Product name: Eclalbasaponin I
Synonym name:
Catalogue No.: BP4201
Cas No.: 158511-59-2
Formula: C₄₂H₆₈O₁₄
Mol Weight: 796.992
Botanical Source: EcliptaprostrataL.
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.

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

Introduction/Overview

Eclalbasaponin I is a natural triterpenoid saponin compound isolated from the traditional medicinal plant Eclipta prostrata L. (Asteraceae). Mohan lotus is widely used in traditional Chinese medicine for clearing heat and detoxifying, promoting blood circulation and stopping bleeding, and protecting the liver. In recent years, the pharmacological effects of its active ingredients have attracted widespread attention. As one of the important active ingredients in this plant, drought lotus saponin I exhibits significant anti-tumor and anti-inflammatory activities, especially in inhibiting the proliferation of liver cancer cells. This article aims to systematically review the chemical structure and physicochemical properties, plant sources and extraction methods, pharmacological activity and mechanism of action, pharmacological evaluation and pharmacokinetic characteristics of drought lotus saponin I, and explore its clinical application prospects and future research directions.

Chemical structure and physicochemical properties

The molecular formula of drought lotus saponin I is C42H66O15, with a molecular weight of 796.9920, and it belongs to the natural triterpenoid saponin class. Its structure is composed of triterpenoid parent nuclei connected to multiple glycosides through glycosidic bonds, exhibiting typical saponin molecular characteristics. The LogP value is 2.6368, indicating that it has moderate lipid solubility, which is beneficial for membrane penetration. The polar surface area (TPSA) is 236.0600, indicating high polarity and hydrogen bond donor/acceptor ability, which is related to its polysaccharide structure. Low water solubility (0.0697) suggests limited solubility in aqueous phase, which may affect oral bioavailability. The low permeability of the blood-brain barrier indicates limited distribution in the central nervous system. The hERG channel inhibition experiment was negative, indicating a low risk of cardiac toxicity. The Ames mutagenicity test result is 0.0, indicating no significant genotoxicity.

Plant sources and extraction methods

The main source of saponin I in Eclipta prolata L. is Eclipta prolata, which is widely distributed in tropical and subtropical regions of Asia, Africa, and the Americas. Traditionally, drought lotus has been used as a herbal medicine to treat various diseases. Modern pharmacological research has found that drought lotus contains various active ingredients, including flavonoids, triterpenoid saponins, volatile oils, and polysaccharides.

The common methods for extracting saponins I from drought lotus include:

1. Solvent extraction Using ethanol or methanol as the main solvent, saponin components can be effectively dissolved through reflux or ultrasound assisted extraction.
2. Separation and purification Using liquid-liquid distribution, silica gel column chromatography, reverse phase high performance liquid chromatography (RP-HPLC) and other techniques, gradually enrich and purify the saponin I of Eclipta alba.
3. Structural Identification Confirm its chemical structure through methods such as mass spectrometry (MS), nuclear magnetic resonance (NMR), and infrared spectroscopy (IR).

In recent years, the application of supercritical fluid extraction and membrane separation technology has also provided new ideas for improving extraction efficiency and purity.

Pharmacological activity research

Antitumor activity

Mojianlian saponin I has shown significant anti-tumor activity in multiple in vitro experiments. Especially in the liver cancer cell line SMMC-7721, drought lotus saponin I can effectively inhibit cell proliferation, with a half maximal inhibitory concentration (IC50) of 111.1703 μ g/ml. This inhibitory effect may be closely related to inducing cell apoptosis, blocking the cell cycle, and inhibiting tumor related signaling pathways.

In addition, the activity of drought lotus saponin I on other tumor cell lines still needs further systematic evaluation, but previous studies have suggested that it has certain growth inhibitory effects on various cancer cells.

anti-inflammatory activity

Inflammatory response is the basis for the occurrence and development of various diseases, and the anti-inflammatory mechanism of drought lotus saponin I is gradually being revealed. It mainly works by regulating various inflammation related targets, including:

• IL-6 and TNF Inhibit the expression of pro-inflammatory cytokines and alleviate inflammatory reactions.
• STAT3 Block the activation of signal transduction and transcription activator 3, and inhibit inflammatory signal transduction.
• CASP1 Regulate the activity of inflammasomes and reduce the release of inflammatory mediators.
• PTGS1 and PTGS2 (COX-1 and COX-2)Inhibit prostaglandin synthesis and reduce levels of inflammatory mediators.
• NOS2 Reduce the expression of inducible nitric oxide synthase and decrease oxidative stress.
• NFKB1 Inhibit the nuclear factor kappa B signaling pathway and block the transcription of inflammatory genes.
• TRPV1 and TRPA1 Regulate pain and inflammation receptors, alleviate inflammation related symptoms.

The comprehensive regulation of these targets results in good anti-inflammatory effects of drought lotus saponin I in various inflammatory models.

Mechanism of action and molecular targets

The pharmacological effects of drought lotus saponin I mainly depend on its interactions with various cellular signaling pathways and key molecules. The molecular mechanisms of its anti-tumor and anti-inflammatory effects mainly include:

1. Inducing cell apoptosis
   Emodin I can activate endogenous apoptotic pathways, regulate the expression of Bcl-2 family proteins, promote Caspase cascade reactions, and ultimately trigger tumor cell apoptosis.

2. Inhibition of cell proliferation and cell cycle arrest
   By regulating cell cycle proteins and their dependent kinases, the cell cycle process is blocked and tumor cell proliferation is inhibited.

3. Regulating inflammatory signaling pathways
   Inhibit the activity of transcription factors such as NF - κ B and STAT3, reduce the expression of pro-inflammatory factors such as IL-6 and TNF - α, and alleviate inflammatory responses.

4. Antioxidant and inhibition of oxidative stress
   By inhibiting the expression of NOS2 and reducing the production of excessive nitric oxide, oxidative damage can be alleviated.

5. Regulating pain and sensory pathways
   Acting on TRPV1 and TRPA1 ion channels to alleviate inflammation related pain.

The synergistic effect of these mechanisms endows drought lotus saponin I with multi-target and multi pathway therapeutic potential.

Evaluation of drug properties and pharmacokinetics

From the perspective of medicinal properties, drought lotus saponin I has the following characteristics:

• High molecular weight (796.9920)Beyond the ideal range of traditional small molecule drugs, it may affect their oral absorption and bioavailability.
• Moderate lipid solubility (LogP 2.6368)It is beneficial for cell membrane penetration, but high polarity (TPSA 236.0600) may limit its ability to pass through the cell membrane.
• Low water solubility (0.0697)It is suggested that its solubility in aqueous phase is limited, and the dissolution and absorption need to be improved through formulation technology.
• Low permeability of blood-brain barrier Reduce the risk of central nervous system side effects, but limit its use for the treatment of central nervous system diseases.
• No hERG channel inhibition Low risk of cardiac toxicity.
• No genotoxicity (Ames test negative)The safety is relatively good.

At present, there is limited pharmacokinetic research on the saponin I of drought lotus. Preliminary data suggests that its oral absorption rate is low, and the metabolic pathway in vivo may involve the corresponding enzyme system in the liver. In the future, systematic ADME (absorption, distribution, metabolism, excretion) research needs to be conducted to clarify its in vivo behavior and optimize the dosing regimen.

Clinical application prospects and prospects

Due to its significant anti-tumor and anti-inflammatory activities, drought lotus saponin I has demonstrated good clinical application potential. Especially in the adjuvant therapy of malignant tumors such as liver cancer, it has great development value. In addition, its ability to regulate inflammation through multiple targets provides a new therapeutic approach for chronic inflammatory diseases such as autoimmune diseases and metabolic syndrome.

However, the clinical application of drought lotus saponin I still faces many challenges:

• Pharmacokinetic Characteristics Limitations Factors such as high molecular weight and poor water solubility affect its bioavailability and in vivo distribution.
• Insufficient safety and toxicology data A systematic assessment of the safety risks of long-term medication is required.
• Lack of preclinical and clinical research Urgent animal model validation and early clinical trials are needed to clarify its efficacy and safety.

Future research should focus on:

1. Optimize the extraction and purification process to improve the purity and stability of the product.
2. Improve its pharmacokinetic properties through structural modifications or drug delivery systems such as nanocarriers.
3. Thoroughly analyze the mechanism of action and explore more potential targets.
4. Conduct systematic toxicological and pharmacological evaluations to promote clinical translation.

Conclusion

As an important active ingredient in drought lotus, drought lotus saponin I has significant anti-tumor and anti-inflammatory activities, and its mechanism of action involves the regulation of multiple targets and signaling pathways. Its good safety indicators provide favorable conditions for future drug development. Despite challenges in terms of drug efficacy and pharmacokinetics, through the application of modern drug design and formulation technology, drought lotus saponin I is expected to become an important candidate molecule in the development of natural product drugs. In the future, it is necessary to strengthen its preclinical research and clinical trials, promote its application in the treatment of tumors and inflammatory diseases, and achieve the transformation from traditional medicinal plants to modern drugs.