun Yat-sen University
Recruiting
Guangzhou, Guangdong, China
Contact: Ming Shi 86-2087343582 ext 86-2087343582 shiming@mail.sysu.edu.cn
Contact: Ping Rong Guo 86-2087343117 ext 86-2087343117 guorongp@mail.sysu.edu.cn
Principal Investigator: Ming Shi 收起 <<
China, Guangdong
... 展开 >>
Minimally Invasive Interventional Division, Medical Imaging Center, Sun Yat-sen University Cancer Center,
Recruiting
Guangzhou, Guangdong, China, 500060
Contact: Ming Zhao, doctor +86 020 87343272 zhaoming@sysucc.org.cn
Contact: Tao Pan, doctor +86 020 87343271 pantao0909@hotmail.com 收起 <<
China, Guangdong
... 展开 >>
Minimally Invasive Interventional Division, Medical Imaging Center, Sun Yat-sen University Cancer Center,
Recruiting
Guangzhou, Guangdong, China, 500060
Contact: Ming Zhao, doctor +86 020 87343272 zhaoming@sysucc.org.cn 收起 <<
Extensive Stage Small Cell Lun... 展开 >>g Cancer 收起 <<
Phase 2
Unknown
December 2018
China, Liaoning
... 展开 >>
The First Affiliated Hospital of China Medical University
Recruiting
Shenyang, Liaoning, China, 110001
Contact: mingfang zhao, professor 13644055129 收起 <<
China, Guizhou
... 展开 >> The affiliated hospital of Guizhou medical university
Recruiting
Guiyang, Guizhou, China, 550004
Contact: Shengfa Su, PhD,MD 86-13608550432 sushengfa2005@163.com 收起 <<
China, Guizhou
... 展开 >> The affiliated hospital of Guizhou medical university
Recruiting
Guiyang, Guizhou, China, 550004
Contact: Shengfa Su, PhD,MD 86-13608550432 sushengfa2005@163.com 收起 <<
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