Camptothecin Chemotherapy
Extract powder camptothecin (CPT) is a type of pyrroloquinoline cytotoxic alkaloid and is one of the most studied natural anti-cytopathic drugs besides Paclitaxel. It is present in the fruits or roots of Camptotheca acuminata, a plant of the Davidia family. Camptotheca acuminata, also known as Eclipta, water chestnut, thousand-foot tree, etc., is a tall deciduous tree. Its root bark clears away heat and, detoxifies, disperses knots, and reduces swelling. The fruit has the effect of activating blood circulation and removing blood stasis. It is often used to treat psoriasis, sores, swelling, and other symptoms.
Researchers found that the pentacyclic monoterpene alkaloid showed vigorous anti-lesion activity on Hela cells (cervical foul cell line), L1210 cells (mouse lymphocytic leukemia cells), and rodents in vitro, and also shows that it has specific curative effects on various malignant lesions such as stomach, rectum, and leukemia, which triggered an upsurge of research on plant camptothecin and CPT compounds in the scientific community. Since discovering that it has topoisomerase I inhibitory effects, people have been committed to finding highly efficient and low-toxic CPT derivatives. So far, a series of semi-synthetic and fully synthetic CPT derivatives have appeared and entered clinical practice application or clinical trial stage.
Recent research has found that it may also have a weight-loss effect. In experiments on mice, it can promote the expression level of growth differentiation factor 15 (GDF 15), thereby inhibiting the food intake of mice and significantly reducing the weight of mice. Experimental data suggest that it may have therapeutic benefits against obesity and its associated metabolic disorders, providing a promising new avenue for the development of anti-obesity drugs. If you are also interested in chemotherapy drugs, please get in touch with Xi'an Sonwu. Xi'an Sonwu can provide you with pure camptothecin.
What Is Camptothecin Used For
1. Lung disease
Pulmonary disease is a common primary malignant lung disease originating from bronchial mucosa or glands. It may be related to smoking, air pollution, ionizing radiation, etc. Patients may experience symptoms such as cough, sputum, and blood in the sputum.
2. Breast disease
Breast disease refers to the uncontrolled proliferation of breast epithelial cells under the action of a variety of carcinogens. It is a malignant cell. Patients may experience breast lumps, breast skin abnormalities, nipple discharge, and other symptoms.
3. Lymphatic diseases
Lymphatic diseases are malignant lesions originating from the lymphatic hematopoietic system. They may be related to infection, immune, physical and chemical factors, etc. Patients may experience fever, night sweats, and weight loss symptoms.
4. Neuroblast diseases
Neuroblastic disease is a common neuroendocrine disorder caused mainly by genetics. Patients may experience fever, abdominal pain, bloating, other symptoms, skin itching, difficulty breathing, and other symptoms.
5. Other diseases
In addition, CPT can also be used to treat melanoma, nephroblastoma, retinoblastomas, and other diseases.
What Is The Mechanism Of Action Of Camptothecins
CPT molecules selectively inhibit topoisomerase Ⅰ (Topo Ⅰ), bind to the complex formed by Topo Ⅰ-DNA, and stabilize this complex so that the broken DNA strand cannot be rejoined, preventing DNA replication and RNA synthesis and providing cells with Drugs specific to the S phase of the cycle do not affect cells in the G0 phase, but have slight lethality on cells in the G1, G2 and M phases. In addition, it can directly damage the DNA structure. DNA topoisomerase is an essential enzyme widely present in organisms. It affects DNA topology by regulating supercoiling, chaining, delinking, and nucleic acid dissociation. It is mainly divided into topoisomerase I (Topoisomerase I, Topo I ) and topoisomerase Ⅱ (Topoisomerase Ⅱ, Topo Ⅱ). Compared with Topo II inhibitors, Topo I inhibitors have high efficacy and a broad anti-badspectrum and have become essential target enzymes for designing new anti-lesion drugs. At the same time, the Topo I content in various diseased cells such as colon, cervix, and ovarian diseases is much higher than in normal tissues, and its activity in S-phase bad cells is significantly increased. Therefore, drugs that inhibit Topo I can selectively inhibit the DNA replication of harmful cells in the proliferative phase have better selectivity. Experiments have proven that TopoⅠ is the main target of CPT and its analogs.
CPT can stabilize the covalent compounds of usually dissociated TopoI and DNA chains. With the formation of cleavable complexes, the DNA cleavage and relinking reactions initially mediated by TopoI are inhibited. The replication fork formed during DNA replication in the S phase conflicts with the broken DNA chain, causing irreversible replication fork blockage, double-stranded DNA breaks, and reversible cleavable complexes transforming into irreversible complexes, resulting in cellular death.
Camptothecin Stack Side Effects
1. Common combinations include combined use with chemotherapy drugs such as Cisplatin, Paclitaxel, Carboplatin, etc.
Combination application with cisplatin treats certain diseases to exert its synergistic anti-lesion effect. Treatment for multiple conditions, such as pancreatic, small-cell lung, and ovarian, is frequently accomplished with this combination of medications. By combining it with cisplatin, an enhanced anti-lesion effect can be expected, as they may act on bad cells through different mechanisms, resulting in a synergistic effect.
Combination with Paclitaxel is widely studied and used in treatment. This combined treatment regimen is often used to treat a variety of malignant lesions such as breast, ovarian, and lung diseases. CPT and Paclitaxel act on bad cells through different mechanisms, so their combined application can exert a synergistic anti-lesion effect. Camptothecin interferes with DNA synthesis and repair by inhibiting topoisomerase I, while Paclitaxel blocks cell mitosis and prevents alarming cell proliferation by promoting microtubule polymerization.
Combined application with carboplatin is commonly used to treat a variety of malignant lesions, including ovary, stomach, and lung. This combined treatment regimen can produce synergistic inhibitory effects on bad cells through two mechanisms, enhancing anti-bad development. Camptothecin interferes with DNA synthesis and repair by inhibiting topoisomerase I, while carboplatin induces DNA damage and apoptosis in cells by cross-linking DNA strands. Therefore, combining these two drugs may produce complementary antilesional effects.
2. When used in conjunction with other anti-bad drugs, it may cause a series of adverse reactions and side effects. Common side effects include:
Myelosuppression: This may result in a drop in platelets, which raises the danger of bleeding and congestion; a reduction in red blood cells, which results in anemia and exhaustion; and a decrease in white blood cells, which increases the patient's susceptibility to infection.
Nausea, vomiting, diarrhea: Gastrointestinal reactions are common side effects that may affect the patient's quality of life.
Hair loss: Hair thinning or loss may occur during treatment.
Neurotoxicity: May cause neurological-related adverse reactions such as abnormal sensation, numbness of hands and feet, and neuralgia.
Liver function damage: It may lead to abnormal liver function, manifested as jaundice, elevated liver enzymes, and other symptoms.
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