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Product name: Ardisiacrispin A
Synonym name: Saxifragifolin B; Deglucocyclamin I
Catalogue No.: BP0188
Cas No.: 23643-61-0
Formula: C52H84O22
Mol Weight: 1061.22
Botanical Source: Ardisia crispa
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 Ardisiacrispin A
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
399.0000
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Ardisiacrispin A is a natural triterpene saponin derived from the genus Ardisia spp., and has attracted widespread attention in recent years due to its remarkable biological activity, especially its potential applications in anti-tumor and immunomodulatory fields. Plants of the Purple Golden Saponin genus are widely used in traditional medicine to treat various diseases, with diverse active components, among which triterpene saponins are among the main bioactive substances. As a representative of this class of compounds, Bailiangjin A exhibits cytotoxic effects on various cancer cell lines, especially significant inhibitory effects on liver cancer cells (such as HepG2 and Bel-7402) and human myeloid leukemia cells (HL-60). In addition, Bailiangjin Su A and its related compounds also demonstrate certain immunomodulatory and antiviral activities, suggesting their potential value in treating various diseases.
This paper aims to systematically review the chemical structure and physicochemical properties of Bailiang Jinsu A, plant origin and extraction methods, pharmacological activity, and mechanism of action. Combined with current druggability evaluations, it explores its clinical application prospects and development directions, providing theoretical basis and reference for subsequent drug development and basic research.
Bailiangjin A has a molecular formula of C_54H_86O_22 and a molecular weight of 1093.20 Da, making it a typical natural product of triterpene saponins. Its structural core is a pentacyclic triterpene backbone, connecting multiple glycoside residues to form a complex glycoside structure. The compound has a LogP value of about 0.10, indicating strong hydrophilicity, a high polar surface area (TPSA) of 399 Ų, and up to 22 hydrogen bond acceptors. These physicochemical properties indicate that Metreukain A has strong water solubility but may limit its ability to penetrate cell membranes.
Polysaccharide groups in the molecular structure not only affect their solubility and stability, but also have a significant impact on their biological activity and molecular targeting. The complex glycan structure of Bailiangjin A may mediate its biological function by specifically binding to cell surface receptors or intracellular targets. Additionally, this compound does not easily cross the blood-brain barrier, suggesting that its main target may be limited to peripheral tissues.
Bailiang Jinsu A mainly comes from plants of the genus Ardisia crenata, especially Ardisia crenata, which is widely used in traditional Asian medicine. Plants of the genus Zijinnius are generally rich in various triterpene saponins, which have diverse structures and rich biological activity. Bailiangjin A, as a representative compound, has been isolated and identified multiple times from the roots, stems, and leaves of plants in this genus.
Common methods for extracting Bailiangjin A include organic solvent extraction and column chromatography separation. Typically, methanol or ethanol is used as the extraction solvent, combined with ultrasound-assisted extraction or reflux extraction techniques to improve extraction efficiency. After concentration, the extract is separated and purified using silica gel column chromatography, reversed-phase high-performance liquid chromatography (RP-HPLC), and other techniques, ultimately obtaining high-purity Bailiang Jinsu A. In recent years, the introduction of supercritical CO_2 extraction and membrane separation technologies has provided new technical means for efficient extraction and purification of Bailiang Jinsu A.
Bailiangjin A exhibits significant cytotoxic effects across various tumor cell lines. Its half-growth inhibition concentration (GI_50) against human liver cancer HepG2 cells was 1.56 μM, demonstrating strong anti-proliferation ability. For another liver cancer cell line, Bel-7402, Bailiangjin A can significantly inhibit cell proliferation by inducing apoptosis and microtubule deaggregation. Additionally, when Bailiangjin A is used in combination with its homologer Ardisiacrispin B, it exhibits a strong inhibitory effect on human acute myeloid leukemia cells HL-60 by blocking cell cycle S and inducing apoptosis.
Triterpene saponins in plants of the genus Zijinnius generally possess immunomodulatory functions, and Bailiangjin A exhibits similar characteristics. Related studies have shown that Bailiangjin A can regulate macrophage function, promote cytokine secretion, and enhance the body's immune response. In addition, Bailiangjin A and its derivatives have shown inhibitory effects on certain viruses in vitro experiments, suggesting its potential application value in the antiviral field.
In recent years, Bailiangjin A has also attracted attention in research related to hyperglycemia. Although there are few reports of direct hypoglycemic activity, its targets involve various key proteins related to glucose metabolism and insulin signaling, such as EHMT2, UBP2, PAI1, AMPK, SGLT2, GCK, APP, BACE1, CES1, and PTPN1. This suggests that Bailiangjin A may participate in glucose metabolism balance through multi-target regulation and is expected to become a new candidate molecule for treating metabolic diseases.
The antitumor mechanisms of Bailiangjin A mainly include inducing apoptosis, cell cycle arrest, and microtubule skeleton destruction. Specifically, this compound activates the mitochondrial-dependent apoptotic pathway, promotes cytochrome C release, activates the caspase family, and ultimately leads to programmed cell death. At the same time, Bailiangjin A can disrupt microtubule structures, disrupt the dynamic balance of the cytoskeleton, and prevent mitosis, causing the cell cycle to stagnate in phase S.
In terms of molecular targets, Bailiangjin A exhibits multi-target effects. Its effects on tumor cells involve regulating key signaling pathways such as PI3K/Akt, MAPK, and NF-κB pathways, which influence cell proliferation, apoptosis, and inflammatory responses. For hyperglycemia-related targets, Bailiangjin A may promote energy metabolism balance by modulating AMPK activity; Reduces renal glucose reabsorption by inhibiting SGLT2; Regulating PTPN1 to enhance insulin signaling and other mechanisms, thereby exerting its potential hypoglycemic effect.
In addition, the immunomodulatory activity of Bailiangjin A may be related to its effects on macrophage surface receptors and nuclear factor regulators, modulating immune cell activation and cytokine secretion profiles, thereby enhancing the body's disease resistance.
From the perspective of druggability, Bailiangjin A has a relatively large molecular weight (1093.20 Da), far exceeding the upper limit of 500 Da recommended by Lipinski's rules. It also has a high polar surface area and hydrogen bond receptor count, suggesting that its oral bioavailability may be low and its membrane permeability is limited. Additionally, its LogP value is close to 0, indicating strong hydrophilicity, but may affect transmembrane absorption.
Bailiang Jinsu A is difficult to cross the blood-brain barrier, limiting its application in central nervous system diseases. Currently, data on its hepatotoxicity, cardiotoxicity, and hERG channel inhibition are lacking, and further systematic evaluation is needed to ensure safety. Ames-related mutagenic assay data have not yet been reported; toxicological research should be strengthened in the future.
In terms of pharmacokinetics, the in vivo absorption, distribution, metabolism, and excretion (ADME) characteristics of Bailiangjin Su A have not yet been systematically elucidated. Given its large molecules and highly polar structure, there may be risks of poor intestinal absorption, slow metabolism, and accumulation in the body. In the future, it is necessary to combine in vivo and in vitro experiments to clarify metabolic pathways and drug interactions, providing scientific evidence for clinical application.
With its remarkable antitumor activity and multi-target regulatory capability, Bailiangjin A has the potential to become a candidate molecule for novel anticancer drugs. Especially in the treatment of liver cancer and leukemia, Bailiangjin A exerts tumor-suppressing effects by inducing apoptosis and blocking the cell cycle, providing new ideas for developing targeted therapies. At the same time, its immunomodulatory and antiviral properties have broadened its application scope, and it is expected to play a role in immunotherapy and anti-infection fields in the future.
Targeting multiple regulatory targets related to hyperglycemia, Bailiangjin A may become a novel molecule for comprehensive treatment of metabolic diseases, especially suitable for multi-target drug development strategies. However, its poor druggability limits the development of oral formulations, requiring structural modification, nanocarrier encapsulation, or drug route optimization to enhance bioavailability and targeting.
Future research should focus on the following aspects: (1) Systematically elucidating the detailed mechanism of action and molecular target network of Bailiang Jinsu A; (2) Conduct comprehensive pharmacokinetic and toxicological evaluations to ensure safety; (3) Enhancing drug properties through medicinal chemical modification and formulation optimization; (4) Conduct animal models and preclinical studies to evaluate treatment efficacy and potential side effects.
Bailiangjin A, as an important triterpene saponin in the genus Zijinnius, demonstrates broad medicinal value due to its diverse biological activity and unique molecular structure. Its potential applications in anti-tumor, immunomodulatory, and metabolic diseases provide abundant material and directions for pharmacological research of natural products. Although challenges remain in druggability and clinical translationality, with the development of modern drug R&D technologies, Bailiangjin Su A is expected to become an important candidate for the new generation of multifunctional natural medicines. In the future, through interdisciplinary collaboration, we will deeply explore its mechanisms of action and optimize drug properties, promoting the application of Bailiangjin Su A and its derivatives in clinical treatment, achieving the successful transformation of natural products into clinical drugs.
Shenshuai
Wenjing
Hedandan
