Synonym name: Neoline
Catalogue No.: BP0292
Cas No.: 466-26-2
Formula: C24H39NO6
Mol Weight: 437.577
Botanical Source: Alkaloid from Aconitum bullatifolium var. homotrichum, Aconitum napellus, Aconitum nagarum, Aconitum sczukini, Aconitum soongoricum, Aconitum sachalinense var. compactum, Aconitum carmichaeli, Aconitum karakolicum, Aconitum teipeicum and Aconitum ibukien
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.
HPLC of Bullatine B
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
Bullatine B, as an important natural diterpenoid alkaloid, is mainly isolated from Aconitum spp. plants. Aconitum plants are widely used in traditional Chinese medicine, especially known for their significant analgesic, anti-inflammatory, and anti-tumor activities. As a derivative of aconitine alkaloids, Artemisia scoparia B has received widespread attention in the fields of pharmacology and natural product chemistry in recent years due to its unique molecular structure and multi-target pharmacological activity. This article provides a systematic review of the chemical structure and physicochemical properties, plant sources and extraction methods, pharmacological activity and mechanism of action, pharmacological evaluation and pharmacokinetic characteristics of Artemisia scoparia B, and prospects for its clinical application prospects, in order to provide theoretical basis and reference for subsequent research and drug development.
Bullatine B (CAS number: 466-26-2) has a molecular formula of C24H39NO6 and a molecular weight of 421.57 Da. Its structure belongs to diterpenoid alkaloids, specifically hydrogenated derivatives of aconitine diterpenoid alkaloids, containing various functional groups such as tertiary alcohols, triols, and secondary alcohols, and has a bridging structure and organic heterocyclic skeleton. The molecule contains multiple hydroxyl and amino groups, endowing it with high polarity and diverse chemical reactivity.
In terms of physical and chemical properties, the LogP value of Artemisia scoparia B is about 1.8, indicating that it has moderate lipid solubility, which is beneficial for cell membrane permeability but not excessively hydrophobic. Its topological polar surface area (TPSA) is 98.96 Å ², and the number of hydrogen bond acceptors is 6, indicating its strong hydrogen bonding ability when binding with biomolecules. The low permeability of the blood-brain barrier suggests limited distribution in the central nervous system. There is currently a lack of systematic data on safety indicators such as hepatotoxicity, cardiotoxicity, hERG channel inhibition, and mutagenicity (Ames test), and further research is urgently needed.
Artemisia selengenin is mainly found in plants of the Aconitum genus, with typical representatives including Aconitum carmichaelii and Aconitum kusnezoffi. These plants are widely distributed in East Asia such as China, Japan, and South Korea, and have always been used as traditional Chinese medicine for the treatment of rheumatism, cardiovascular diseases, and tumors.
The extraction method usually adopts organic solvent extraction combined with separation and purification technology. Traditional processes often use ethanol or methanol aqueous solutions for reflux extraction of dried plant rhizomes, followed by enrichment of alkaloids through acid-base regulation. The purification steps include liquid-liquid extraction, column chromatography (such as silica gel column, C18 reverse phase column), and high-performance liquid chromatography (HPLC) separation, ultimately obtaining high-purity artemisinin from Artemisia scoparia. In recent years, new technologies such as ultrasound assisted extraction and microwave-assisted extraction have also been applied to improve extraction efficiency and purity.
The pharmacological activity research of Artemisia scoparia B mainly focuses on its anti-tumor effect. A large number of in vitro cell experiments and some in vivo model studies have shown that Artemisia scoparia B can significantly inhibit the proliferation of various tumor cells, induce cell apoptosis, and inhibit tumor metastasis. Its anti-tumor spectrum covers breast cancer, lung cancer, liver cancer and other solid tumor types.
In addition, Artemisia scoparia B also exhibits certain anti-inflammatory and immune regulatory effects, which may exert auxiliary anti-tumor effects by regulating inflammatory factors and immune cell functions. Some studies have also found that it has an inhibitory effect on angiogenesis in the tumor microenvironment, further blocking the tumor's nutritional supply.
The anti-tumor mechanism of Artemisia scoparia B involves multiple signaling pathways and key molecular targets, reflecting its pharmacological characteristics of multi-target and multi mechanism. The main targets include:
MCL1 and BCL2 As anti apoptotic proteins, MCL1 and BCL2 play a crucial role in tumor cell survival. Xueshang Yizhihao Yi Su promotes apoptosis signaling in tumor cells by downregulating the expression of these proteins.
STAT3 Signal transducer and activator of transcription factor 3 (STAT3) is an important regulatory factor for tumor cell proliferation and immune escape. Xueshang Yizhihao Yi Su can inhibit the phosphorylation and activation of STAT3, and block the expression of downstream tumor promoting genes.
MMP2 Matrix metalloproteinase-2 (MMP2) is involved in the invasion and metastasis of tumor cells. Xueshang Yizhihao Yi Su reduces the migration ability of tumor cells by inhibiting MMP2 activity.
TOP1 and TOP2A DNA topoisomerases I and II α are important enzymes involved in cellular DNA replication and transcription. Artemisia argyi on the snow may interfere with the function of these enzymes and block the DNA metabolism process of tumor cells.
HIF1A Hypoxia inducible factor 1 alpha regulates the adaptation of tumor cells to hypoxic environments and promotes angiogenesis. Artemisia argyi on snow inhibits the expression of HIF1A and suppresses tumor angiogenesis.
MAPK1 Mitogen activated protein kinase 1 is involved in cell proliferation and differentiation signaling. Its inhibition helps to block the proliferation signal of tumor cells.
ESR1 and CYP19A1 Estrogen receptor alpha (ESR1) and aromatase (CYP19A1) play an important role in hormone dependent tumors such as breast cancer. Xueshang Yizhihao Yi Su may have potential therapeutic value for hormone related tumors by regulating these targets.
In summary, Xueshang Yizhihao Yi Su exhibits excellent anti-tumor potential by regulating key processes such as tumor cell proliferation, apoptosis, invasion, and angiogenesis through multi-target synergistic effects.
From the perspective of medicinal properties, the molecular weight (421.57 Da) and LogP (1.8) of Artemisia scoparia B meet the "drug similarity" criteria in drug design, indicating its good membrane permeability and potential for in vivo distribution. Its TPSA (98.96 Å ²) and hydrogen bond acceptor number (6) indicate moderate molecular polarity, which is conducive to stable binding with target proteins.
The low permeability of the blood-brain barrier may limit its application in the central nervous system, but it has no significant adverse effects on the treatment of most peripheral tumors. The existing data has not yet clarified its liver metabolic pathways and metabolites, and safety indicators such as liver toxicity, cardiac toxicity, and hERG channel inhibition lack systematic evaluation. Systematic pharmacokinetic (PK) and toxicological studies are needed.
Preliminary pharmacokinetic studies in vivo have shown that Artemisia scoparia B has a moderate half-life in plasma after oral and injection administration, and its bioavailability needs further optimization. Its metabolism may involve the liver cytochrome P450 enzyme system, and in the future, it is necessary to combine in vivo and in vitro metabolic enzyme research to clarify its metabolic pathway and potential drug interaction risks.
As a natural diterpenoid alkaloid, Artemisia scoparia B has good clinical translational potential due to its multi-target anti-tumor activity. Its anti-tumor mechanism is diverse, which can induce tumor cell apoptosis, inhibit tumor invasion and angiogenesis, and is suitable for development as an active ingredient in multi mechanism anticancer drugs or combination therapy regimens.
Future research should focus on the following aspects:
Pharmacokinetic and toxicological evaluation of the system Clarify its metabolic pathways, half-life, distribution characteristics, and safety in vivo, providing scientific basis for clinical trials.
Structural modification and drug design Based on the core skeleton of Artemisia scoparia B, structural optimization is carried out to enhance its bioavailability and targeting, and reduce potential toxic side effects.
In depth study of mechanisms Using multi omics techniques and molecular biology methods to further reveal its mechanism of action and synergistic effects with other drugs.
Preclinical and clinical trials Carry out systematic efficacy and safety evaluation of animal models, gradually advance to the clinical trial stage, and verify their therapeutic effects and tolerability.
Multi target combination therapy strategy Combining modern precision medicine concepts, explore the combined application of Artemisia scoparia B with targeted drugs and immunotherapy drugs to enhance anti-tumor efficacy.
As an important diterpenoid alkaloid in Aconitum plants, Artemisia scoparia B has shown broad prospects for drug development due to its unique chemical structure and multi-target anti-tumor activity. Although its pharmacokinetics and safety research are not yet sufficient, with the continuous advancement of modern pharmacology and molecular biology techniques, Artemisia scoparia is expected to become an important candidate molecule for new anti-tumor drugs. In the future, through systematic pharmacological mechanism research, structural optimization, and clinical evaluation, Artemisia scoparia B is expected to bring new breakthroughs and contributions to the field of cancer treatment.
