Deoxypodophyllotoxin not only has pharmacological effects such as anti-allergy,anti-angiogenesis and liver protection,but also has good anti-tumor activity.It can play an anti-tumor role by inhibiting cell viability,i...Deoxypodophyllotoxin not only has pharmacological effects such as anti-allergy,anti-angiogenesis and liver protection,but also has good anti-tumor activity.It can play an anti-tumor role by inhibiting cell viability,inducing apoptosis,blocking cell cycle and inhibiting cell migration.In this paper,the related research on pharmacological effect and mechanism of deoxypodophyllotoxin is reviewed,to lay a foundation for the follow-up study of deoxypodophyllotoxin and drug development.展开更多
Seven novel spin labeled derivatives of 4＇-demethyl-4-deoxypodophyllotoxin with nitroxyl radi- cals（TMHPO and TMPRO） were prepared and their cytotoxic and antioxidative activities were tested. Their cytotoxic activ...Seven novel spin labeled derivatives of 4＇-demethyl-4-deoxypodophyllotoxin with nitroxyl radi- cals（TMHPO and TMPRO） were prepared and their cytotoxic and antioxidative activities were tested. Their cytotoxic activities were tested against two tumor cell lines（A-549 and HL-60） in vitro. Among them, five compounds show higher inhibition activity against A-549 cells compared with the clinical drug VP-16（2） and parent compound 4＇-demethyl-4-deoxypodophyllotoxin（DDPT, 6）. Compounds 8, 10 and 13 show excellent inhibition activity against HL-60 cells. Furthermore, the antioxidative activities of them were tested. All the seven spin labeled compounds show stronger antioxidative activity compared with VP-16（2） and DDPT（6）. The partition coefficients P of these derivatives were determined.展开更多
The therapeutic application of deoxypodophyllotoxin(DPT) is limited due to its poor water solubility and stability. In the present study, the micelles assembled by the amphiphilic block copolymers(m PEG-PDLLA) were co...The therapeutic application of deoxypodophyllotoxin(DPT) is limited due to its poor water solubility and stability. In the present study, the micelles assembled by the amphiphilic block copolymers(m PEG-PDLLA) were constructed to improve the solubility and safety of DPT for their in vitro and in vivo application. The central composite design was utilized to develop the optimal formulation composed of 1221.41 mg m PEG-PDLLA, the weight ratio of 1 : 4(m PEG-PDLLA : DPT), 30 m L hydration volume and the hydration temperature at 40 oC. The results showed that the micelles exhibited uniformly spherical shape with the diameter of 20 nm. The drug-loading and entrapment efficiency of deoxypodophyllotoxin-polymeric micelles(DPT-PM) were about(20 ± 2.84)% and(98 ± 0.79)%, respectively, indicating that the mathematical models predicted well for the results. Compared to the free DPT, the cytotoxicity showed that blank micelles possessed great safety for Hela cells. In addition, the DPT loaded micelle formulation achieved stronger cytotoxicity at the concentration of 1 × 10^(-7) mol·L^(-1), which showed significant difference from free DPT(P < 0.05). In conclusion, the micelles were highly promising nano-carriers for the anti-tumor therapy with DPT.展开更多
基金Supported by the Talent Training Program for the Reform and Development of Local Colleges and University of the Central Government(2020GSP16)Innovation and Entrepreneurship Training Program for College Students in Heilongjiang Province(202210223048)。
文摘Deoxypodophyllotoxin not only has pharmacological effects such as anti-allergy,anti-angiogenesis and liver protection,but also has good anti-tumor activity.It can play an anti-tumor role by inhibiting cell viability,inducing apoptosis,blocking cell cycle and inhibiting cell migration.In this paper,the related research on pharmacological effect and mechanism of deoxypodophyllotoxin is reviewed,to lay a foundation for the follow-up study of deoxypodophyllotoxin and drug development.
基金Supported by the State Key Laboratory of Applied Organic Chemistry, Lanzhou University, China(2009)
文摘Seven novel spin labeled derivatives of 4＇-demethyl-4-deoxypodophyllotoxin with nitroxyl radi- cals（TMHPO and TMPRO） were prepared and their cytotoxic and antioxidative activities were tested. Their cytotoxic activities were tested against two tumor cell lines（A-549 and HL-60） in vitro. Among them, five compounds show higher inhibition activity against A-549 cells compared with the clinical drug VP-16（2） and parent compound 4＇-demethyl-4-deoxypodophyllotoxin（DDPT, 6）. Compounds 8, 10 and 13 show excellent inhibition activity against HL-60 cells. Furthermore, the antioxidative activities of them were tested. All the seven spin labeled compounds show stronger antioxidative activity compared with VP-16（2） and DDPT（6）. The partition coefficients P of these derivatives were determined.
基金supported by the Ministry of Science and Technology of China(No.2014ZX09507001006)the National Natural Science Foundation of China(No.81501579)+2 种基金the Natural Science Foundation of Jiangsu Province(No.BK20150702)the Science and Technology Development Fund of Nanjing Medical University(No.2016NJMU105)the Priority Academic Program Development of Jiangsu Higher Education Institutions
文摘The therapeutic application of deoxypodophyllotoxin(DPT) is limited due to its poor water solubility and stability. In the present study, the micelles assembled by the amphiphilic block copolymers(m PEG-PDLLA) were constructed to improve the solubility and safety of DPT for their in vitro and in vivo application. The central composite design was utilized to develop the optimal formulation composed of 1221.41 mg m PEG-PDLLA, the weight ratio of 1 : 4(m PEG-PDLLA : DPT), 30 m L hydration volume and the hydration temperature at 40 oC. The results showed that the micelles exhibited uniformly spherical shape with the diameter of 20 nm. The drug-loading and entrapment efficiency of deoxypodophyllotoxin-polymeric micelles(DPT-PM) were about(20 ± 2.84)% and(98 ± 0.79)%, respectively, indicating that the mathematical models predicted well for the results. Compared to the free DPT, the cytotoxicity showed that blank micelles possessed great safety for Hela cells. In addition, the DPT loaded micelle formulation achieved stronger cytotoxicity at the concentration of 1 × 10^(-7) mol·L^(-1), which showed significant difference from free DPT(P < 0.05). In conclusion, the micelles were highly promising nano-carriers for the anti-tumor therapy with DPT.
