Product name: Tubeimoside I
Synonym name: Lobatoside H
Catalogue No.: BP1415
Cas No.: 102040-03-9
Formula: C₆₃H₉₈O₂₉
Mol Weight: 1319.45
Botanical Source: Bolbostemma paniculatum（Maxim.）Franquet
Physical Description:
Type of Compound: Triterpenoids

Purity: 95%~99%
Analysis Method: HPLC-DAD or/and HPLC-ELSD
Identification Method: Mass, NMR
Packing: Brown vial or HDPE plastic bottle

Storage: Store in a well closed container, protected from air and light. Put into refrigerate or freeze for long term storage.
Whenever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20℃. Generally, these will be useable for up to two weeks.

The product could be supplied from milligrams to grams
Inquire for bulk scale.




Chengdu Biopurify Phytochemicals Ltd. is a leading company in the research, development, manufacture and marketing of High Quality Phytochemicals and Extracts(especially Active Ingredients from Traditional Chinese Medicine，TCM), Natural Active Pharmaceutical Ingredients worldwide.
The main services:
A. Supply active ingredients and reference standards of TCM, from mgs to kgs scale
B. Custom extraction and purification, target Herb Active Ingredients
C. Custom synthesis and semi-synthesis for Natural Active Ingredients
D. CR(contract research), CM(contract manufacture) and PD(process development) services from lab scale, pilot scale to commercial scale(GMP is also available)
E. TCM compounds library for drug screen,more than 3000 compounds available, many of them are rare and unique.

HPLC of Tubeimoside I

HNMR of Tubeimoside I

Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃

Introduction/Overview

Tubeimoside I (CAS number: 102040-03-9) is a type of saponin derived from the Chinese medicinal herb Tubeimoside（Bolbostemma paniculatum）Natural triterpenoid saponins. As a natural product with significant biological activity, saponin A from Fritillaria thunbergii has attracted much attention in pharmacological research in recent years, especially in its potential therapeutic value in various disease models such as anti-inflammatory, anti-tumor, and sepsis. Its unique molecular structure endows it with multi-target regulatory ability, which can induce cellular autophagy, inhibit the production of pro-inflammatory cytokines, and promote angiogenesis by inhibiting heat shock protein 60 (HSPD1), regulating nuclear factor kappa B (NF - κ B) and mitogen activated protein kinase (MAPK) signaling pathways, thereby exerting cell protection and disease relief effects.

This review aims to systematically summarize the chemical structure and physicochemical properties, plant sources, and extraction methods of saponin A from Fritillaria thunbergii, comprehensively evaluate its pharmacological activity and mechanism of action, explore its pharmacological properties and pharmacokinetic characteristics, and look forward to its potential and development direction in clinical applications. By integrating the research progress in recent years, it is expected to provide theoretical basis and reference for the further drug development and clinical translation of saponins A from Fritillaria thunbergii.

Chemical structure and physicochemical properties

Tu Bei Mu saponin A belongs to the triterpenoid saponin class, with a molecular weight of 1319.4480 and a complex molecular formula, containing multiple glycosylated triterpenoid skeletons. Its structural features include a typical pentacyclic triterpenoid core that connects multiple sugar chains, endowing it with high polarity and water solubility. The specific physicochemical properties are as follows:

• molecular weight：1319.4480 Da
• LogP value 1.3718, indicating moderate lipid solubility, facilitating cell membrane penetration
• Topological Polar Surface Area (TPSA)445.19 Å ² indicates high polarity, which may affect oral absorption and bioavailability
• Water solubility：0.1932 mg/mL， Belonging to low solubility compounds
• Blood-brain barrier permeability Low, indicating limited distribution in the central nervous system
• HERG channel inhibition No inhibitory effect, reducing the risk of cardiac toxicity
• Ames mutagenicity test Negative, indicating no significant genetic toxicity risk

The structure of saponin A in Fritillaria thunbergii is complex and highly polar, and the presence of sugar groups significantly affects its pharmacokinetic properties and biological activity. Its moderate lipophilicity and high polarity enable it to exhibit tissue selectivity in its distribution within the body, particularly in the inflammatory and tumor microenvironment, demonstrating good targeting properties.

Plant sources and extraction methods

The main source of saponin A in Platycodon grandiflorus comes from the Cucurbitaceae plant Platycodon grandiflorus（Bolbostemma paniculatum）This plant is widely used in traditional Chinese medicine to treat tumors, inflammation, and abscesses. As one of its main active ingredients, saponin A from Fritillaria thunbergii has significant pharmacological effects.

Plant-based

Tu Beimu is a perennial herbaceous plant mainly distributed in southern China and Southeast Asia. Both its root and aboveground parts contain abundant triterpenoid saponins. The content of saponin A in Fritillaria thunbergii varies at different growth stages and harvesting sites, usually extracted mainly from dried tubers.

Extraction and Separation Methods

The extraction of saponin A from Fritillaria thunbergii is usually carried out using the following steps:

1. Crude extraction After crushing the dried root tubers of Fritillaria thunbergii, ethanol or methanol is used for reflux extraction, and the extract is concentrated to obtain the crude extract.
2. Separation and purification The crude extract is subjected to liquid-liquid distribution (such as ethyl acetate water system) to remove lipophilic impurities; Subsequently, multi-stage column chromatography (silica gel, reverse phase C18, gel permeation chromatography, etc.) was used for separation and purification.
3. appraisal The purified saponin A of Fritillaria thunbergii was structurally confirmed by high performance liquid chromatography (HPLC), mass spectrometry (MS), and nuclear magnetic resonance (NMR) techniques.

In recent years, the application of new technologies such as ultrasound assisted extraction and microwave-assisted extraction has improved extraction efficiency and purity, providing technical support for large-scale preparation.

Pharmacological activity research

Tu Bei Mu saponin A exhibits a wide range of pharmacological activities in various disease models, mainly including anti-inflammatory, anti-tumor, anti sepsis, and promotion of angiogenesis.

anti-inflammatory activity

Tu Bei Mu saponin A effectively reduces inflammation by inhibiting the production of pro-inflammatory cytokines such as IL-6 and IL-1 β. Its mechanism of action involves inhibiting the activation of NF - κ B and MAPK signaling pathways, and reducing the expression of inflammatory mediators. In addition, saponin A of Fritillaria thunbergii can regulate the eNOS VEGF axis, promote endothelial function repair, and further alleviate tissue damage caused by inflammation.

Antitumor activity

Tu Bei Mu saponin A exhibits significant inhibitory effects on various cancer cell lines, especially in solid tumor models such as cervical cancer, lung cancer, and liver cancer. Its anti-tumor mechanism mainly includes:

• Inducing cell apoptosis: By regulating key regulatory factors such as BCL2 family proteins (BCL2, BAX), TP53, and CDKN1A, the intracellular apoptotic pathway is activated.
• Inhibiting cell proliferation: affecting signaling molecules such as EGFR, TOP1, and RB1, and blocking cell cycle progression.
• Anti metastasis and invasion: By inhibiting the NF - κ B signaling pathway, it reduces the migration and invasion ability of tumor cells.
• Induced autophagy: Activation of cell protective autophagy through Akt mediated signaling pathway enhances cell sensitivity to chemotherapy drugs.

Anti sepsis and ischemic diseases

In the sepsis model, saponins A from Fritillaria thunbergii significantly alleviate sepsis symptoms by regulating immune response, inhibiting excessive inflammatory response, improving angiogenesis and microcirculation function. It promotes the activation of the eNOS VEGF signaling pathway, which helps to restore blood flow supply to ischemic tissues and alleviate ischemic injury.

Mechanism of action and molecular targets

The multi-target mechanism of action of saponin A from Fritillaria thunbergii is the basis for its broad pharmacological activity. Current research indicates that its main targets and mechanisms of action include:

HSPD1 inhibition

Heat shock protein 60 (HSPD1), as an important molecular chaperone in cells, participates in protein folding and cellular stress response. As an orally active HSPD1 inhibitor, Tu Bei Mu saponin A can intervene in cellular stress response, regulate cell fate, and play a key role in tumor cells and inflammatory cells.

Regulation of NF - κ B and MAPK signaling pathway

NF - κ B and MAPK are important signaling pathways that regulate inflammatory response and cell survival. Tu Bei Mu saponin A inhibits the activation of these pathways, reduces the expression of pro-inflammatory cytokines, alleviates inflammatory responses, and suppresses the proliferation and metastasis of tumor cells.

ENOS VEGF axis regulation

Tu Bei Mu saponin A can activate endothelial nitric oxide synthase (eNOS), promote the production of nitric oxide (NO), regulate the expression of vascular endothelial growth factor (VEGF), promote angiogenesis, and repair ischemic tissues.

Akt mediated autophagy induction

By activating the Akt signaling pathway, saponin A from Fritillaria thunbergii induces protective autophagy in cells, enhancing their resistance to external stimuli, especially in tumor cells, which helps regulate the balance between cell survival and death.

Other molecular targets

In tumors such as cervical cancer, tubeimu saponin A acts on multiple key molecular targets, including BCL2, TOP1, EGFR, TP53, CDKN2A, RB1, BAX, CDKN1A, and HPVE6, regulating multiple processes such as cell cycle, apoptosis, and DNA repair, exerting a comprehensive anti-tumor effect.

Evaluation of drug properties and pharmacokinetics

The pharmacological evaluation of saponins A from Fritillaria thunbergii shows that it has certain advantages and challenges:

Pharmaceutical advantages

• Low hERG inhibitory effect Reducing the risk of cardiac toxicity is beneficial for safety evaluation.
• Ames test negative No genetic toxicity risk, meets safety requirements.
• Moderate LogP value Beneficial for cell membrane penetration and in vivo distribution.
• Oral activity Has potential for oral drug development.

Drug Challenge

• High molecular weight：1319.4480 Da， Exceeding the ideal molecular weight range in traditional "drug similarity rules" may affect oral absorption and bioavailability.
• High TPSA value 445.19 Å ² indicates strong polarity and may limit the ability to pass through the cell membrane.
• Low water solubility：0.1932 mg/mL， Optimization of solubility is required in formulation development.
• Low permeability of blood-brain barrier Limit its application in central nervous system diseases.

pharmacokinetics

At present, there is limited research on the pharmacokinetics of saponin A in Fritillaria thunbergii. Previous studies have shown that it can reach effective concentrations in the blood after oral administration, and is mainly metabolized by the liver and excreted by the kidneys. Its metabolic pathway may involve glycoside hydrolysis and oxidation reactions. In the future, it is necessary to strengthen systematic research on its absorption, distribution, metabolism, and excretion (ADME) characteristics to guide clinical dosage form design and optimize dosing regimens.

Clinical application prospects and prospects

Tu Bei Mu saponin A, with its multi-target and multi mechanism pharmacological properties, has shown broad application prospects in fields such as inflammatory diseases, tumors, sepsis, and ischemic diseases.

Inflammatory diseases

By inhibiting the NF - κ B and MAPK pathways and reducing the production of pro-inflammatory factors, saponin A of Fritillaria thunbergii is expected to become a novel anti-inflammatory drug, particularly suitable for the treatment of chronic inflammation and autoimmune diseases.

tumor therapy

Regarding cervical cancer and other solid tumors, saponins from Fritillaria thunbergii exhibit potential anti-tumor activity by regulating cell apoptosis, autophagy, and cell cycle. In the future, it can be combined with existing chemotherapy drugs to enhance efficacy and reduce drug resistance.

Sepsis and ischemic diseases

Promote angiogenesis and improve microcirculation function, giving Tu Bei Mu saponin A unique advantages in the treatment of sepsis and ischemic injury, especially with potential value in acute phase management.

Future research directions

• Pharmacokinetic and Toxicological Systematic Review Clarify the safe dosage range and long-term medication risks.
• Formulation optimization Improve water solubility and bioavailability, and develop oral sustained-release or targeted formulations.
• clinical trial Conduct early clinical studies to verify its safety and efficacy.
• Structural modification and derivative development Improve drug properties, enhance targeting and activity through chemical modification.

Conclusion

As a natural triterpenoid saponin derived from traditional Chinese medicine, Tu Bei Mu saponin A has shown great research and application value in anti-inflammatory, anti-tumor, and sepsis fields due to its unique chemical structure and multi-target pharmacological effects. Although its large molecular weight and high polarity pose certain challenges for drug development, its good safety and diverse mechanisms of action provide a solid foundation for new drug development. In the future, through in-depth pharmacological mechanism research, pharmacokinetic optimization, and clinical validation, saponins from Fritillaria thunbergii are expected to become important candidate drugs for the treatment of various diseases, promoting the development and clinical translation of natural product pharmacology.