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Cancer is a major disease that seriously endangers human life and health.
Human mortality due to cancer accounts for the second highest mortality rate of all diseases
.
Anticancer drug therapy (chemotherapy) is one of the main means of clinical cancer treatment
.
Anticancer drugs inhibit the proliferation of tumor cells through different mechanisms of action, and even achieve the effect of killing tumor cells
.
At present, traditional anticancer drugs commonly used in clinic can be divided into alkylating agents, antimetabolites, antitumor antibiotics and hormones
.
However, these anticancer drugs have poor recognition and selectivity for tumor cells, and they can kill many fast-growing normal cells in the human body while inhibiting or killing tumor cells
.
Therefore, to eliminate cancer cells, it is almost "killing a thousand enemies and destroying eight hundred", which is the "side effect" of chemotherapy that everyone often hears
.
To find chemotherapeutic measures with high cure rates and low side effects, efforts have been made to develop a class of antitumor prodrugs that can be selectively activated by characteristic factors such as tumor cells or the tumor microenvironment
.
So, what is a prodrug? The so-called prodrugs, also known as prodrugs, refer to the compounds obtained by chemical structure modification which are inactive or less active in vitro, and are converted in vivo by factors such as enzymes or non-enzymes to release the compounds that exert their medicinal effects
.
To this end, traditional anticancer drugs are designed as prodrugs selectively activated by characteristic factors of tumor cells, which can release anticancer drugs at the tumor site and play a role in treating tumors, effectively reducing the effect of anticancer drugs on normal cells.
Cell toxicity, while improving the efficacy of anticancer drugs, has become an important part of the current anticancer drug research and development
.
Information on the release process and biodistribution of prodrugs in vivo is crucial to the efficacy of anticancer drugs, and real-time accurate tracking of prodrugs in vivo is also helpful for the development of new anticancer drugs
.
However, how to observe the drug release process and biodistribution of anticancer prodrugs in vivo in real time is a difficult and core problem that urgently needs to be solved by analytical scientists
.
The design and research of prodrugs for diagnosis and treatment can effectively solve this problem, which has attracted extensive attention of researchers in recent years
.
As a kind of prodrug, diagnosis and treatment prodrugs have dual functions of diagnosis and treatment.
They can realize the controlled release of drugs at the tumor site, monitor the release of active drugs, and timely feedback the therapeutic effect (Figure 1)
.
Through this prodrug molecule, people can visually monitor and judge the activity of drug molecules in the body, and at the same time provide an important basis for doctors to formulate reasonable drug regimens according to the treatment situation of the drug in the body and the development of the disease
.
Figure 1 Schematic diagram of diagnosis and treatment prodrugs (from Lee et al.
Chem.
Soc.
Rev.
, 2018, 47, 28-52) The team of Shi Yanping, Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences focused on the delivery and targeted drug release process of anticancer drugs A series of research work has been carried out on the precise tracer
.
Recently, Dr.
Zhao Xiaobo of the team designed and prepared an innovative diagnosis and treatment prodrug NMAC4A-CyNH2 based on the characteristics of tumor hypoxic microenvironment and the innovative concept of non-covalent binding
.
The diagnostic prodrug is designed and synthesized by an anticancer prodrug (NMAC4A) and a near-infrared probe (CyNH2) through a host-guest non-covalent assembly (Figure 2)
.
Figure 2 Schematic diagram of preparation (a) and release (b) of NMAC4A-CyNH2, a diagnostic prodrug targeting tumor hypoxic microenvironment molecule (NM), while illuminating the fluorescent signal
.
Using the synchronization between the release of anti-tumor drug molecules and the opening of the fluorescent signal, the visual monitoring and tracking of the targeted drug release process of anti-tumor drug molecules in vitro and in vivo can be realized
.
As shown in Figure 3, the researchers used the prepared diagnostic prodrug NMAC4A-CyNH2 to visually monitor the release of drug molecule NM in tumor cells by laser confocal microscopy
.
Subsequently, by injecting NMAC4A-CyNH2 into tumor-bearing mice, and using a small animal in vivo imager, real-time monitoring of the directional release of drug molecules was achieved in mice
.
In addition, the researchers further verified the targeted activation properties of NMAC4A-CyNH2 in tumor tissues at the molecular level using mass spectrometry imaging
.
Fig.
3 Imaging images of NMAC4A-CyNH2 in tumor cells (a) and tumor-bearing mice (b) In general, the development of novel prodrugs for diagnosis and treatment not only enables the release and effect of anticancer drugs at the tumor site , and the release process of anticancer prodrugs in tumor cells and animals can be seen in real time
.
This research has strong practicability and operability, and can provide an effective tool for the targeted delivery and precise tracking of anticancer drug molecules at tumor sites, which is expected to provide anticancer drug development and personalized treatment of tumors.
important opportunity
.
This work was supported by the National Natural Science Foundation of China
.
Source: Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences
Human mortality due to cancer accounts for the second highest mortality rate of all diseases
.
Anticancer drug therapy (chemotherapy) is one of the main means of clinical cancer treatment
.
Anticancer drugs inhibit the proliferation of tumor cells through different mechanisms of action, and even achieve the effect of killing tumor cells
.
At present, traditional anticancer drugs commonly used in clinic can be divided into alkylating agents, antimetabolites, antitumor antibiotics and hormones
.
However, these anticancer drugs have poor recognition and selectivity for tumor cells, and they can kill many fast-growing normal cells in the human body while inhibiting or killing tumor cells
.
Therefore, to eliminate cancer cells, it is almost "killing a thousand enemies and destroying eight hundred", which is the "side effect" of chemotherapy that everyone often hears
.
To find chemotherapeutic measures with high cure rates and low side effects, efforts have been made to develop a class of antitumor prodrugs that can be selectively activated by characteristic factors such as tumor cells or the tumor microenvironment
.
So, what is a prodrug? The so-called prodrugs, also known as prodrugs, refer to the compounds obtained by chemical structure modification which are inactive or less active in vitro, and are converted in vivo by factors such as enzymes or non-enzymes to release the compounds that exert their medicinal effects
.
To this end, traditional anticancer drugs are designed as prodrugs selectively activated by characteristic factors of tumor cells, which can release anticancer drugs at the tumor site and play a role in treating tumors, effectively reducing the effect of anticancer drugs on normal cells.
Cell toxicity, while improving the efficacy of anticancer drugs, has become an important part of the current anticancer drug research and development
.
Information on the release process and biodistribution of prodrugs in vivo is crucial to the efficacy of anticancer drugs, and real-time accurate tracking of prodrugs in vivo is also helpful for the development of new anticancer drugs
.
However, how to observe the drug release process and biodistribution of anticancer prodrugs in vivo in real time is a difficult and core problem that urgently needs to be solved by analytical scientists
.
The design and research of prodrugs for diagnosis and treatment can effectively solve this problem, which has attracted extensive attention of researchers in recent years
.
As a kind of prodrug, diagnosis and treatment prodrugs have dual functions of diagnosis and treatment.
They can realize the controlled release of drugs at the tumor site, monitor the release of active drugs, and timely feedback the therapeutic effect (Figure 1)
.
Through this prodrug molecule, people can visually monitor and judge the activity of drug molecules in the body, and at the same time provide an important basis for doctors to formulate reasonable drug regimens according to the treatment situation of the drug in the body and the development of the disease
.
Figure 1 Schematic diagram of diagnosis and treatment prodrugs (from Lee et al.
Chem.
Soc.
Rev.
, 2018, 47, 28-52) The team of Shi Yanping, Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences focused on the delivery and targeted drug release process of anticancer drugs A series of research work has been carried out on the precise tracer
.
Recently, Dr.
Zhao Xiaobo of the team designed and prepared an innovative diagnosis and treatment prodrug NMAC4A-CyNH2 based on the characteristics of tumor hypoxic microenvironment and the innovative concept of non-covalent binding
.
The diagnostic prodrug is designed and synthesized by an anticancer prodrug (NMAC4A) and a near-infrared probe (CyNH2) through a host-guest non-covalent assembly (Figure 2)
.
Figure 2 Schematic diagram of preparation (a) and release (b) of NMAC4A-CyNH2, a diagnostic prodrug targeting tumor hypoxic microenvironment molecule (NM), while illuminating the fluorescent signal
.
Using the synchronization between the release of anti-tumor drug molecules and the opening of the fluorescent signal, the visual monitoring and tracking of the targeted drug release process of anti-tumor drug molecules in vitro and in vivo can be realized
.
As shown in Figure 3, the researchers used the prepared diagnostic prodrug NMAC4A-CyNH2 to visually monitor the release of drug molecule NM in tumor cells by laser confocal microscopy
.
Subsequently, by injecting NMAC4A-CyNH2 into tumor-bearing mice, and using a small animal in vivo imager, real-time monitoring of the directional release of drug molecules was achieved in mice
.
In addition, the researchers further verified the targeted activation properties of NMAC4A-CyNH2 in tumor tissues at the molecular level using mass spectrometry imaging
.
Fig.
3 Imaging images of NMAC4A-CyNH2 in tumor cells (a) and tumor-bearing mice (b) In general, the development of novel prodrugs for diagnosis and treatment not only enables the release and effect of anticancer drugs at the tumor site , and the release process of anticancer prodrugs in tumor cells and animals can be seen in real time
.
This research has strong practicability and operability, and can provide an effective tool for the targeted delivery and precise tracking of anticancer drug molecules at tumor sites, which is expected to provide anticancer drug development and personalized treatment of tumors.
important opportunity
.
This work was supported by the National Natural Science Foundation of China
.
Source: Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences
