| Catalog No | Package | Original Price | Price | Inventory | Quantity | Operating |
|---|---|---|---|---|---|---|
| BP0324-20mg | 20mg | $30.00 | Sign in |
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Synonym name:
Catalogue No.: BP0324
Cas No.: 2468-21-5
Formula: C21H24N2O2
Mol Weight: 336.435
Botanical Source: Alkaloid from Catharanthus ovalis and other Catharanthus spp. and from Vinca rosea (Apocynaceae)
Purity: 95%~99%
Analysis Method: HPLC-DAD or/and HPLC-ELSD
Identification Method: Mass, NMR
Packing: Brown vial or HDPE plastic bottle
Can be supplied from milligrams to grams.
For Reference Standard and R&D, Not for Human Use Directly.
Inquire for bulk scale.
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
Catharantine (CAS number: 2468-21-5) is an important alkaloid isolated from Catharanthus roseus and belongs to the family of alkaloids in Catharanthus roseus. This type of alkaloid has attracted much attention due to its significant anti-cancer activity and multi-target pharmacological effects. Changchun alkaloids, as one of the active ingredients in Changchun flower alkaloids, have attracted extensive research in pharmacology and natural product drug development in recent years. It not only exhibits inhibitory effects on various tumor cells, especially in hematological malignancies such as leukemia, but also demonstrates the potential to regulate cardiovascular function due to its inhibitory effect on voltage dependent L-type calcium channels (VOCC).
This article aims to systematically review the chemical structure and physicochemical properties, plant sources and extraction methods, pharmacological activity and mechanism of action, pharmacological evaluation and pharmacokinetic characteristics of Changchun alkaloids, and explore their prospects and challenges in clinical applications, providing theoretical basis and reference for subsequent basic research and drug development.
The chemical name of Changchun alkaloids is (+) -3,4-Didehydrocoronaridine, with a molecular formula of C21H26N2O2 and a molecular weight of 336.43. Its structure belongs to the indole alkaloid class, with a complex polycyclic structure and multiple chiral centers. The LogP value of Changchun alkaloids is 3.1, indicating that they have moderate lipid solubility, which is beneficial for cell membrane penetration and in vivo distribution. Its topological polar surface area (TPSA) is 55.12 Å ², and the number of hydrogen bond acceptors is 4, indicating that it may form certain hydrogen bond interactions when binding with biomolecules.
The molecular structure of Changchun alkaloids contains indole rings and various functional groups, endowing them with rich chemical and biological reactivity. The stability and three-dimensional configuration of its structure are the basis for its biological activity. It is worth noting that vinblastine has a high blood-brain barrier permeability (BBB permeability is high), indicating its potential application in central nervous system diseases.
Changchun alkaloids mainly come from Catharanthus roseus, a perennial herbaceous plant in the Apocynaceae family, widely distributed in tropical and subtropical regions. Changchun flower contains various alkaloids, among which Changchun alkaloids are one of the important components, often coexisting with other Changchun flower alkaloids such as Vincristine and Vinblastine.
Traditional extraction methods often use organic solvent extraction combined with acid-base stepwise extraction. The general process includes:
In recent years, new technologies such as ultrasound assisted extraction and microwave-assisted extraction have been applied to improve the extraction efficiency and purity of Changchun alkaloids. In addition, the study of biosynthetic pathways also provides the possibility of increasing the yield of Changchun alkaloids through genetic engineering methods.
Changchun alkaloids, as an important component of Changchun flower alkaloids, exhibit significant anti-tumor activity. Research has shown that Changchun alkaloids can inhibit tumor cell proliferation, induce apoptosis, and block the tumor cell cycle through various mechanisms. Especially in leukemia cell lines, vinblastine exhibits strong cytotoxicity.
Its anti-cancer activity is closely related to regulating multiple signaling pathways, including key molecules such as AMPK, MCL1, BCL2, NOTCH1, STAT3, which affect cell metabolism, apoptosis, and proliferation. Changchun alkaloids can also affect targets such as TOP1 and SIRT1, regulate DNA repair and cellular stress response.
Changchun alkaloids have inhibitory effects on voltage driven L-type calcium channels (VOCC), with IC50 values of 220 μ M in cardiomyocytes and 8 μ M in vascular smooth muscle cells (VSMCs), demonstrating their high selectivity and sensitivity to calcium channels in vascular smooth muscle cells. By inhibiting VOCC, vinblastine reduces intracellular calcium ion concentration, leading to vasodilation and subsequently lowering blood pressure (BP) and heart rate (HR). This effect makes it potentially valuable in the treatment of hypertension and related cardiovascular diseases.
Current research shows that Changchun alkaloids also have certain effects on the central nervous system, possibly regulating neuronal excitability and neuroprotection through their high blood-brain barrier permeability. In addition, the anti-inflammatory, antioxidant and other auxiliary effects of Changchun alkaloids have gradually been paid attention to, but the relevant mechanisms still need to be further explored.
The pharmacological basis of Changchun alkaloids lies in their interactions with various molecular targets, and the specific mechanism is as follows:
Inhibition of L-type calcium channels (VOCC)
Changchun alkaloids bind to VOCC, block the influx of calcium ions into cells, reduce intracellular calcium concentration, regulate the contractile function of myocardium and vascular smooth muscle, and exert the effects of lowering blood pressure and slowing heart rate.
Regulating tumor related signaling pathways
NFE2L2（NRF2）Regulating cellular antioxidant response and affecting the oxidative stress state of tumor cells.
Other targets
The regulation of targets such as MAPT (microtubule associated protein Tau) and IDH1 (isocitrate dehydrogenase 1) may be involved in cytoskeleton reorganization and metabolic reprogramming, further affecting the survival and proliferation of tumor cells.
Through the synergistic effect of multiple targets and pathways, Changchun alkaloids exhibit a complex and effective anti-tumor mechanism.
The molecular weight of Changchun alkaloids is 336.43, which is within the ideal range for small molecule drugs. Its LogP value of 3.1 shows moderate lipid solubility, which is beneficial for cell membrane penetration and in vivo distribution. The TPSA is 55.12 Å ², which is lower than 140 Å ², indicating its good oral absorption potential. The number of hydrogen bond receptors is 4, which conforms to Lipinski's rule and is beneficial for the binding of drugs to targets.
Changchun alkaloids have high blood-brain barrier permeability, suggesting their potential use in the treatment of central nervous system diseases, but potential neurotoxic risks also need to be considered.
At present, there is no clear data on the hepatotoxicity, cardiotoxicity, and hERG channel inhibition of Changchun alkaloids, and further systematic evaluation is needed. The Ames test result is negative, indicating that it does not have significant induction of gene mutations and has ideal safety.
The pharmacokinetic studies of vinblastine in existing literature are relatively limited. Its high lipid solubility and blood-brain barrier permeability suggest that it is widely distributed in the body, and there may be rapid tissue distribution and metabolism. In the future, systematic in vivo absorption, distribution, metabolism, and excretion (ADME) research is needed to clarify its bioavailability, half-life, and metabolic pathways, providing a basis for clinical dosage form design.
Changchun alkaloid, as an important active ingredient of Changchun flower alkaloids, has multi-target anticancer activity, especially with potential therapeutic value for hematological malignancies such as leukemia. Its inhibitory effect on VOCC also demonstrates potential applications in the field of cardiovascular diseases, such as adjuvant therapy for hypertension and arrhythmia.
However, the clinical application of Changchun alkaloids is still in its early stages and faces the following challenges:
Balance between efficacy and safety
Further clarification is needed on the effective dosage range and toxic side effects, especially in the systematic evaluation of cardiac and hepatic toxicity.
Pharmacokinetic optimization
Improve its in vivo stability and targeting through structural modification or drug carrier technology, and enhance its bioavailability.
Combination therapy strategy
Explore the combination application with other anti-cancer drugs or cardiovascular drugs to achieve synergistic effects.
Preclinical and clinical research
Strengthen animal model and clinical trial research, verify its efficacy and safety, and promote its translation into clinical drugs.
In the future, with the development of molecular biology and medicinal chemistry technology, the mechanism of action of Changchun alkaloids will be further elucidated, and its structural optimization and dosage form innovation will also promote its clinical application.
Changchun alkaloid, as a natural alkaloid derived from Changchun flower, has shown broad application prospects in anti-cancer and cardiovascular disease treatment due to its unique chemical structure and multi-target pharmacological activity. It exerts multiple biological effects by inhibiting L-type calcium channels and regulating multiple tumor related signaling pathways. Although there are still certain challenges in drug development and clinical application, with the deepening of research, vinblastine is expected to become an important candidate molecule for new anti-cancer and cardiovascular drugs. Future research should focus on its safety evaluation, pharmacokinetic optimization, and clinical validation, promoting its transition from laboratory to clinical use and benefiting patients.
