Product name: Cauloside D
Synonym name: Hederoside G
Catalogue No.: BP2105
Cas No.: 12672-45-6
Formula: C₅₃H₈₆O₂₂
Mol Weight: 1075.25
Botanical Source: Hedera helix
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 Cauloside D

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

Introduction/Overview

Cauloside D is a triterpene saponin derived from the traditional Chinese medicinal herb Caulophyllum robustum Max, and has attracted widespread attention in recent years due to its remarkable biological activity. As a triterpene saponin with a complex structure, heptasaponin D demonstrates unique potential in multiple pharmacological effects such as anti-inflammatory and antitumor effects, especially in the treatment of malignant tumors like ovarian cancer. This paper aims to systematically review the chemical structure, origin, pharmacological activity, and mechanism of action of Hongmao heptasaponin D, and, combined with its druggability parameters, explore its clinical application prospects and development direction as a candidate molecule for novel natural medicines.

Chemical structure and physicochemical properties

Erythrosaponin D belongs to the triterpene saponin class with a complex molecular formula and a triterpene backbone modified by polysaccharide chains. Its molecular weight is 1075.2490, with a LogP value of 2.0240, showing moderate lipid solubility that facilitates penetration of cell membranes. The polar surface area (TPSA) reached as high as 353.9, indicating that the molecule contains a large number of polar groups, which may affect its oral bioavailability and membrane permeability. The water solubility is 0.2109, indicating low water solubility but still possessing some solubility. Low blood-brain barrier permeability means limited impact on the central nervous system, reducing potential neurotoxicity risk. The hERG inhibition test results were negative, indicating that heptasaponin D has a weak inhibitory effect on cardiac potassium channels and is relatively safe. The Ames mutagenic test result was 0.0, indicating no significant genotoxicity and meeting the basic requirements for safe medication.

Plant Origins and Extraction Methods

Caulophyllum robustum Max is mainly isolated from the rhizome of Caulophyllum robustum Max. Hongmao Qi is a plant in the Ranunculaceae family, widely distributed in Northeast and Southwest China. In traditional Chinese medicine, it is used to promote blood circulation, remove blood stasis, regulate menstruation, and relieve pain. During extraction, ethanol or methanol is usually used as solvents for extraction and then purified by liquid-liquid separation, silica gel column chromatography, and high-performance liquid chromatography (HPLC). In recent years, the application of ultrasound-assisted extraction and microwave-assisted extraction technologies has significantly improved the extraction efficiency and purity of Heptosaponin D, laying the foundation for its large-scale preparation.

Pharmacological activity research

The pharmacological activity of Hongmao Heptasaponin D mainly focuses on anti-inflammatory and antitumor aspects. Multiple in vivo and in vitro experiments have shown that heptasaponin D can significantly inhibit the expression of induced nitric oxide synthase (iNOS), reduce the secretion of pro-inflammatory cytokines such as TNF-α, IL-1β, and IL-6, thereby exerting anti-inflammatory effects. Its anti-inflammatory mechanism involves regulating the nuclear factor κB (NF-κB) signaling pathway, reducing tissue damage caused by inflammatory responses.

In the field of oncology, especially in ovarian cancer models, heptasaponin D demonstrates anti-cancer potential through multi-target regulation. It can regulate the expression of the apoptosis-related protein BCL2, promoting apoptosis in cancer cells; At the same time, it inhibits the STAT3 signaling pathway, blocking tumor cell proliferation and metastasis. Additionally, the inhibition of multidrug resistance-related protein ABCB1 by heptasaponin D helps reverse chemotherapy resistance. Its effect on the oxidative stress regulator NFE2L2 also suggests its role in antioxidant stress. TOP1 and TOP2A, as DNA topoisomerases, further hinder the DNA replication and repair processes of cancer cells. Regulation of MAPK1 and ESR1 involves cell signal transduction and hormone receptor-mediated tumor growth regulation. Overall, heptasaponin D has broad application prospects in ovarian cancer treatment through its multi-target and multi-pathway synergistic effects.

Mechanism of action and molecular targets

The mechanism of action of heptasaponin D mainly revolves around its regulation of inflammation- and tumor-related signaling pathways. By inhibiting iNOS (NOS2) expression, it reduces excessive production of nitric oxide (NO), lowers the release of inflammatory mediators, and alleviates inflammatory responses. Meanwhile, heptagenin D can downregulate the expression of pro-inflammatory cytokines TNF-α, IL-1β, and IL-6, inhibit activation of NF-κB and STAT3 signaling pathways, and block the transmission of inflammatory signals.

In tumor cells, heptasaponin D promotes mitochondrial pathway-mediated apoptosis by regulating BCL2 family proteins. Its inhibition of STAT3 not only reduces tumor cell proliferation but also suppresses tumor immune evasion. The inhibitory effect of ABCB1 helps increase the intracellular concentration of chemotherapy drugs and enhances their efficacy. Regulation of NFE2L2 improves cellular antioxidant capacity, protecting normal cells from oxidative damage. Inhibition of TOP1 and TOP2A blocks DNA topoisomerase activity, interferes with DNA replication and transcription, and suppresses tumor cell proliferation. Regulation of the MAPK1 signaling pathway affects the cell cycle and apoptosis, while ESR1 regulation may influence the growth of hormone-dependent tumors. As a key component of the PI3K/AKT signaling pathway, PIK3CA's regulation helps inhibit tumor cell survival and migration.

In summary, Erythrosaponin D exerts its combined anti-inflammatory and antitumor effects through synergistic regulation of multiple targets and multi-signal pathways, providing new ideas for targeted therapy.

Druggability evaluation and pharmacokinetics

From the perspective of druggability, heptasaponin D demonstrates certain advantages and challenges. Its molecular weight is relatively large (1075.2490), exceeding the ideal range for traditional oral medications and potentially limiting its oral absorption. A high TPSA value (353.9) suggests strong molecular polarity, which may affect membrane permeability and bioavailability. The LogP was 2.024, indicating moderate lipid-water affinity and favorable for distribution in the body.

Low water solubility (0.2109) may affect formulation design and in vivo solubility, but can be improved through drug delivery systems such as nanocarriers and liposomes. The blood-brain barrier has low permeability, reducing the risk of central nervous system toxicity but limiting its application in brain diseases. The inhibition of hERG channels and their lack of mutagenicity (Ames test 0.0) provide good safety assurance.

Currently, pharmacokinetic data on heptasaponin D are not yet complete, and it is speculated that its metabolism may involve glycoside hydrolysis of liver enzymes and oxidative modification of the triterpene skeleton. In the future, systematic ADME (Absorption, Distribution, Metabolism, Excretion) studies are needed to clarify its in vivo kinetic characteristics and provide a basis for clinical application.

Prospects and outlooks for clinical applications

As a natural triterpenoid saponin with multiple biological activities, heptosaponin D shows significant potential, especially in the fields of anti-inflammatory and anti-tumor treatments. By regulating multiple key molecular pathways, it provides new targets and strategies for the treatment of malignant tumors such as ovarian cancer. Combined with its excellent safety indicators, heptasaponin D is expected to become an important candidate molecule for natural drug development.

However, current research mostly focuses on in vitro cell and animal models, lacking systematic preclinical and clinical trial data. In the future, in-depth research on pharmacokinetics, toxicology, and pharmacodynamics should be strengthened, optimizing drug formulations and administration routes. At the same time, by integrating modern drug design technologies such as structural modification and nanocarrier delivery, their bioavailability and targeting are enhanced.

In addition, the potential of heptagenin D in combination chemotherapy, immune regulation, and chronic inflammatory diseases is also worth further exploration. Interdisciplinary research collaboration will promote the transition from the laboratory to clinical practice, driving the development of natural product drugs.

Conclusion

As a natural triterpene saponin with a clear origin and unique structure, Hongmao Heptacenoside D demonstrates broad medicinal value due to its remarkable anti-inflammatory and antitumor activities. Its multi-target and multi-mechanism mode of action offers new ideas for the treatment of complex diseases. Although there are still certain challenges in druggability and clinical translationality, with deeper research and technological advancements, Hongmaoheptasaponin D is expected to become an important breakthrough in the field of natural product pharmacology, contributing to innovative development of natural medicines. Future research should focus on systematic pharmacokinetic evaluation, mechanistic analysis, and preclinical validation to advance clinical application.