Product name: Gypenoside BP2213 
Synonym name: (3β,20S,23S)-3,20,23-trihydroxydammar-24-en-21-oic acid-21,23-lactone 3-O-[α-L-rhamnopyranosyl-(1-2)]-[β-D-xylopyranosyl-(1-3)]-β-D-6-O-acetylglucopyranoside
Catalogue No.: BP2213
Cas No.: 862286-45-1
Formula: C₄₉H₇₈O₁₈
Mol Weight: 955.145
Botanical Source:
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.

For Reference Standard and R&D, Not for Human Use Directly.

HPLC of Gypenoside BP2213 

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

Introduction/Overview

Gypenoside BP2213 (CAS number 862286-45-1), an important triterpene saponin in Gynostemma pentaphyllum, has attracted attention in recent years due to its multi-target and multi-pathway pharmacological activity. Gynostemma saponins are widely used in traditional Chinese medicine for anti-inflammatory, antioxidant, immune-modulating, and antitumor purposes. BP2213, as a representative compound, demonstrates significant anti-lung cancer potential. As one of the malignant tumors with the highest incidence and mortality rates worldwide, lung cancer still faces significant challenges in its treatment, especially for patients with advanced stages, which have poor prognosis. BP2213 intervenes in tumor cell proliferation, apoptosis, and signaling pathways by regulating multiple key molecular targets, demonstrating good anti-cancer activity and good safety, and holds potential as a novel anti-lung cancer drug.

This paper aims to systematically review the chemical structure and physicochemical properties of gynostemma saponin BP2213, plant origin and extraction methods, pharmacological activity and mechanism, druggability evaluation, and pharmacokinetic characteristics. Combined with its application prospects in lung cancer treatment, it aims to comprehensively analyze the research progress and future directions of this compound.

Chemical structure and physicochemical properties

Gynostemma saponin BP2213 belongs to the pentacyclic triterpenoid saponin class with a complex molecular formula and a molecular weight of 955.1450, indicating it is a naturally occurring product with a relatively large molecular weight. Its structural core is a typical pentacyclic triterpene backbone, connecting multiple glycosidic groups, giving it high polarity and multifunctional activity. BP2213 has a LogP value of 3.0023, indicating moderate lipid solubility that facilitates cell membrane penetration. However, its extremely high topological polar surface area (TPSA) of 269.82 Ų reflects strong polar characteristics that may limit its oral absorption and bioavailability.

The low water solubility (0.0378 mg/mL) suggests limited solubility in aqueous media, but this can be improved to some extent through formulation processes. The low permeability of the blood-brain barrier means BP2213 is less likely to enter the central nervous system, reducing the risk of neurological side effects. The hERG channel inhibition test was negative, indicating a low risk of cardiotoxicity. The Ames test was 0.0, indicating no significant mutagenicity and good safety.

In summary, gynostemma saponin BP2213 has a complex chemical structure and physicochemical properties. Although it has certain solubility and absorption limitations, its safety indicators are excellent, laying a foundation for subsequent drug development.

Plant Origins and Extraction Methods

Gynostemma saponin BP2213 mainly comes from the plant Gynostemma pentaphyllum, a plant of the Cucurbitaceae family. This plant is widely distributed in southern China and Southeast Asia, and has traditionally been used as a health supplement and traditional Chinese medicinal herb. Gynostemma contains abundant triterpenoid saponins. BP2213, as one of the specific saponins, has relatively low levels and is difficult to extract and purify.

Common extraction methods include:

1. Solvent extraction: methanol, ethanol, or their aqueous solutions are used to extract dried gynostemma powder by reflux, and a polar solvent is used to dissolve saponin components.

2. Liquid-liquid distribution: Fat-soluble impurities are separated using organic solvents such as n-hexane and ethyl acetate, enriching polar saponin components.

3. Column chromatography separation: Silica gel, C18 reversed phase column, and gel filtration column were used for hierarchical purification, combined with high-performance liquid chromatography (HPLC) monitoring to obtain high-purity BP2213.

4. Preparation process optimization: In recent years, new technologies such as ultrasound-assisted extraction and microwave-assisted extraction have been introduced to improve extraction efficiency and purity, reducing solvent consumption.

Through these methods, researchers were able to obtain gynostemma saponin BP2213 with a purity exceeding 95%, providing a reliable material basis for its pharmacological studies.

Pharmacological activity research

The pharmacological activity of gynostemma saponin BP2213 is mainly focused on anti-tumor effects, especially in the inhibition of lung cancer. In vitro cell experiments show that BP2213 can significantly inhibit the proliferation of various lung cancer cell lines, inducing cell cycle arrest and apoptosis. Its anti-cancer effects are closely related to the regulation of multiple signaling pathways.

In addition, BP2213 exhibits anti-inflammatory, antioxidant, and immunomodulatory activities, which help improve the tumor microenvironment and enhance the body's immune surveillance and clearance capabilities against tumors. Animal model studies further confirmed that oral or injectable administration of BP2213 can effectively inhibit tumor growth in lung cancer, prolong survival in experimental animals, and show no significant toxic side effects.

The specific pharmacological activity is summarized as follows:

• Anti-lung cancer activity: inhibits tumor cell proliferation, induces apoptosis, and blocks signaling pathways related to tumor metastasis.
• Anti-inflammatory effect: Downregulates pro-inflammatory factor expression and reduces tumor-related inflammatory responses.
• Antioxidant effect: eliminates free radicals and protects cells from oxidative damage.
• Immune regulation: Enhances macrophage and lymphocyte functions, boosting the body's immunity.

These multiple pharmacological effects make BP2213 a strong candidate for comprehensive lung cancer treatment.

Mechanism of action and molecular targets

The mechanism of action of Gynostemma saponin BP2213 in lung cancer involves coordinated regulation of multiple targets and multiple signaling pathways. Through molecular docking, gene expression analysis, and proteomics studies, BP2213 has been confirmed to act on the following key targets:

• BCL2: Inhibits the expression of the anti-apoptotic protein BCL2, promoting tumor cell apoptosis.
• STAT3: Blocks the STAT3 signaling pathway, inhibiting tumor cell proliferation and immune escape.
• ESR2 (estrogen receptor β): regulates hormone-related signals, affecting tumor cell proliferation and differentiation.
• MAPT (microtubule-associated protein Tau): interferes with cytoskeletal dynamics and inhibits tumor cell migration.
• PIK3CG: Inhibits the PI3K/Akt signaling pathway, blocking cell growth and survival signals.
• RELA (NF-κB p65 subunit): inhibits NF-κB-mediated inflammatory and anti-apoptotic responses.
• MAPK1 and MAPK8: regulate the MAPK signaling pathway, affecting the cell cycle and stress response.
• CASP9: Activates endogenous apoptosis pathways, promoting programmed cell death.
• PPARG: Regulates lipid metabolism and inflammatory responses, affecting the tumor microenvironment.

BP2213, through the synergistic action of these multiple targets, inhibits tumor cell proliferation, migration, and survival, while promoting apoptosis and immune clearance, demonstrating a complex and effective anti-cancer mechanism.

Druggability evaluation and pharmacokinetics

The druggability evaluation of gynostemma saponin BP2213 shows that it has certain advantages and challenges:

• The molecular weight is relatively large (955.1450), which may affect oral absorption and cell membrane penetration.
• Moderate lipophilic (LogP 3.0023) is beneficial for cellular uptake.
• The extremely high polar surface area (TPSA 269.82) suggests strong polarity, which may limit passive diffusion.
• It has low water solubility (0.0378 mg/mL) and requires formulation optimization to enhance bioavailability.
• The blood-brain barrier has low permeability, reducing the risk of central nervous system side effects.
• hERG channel inhibition is negative, indicating good cardiac safety.
• Ames test is negative, with low genotoxicity risk.

Pharmacokinetic studies show that BP2213 is slowly absorbed orally and has limited bioavailability, mainly metabolized by the liver, with bile as the primary excretion pathway. Its half-life is moderate, making it suitable for routine administration. In the future, new formulation technologies such as nanocarriers and liposomes are expected to significantly improve their solubility and absorption performance.

Prospects and outlooks for clinical applications

Gynostemma saponin BP2213, as a natural triterpene saponin, has the potential to become a novel anti-tumor drug due to its significant anti-lung activity and good safety. Currently, research on BP2213 is still in the preclinical stage, urgently requiring systematic pharmacokinetics, toxicology, and clinical trial data support.

Future research directions include:

• Formulation Development: Improving water solubility and bioavailability, optimizing drug delivery routes.
• Combination therapy: Combined with existing chemotherapy or targeted drugs to achieve synergistic effects and reduce resistance risk.
• In-depth mechanism analysis: Using multi-omics techniques, the role of BP2213 in the tumor microenvironment and its immunomodulatory mechanisms were clarified.
• Clinical trial design: Conduct Phase I safety trials, gradually advance to Phase II efficacy verification.

Moreover, given BP2213's multi-target nature, its potential for application in other tumor types and chronic inflammatory diseases is also worth exploring.

Conclusion

Gynostemma saponin BP2213, as an important triterpene saponin active ingredient in gynostemma, demonstrates good anti-lung cancer activity and safety. Its complex chemical structure, multi-target mechanism, and multiple pharmacological effects make it a strong candidate for the development of naturally derived anticancer drugs. Despite challenges in bioavailability and druggability, with the development of modern drug formulation technologies, BP2213 is expected to overcome these bottlenecks and become an important new drug in lung cancer treatment.

In the future, systematic pharmacokinetic research, mechanism exploration, and clinical validation will be key to driving the clinical translation of BP2213. Through multidisciplinary collaboration, gynostemma saponin BP2213 is expected to offer new treatment options for lung cancer patients and promote innovative development of natural product drugs.