Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
Jolkinolide B (CAS number: 37905-08-1) is a natural diterpenoid derived from Euphorbia fischeriana. As a natural compound with significant biological activity, Euphorbiaceae B has received widespread attention in recent years due to its excellent anti-tumor activity. Multiple studies have shown that this compound can induce cancer cell apoptosis through various molecular mechanisms, inhibit tumor cell proliferation and migration, and demonstrate good pharmacological potential. This article will provide a systematic review of the chemical structure and physicochemical properties, plant sources and extraction methods, pharmacological activity and mechanism of action, pharmacological evaluation, pharmacokinetic characteristics, and clinical application prospects of Euphorbiaceae B, aiming to provide theoretical basis and reference for the in-depth research and drug development of this natural product.
Rock Euphorbia B belongs to the class of diterpenoid lactones, with a molecular formula of C20H26O5 and a molecular weight of 330.4240. Its structural feature is a typical diterpene skeleton, containing lactone rings and multiple oxygen functional groups, endowing it with unique biological activity. According to calculations, its LogP value is 4.1364, indicating that it has good lipid solubility, which is beneficial for cell membrane penetration. The polar surface area (TPSA) is 51.3600, indicating moderate molecular polarity that may affect its bioavailability and targeting. The low water solubility (0.0084 mg/mL) to some extent limits the development of its pharmaceutical formulations, but the high fat solubility is beneficial for oral absorption and blood-brain barrier penetration. Relevant studies have shown that it has a high blood-brain barrier penetration ability. In addition, Euphorbiaceae B did not exhibit hERG channel inhibition, indicating a low risk of cardiac toxicity; The Ames test result is 0.9, indicating that its genotoxicity risk is relatively low and has a good safety basis.
Rock Euphorbia fischeriana Steud B is mainly extracted from the roots of Euphorbia fischeriana Steud. Euphorbia fischeriana is a plant of Euphorbiaceae, which is widely distributed in Northeast China and the Korean Peninsula. It has always been used as a traditional Chinese medicine to treat tumors, inflammation and infectious diseases. The traditional methods for extracting Euphorbiaceae B include ethanol or methanol extraction, followed by liquid-liquid partitioning, column chromatography (such as silica gel column, reverse phase C18 column), and purification by high performance liquid chromatography (HPLC) to obtain high-purity target compounds. In recent years, the application of ultrasound assisted extraction and microwave-assisted extraction technologies has improved extraction efficiency and purity, reduced solvent usage and extraction time. In addition, researchers have also developed selective adsorption materials based on molecular imprinting technology for efficient separation and purification of Euphorbiaceae B, targeting its structural characteristics.
The anti-tumor effect of Euphorbia officinalis lactone B is its most significant biological activity, covering a variety of cancer types, including but not limited to breast cancer, lung cancer, liver cancer, colorectal cancer and leukemia. In vitro cell experiments have shown that Euphorbiaceae B can significantly inhibit the proliferation of tumor cells, induce cell cycle arrest and apoptosis. Its IC50 value is usually in the micromolar range, indicating strong cytotoxicity. Animal model studies have further confirmed its anti-tumor effect, and Euphorbiaceae B can effectively inhibit tumor growth, prolong the survival of experimental animals, and have minimal toxic side effects.
Rock Euphorbia B induces programmed cell death in cancer cells by activating endogenous and exogenous apoptotic pathways. Its mechanism of action involves loss of mitochondrial membrane potential, activation of the caspase family (such as caspase-3, caspase-9), and regulation of BCL-2 family protein expression. In addition, rock Euphorbia lactone B can promote the generation of intracellular ROS (reactive oxygen species), induce oxidative stress, and further promote the transmission of apoptosis signals.
Iwata Euphorbia B has inhibitory effects on the migration and invasion of tumor cells. It inhibits tumor cell matrix degradation and infiltration by downregulating the expression of matrix metalloproteinase MMP2. At the same time, Euphorbiaceae B can inhibit tumor associated angiogenesis, partially by regulating the HIF1A (hypoxia inducible factor 1 alpha) signaling pathway, blocking neovascularization in the tumor microenvironment, and limiting tumor nutrient supply.
The anti-tumor effect of Euphorbiaceae B involves multiple key molecular targets and signaling pathways, reflecting its pharmacological characteristics of multi-target and multi mechanism.
The above multi-target mechanism of action demonstrates the broad adaptability and potential synergistic effect of Euphorbiaceae B in anti-tumor therapy.
The pharmacological evaluation of Euphorbiaceae B shows that it has certain advantages and challenges. Its high lipid solubility (LogP=4.1364) facilitates cell membrane penetration and oral absorption, but its low water solubility (0.0084 mg/mL) limits its bioavailability and formulation development. Its polar surface area is moderate (TPSA=51.3600), which helps to penetrate the blood-brain barrier. Relevant experiments support its potential application in central nervous system diseases.
In terms of safety, Euphorbia lactiflora B did not exhibit significant hERG channel inhibition, reducing the risk of cardiac toxicity. The Ames test result is 0.9, indicating low genotoxicity and good safety. Pharmacokinetic studies have shown that berberine B has good distribution characteristics in vivo and can effectively enter tumor tissues. Its metabolic pathway mainly involves the liver enzyme system, and the metabolites need further identification and evaluation.
At present, the oral bioavailability and in vivo half-life of Euphorbia lactiflora B still need to be optimized, and the development of new drug delivery systems such as nanocarriers and liposomes provides the possibility for its clinical translation.
As a natural product with multi-target anti-tumor activity, Euphorbianolactone B has great clinical application potential. Its multiple mechanisms of inducing cancer cell apoptosis, inhibiting tumor metastasis, and angiogenesis provide new ideas for comprehensive cancer treatment. Especially in the treatment of drug-resistant tumors and multi drug combination therapy, Euphorbia lactiflora B is expected to exert a synergistic effect.
Future research should focus on the following aspects:
In summary, as a multifunctional natural product, Euphorbiaceae B has the potential to become a new type of anti-tumor drug and deserves further in-depth research and development.
As an important diterpenoid active ingredient in Euphorbia lanceolata, Euphorbiaceae B has become a hot topic in natural product pharmacology research due to its unique chemical structure and significant anti-tumor activity. It regulates the growth, apoptosis, and metastasis of tumor cells through multiple targets and pathways, demonstrating good pharmacological effects and safety foundation. Although there are certain limitations in its water solubility and pharmacokinetic characteristics, with the help of modern drug design and formulation technology, it is expected to achieve clinical translation. In the future, with the deepening of mechanism research and the advancement of clinical evaluation, Euphorbiaceae B is expected to become an important drug in the field of anti-tumor therapy, bringing new treatment options for cancer patients.
