Product name: Catechin hydrate
Synonym name: (+)-Catechin hydrate
Catalogue No.: BP0511
Cas No.: 225937-10-0
Formula: C₁₅H₁₄O₆·xH2O
Mol Weight: 290.271(anhydrous basis)
Botanical Source: Green Tea
Physical Description:
Type of Compound: Polyphenols

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.

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

Introduction/Overview

Catechin hydrate, as an important natural polyphenolic compound, has attracted widespread attention in the field of natural product pharmacology in recent years due to its remarkable biological activity and potential medicinal value. Catechin compounds are widely found in various plants, especially abundant in tea, and possess good antioxidant, anti-inflammatory, anti-tumor, and cardiovascular protective effects. Hydrated catechins, as the hydrated form of catechins, exhibit excellent inhibition of cyclooxygenase-1 (COX-1) activity, with an IC50 value of 1.4 μM, indicating strong anti-inflammatory potential. Additionally, hydrated catechins demonstrate strong cellular protective abilities by regulating various antioxidant-related targets such as NFE2L2 (NRF2), SOD1, CAT, GPX1, HMOX1, and SOD2 in terms of antioxidant damage. This paper will systematically review the chemical structure and physicochemical properties of hydrated catechins, plant origins and extraction methods, pharmacological activity, mechanism of action, druggability evaluation, and clinical application prospects, aiming to provide a theoretical basis and reference for further research and development of this compound.

Chemical structure and physicochemical properties

The chemical name of hydrated catechin is (2R,3S)-3,3',4',5,7-pentahydroxyflavan-3-ol, with a molecular formula C15H14O6 and a molecular weight of 290.2710. Its CAS number is 225937-10-0. Hydrated catechins belong to flavan-3-ol compounds containing multiple hydroxyl groups in their structure, which impart excellent hydrophilicity and antioxidant activity. Its physicochemical properties show a LogP value of 0.9710, indicating moderate lipid solubility, which benefits bioavailability in the body. The polar surface area (TPSA) is 110.38 Ų, reflecting its high molecular polarity, which may affect its cell membrane penetration ability. Water solubility is 0.7536, indicating a certain solubility in water, which aids in formulation development and absorption in the body. The low permeability of the blood-brain barrier suggests that its role in the central nervous system may be limited. The hERG channel inhibition test was negative, indicating a low risk of cardiotoxicity. The Ames test result was 0.0, indicating that hydrated catechins showed no significant genotoxicity.

Plant Origins and Extraction Methods

Hydrated catechins are widely found in various plants, especially abundant in tea leaves (Camellia sinensis) and its products. Besides tea, hydrated catechins can also be detected in certain fruits, nuts, and medicinal plants. Its extraction mainly uses water or alcohol solvents, and is obtained through extraction techniques, ultrasound-assisted extraction, or microwave-assisted extraction. In recent years, green extraction technologies such as supercritical fluid extraction and enzyme-assisted extraction have been gradually applied to improve extraction efficiency and purity, while also reducing environmental pollution. After extraction, purity analysis and structural identification are often performed using liquid chromatography (HPLC) and mass spectrometry techniques. During purification, reversed-phase high-performance liquid chromatography (RP-HPLC) is a commonly used separation method, effectively separating hydrated catechins from other structurally similar isomers.

Pharmacological activity research

The pharmacological activity of hydrated catechins is mainly reflected in antioxidant, anti-inflammatory, anti-tumor, and cardiovascular protection.

1. Antioxidant activity
   Hydrated catechins significantly reduce oxidative stress damage by scavenging free radicals, inhibiting lipid peroxidation, and enhancing endogenous antioxidant enzyme activity. In vitro studies have shown that hydrated catechins can activate the NFE2L2/NRF2 signaling pathway, promoting the expression of downstream antioxidant enzymes such as SOD1, CAT, GPX1, and HMOX1, thereby enhancing cellular resistance to oxidative damage.

2. Anti-inflammatory effects
   Hydrated catechins exhibited strong inhibitory effects on cyclooxygenase-1 (COX-1), with an IC50 of 1.4 μM, suggesting potential anti-inflammatory activity. COX-1 is a key enzyme in prostaglandin synthesis, involved in inflammatory responses and gastrointestinal protection. Hydrated catechins reduce inflammatory responses by inhibiting COX-1 activity, and due to their high selectivity, they have relatively fewer side effects.

3. Antitumor effects
   Some studies have shown that hydrated catechins can exert anti-tumor effects by inducing cancer cell apoptosis and inhibiting tumor cell proliferation and migration. Its mechanism involves regulating cell cycle-related proteins, activating apoptotic signaling pathways, and inhibiting the tumor-related inflammatory microenvironment.

4. Cardiovascular protection
   Hydrated catechins improve vascular endothelial function, lower blood lipids, and inhibit platelet aggregation through antioxidant and anti-inflammatory effects, providing protection against cardiovascular diseases. Its regulation of vasodilatory factors such as nitric oxide (NO) further enhances its cardiovascular protective effects.

Mechanism of action and molecular targets

The multi-target mechanism of hydrated catechins mainly involves antioxidant and anti-inflammatory aspects:

1. Antioxidant mechanism
   Hydrated catechins promote the expression of antioxidant enzyme genes by activating the NFE2L2/NRF2 signaling pathway, thereby enhancing intracellular antioxidant capacity. NFE2L2, as a key transcription factor in cells, regulates the expression of antioxidant enzymes such as SOD1, CAT, GPX1, HMOX1, and SOD2, helping to resist cellular damage caused by oxidative stress. Additionally, hydrated catechins directly scavenge free radicals, reduce ROS accumulation, and protect cell membrane lipids from oxidation.

2. Anti-inflammatory mechanism
   Hydrated catechins reduce prostaglandin synthesis and lower the release of inflammatory mediators by inhibiting COX-1 activity. COX-1 inhibitors are often associated with gastrointestinal side effects, but the selective inhibition of hydrated catechins and their natural sources may make them safer anti-inflammatory candidate compounds. Additionally, hydrated catechins may further exert anti-inflammatory effects by inhibiting the NF-κB signaling pathway, reducing the expression of pro-inflammatory cytokines such as TNF-α and IL-6.

3. Other targets and signaling pathways
   Research also indicates that hydrated catechins may affect signaling pathways such as MAPK and PI3K/Akt, regulate cell apoptosis and proliferation, and participate in anti-tumor and cell-protective effects.

Druggability evaluation and pharmacokinetics

The druggability parameters of hydrated catechins indicate that they have certain potential for drug development. The molecular weight is 290.2710, which complies with the Lipinski rule, and the LogP value is 0.9710, indicating moderate lipid solubility, which is beneficial for absorption and distribution in the body. TPSA was 110.38 Ų, indicating moderate polarity, which may affect oral bioavailability and cell membrane permeability. Water solubility is 0.7536, making it suitable for the development of water-based formulations.

The lower permeability of the blood-brain barrier limits its application in central nervous system diseases, but also reduces the risk of CNS toxicity. The hERG channel inhibition test was negative, indicating a low risk of cardiotoxicity and good safety. The Ames test result was 0.0, indicating no significant genotoxicity and meeting drug safety requirements.

Pharmacokinetics, hydrated catechins are absorbed orally relatively quickly, but due to their high polarity, their bioavailability may be limited. Metabolism in the body mainly occurs through the liver enzyme system, with most metabolic products being glucuronide and sulfate complexes. Its half-life is moderate, making it suitable for routine administration. Further research is needed in the future on its internal distribution, metabolic kinetics, and excretion pathways to optimize the administration regimen.

Prospects and outlooks for clinical applications

As a naturally derived polyphenolic compound, hydrated catechins exhibit significant antioxidant and anti-inflammatory activities, showing broad clinical application prospects. Its potential therapeutic value in chronic inflammatory diseases such as arthritis, cardiovascular diseases, and metabolic syndrome has attracted significant attention. Due to its good safety and low toxicity, hydrated catechin is expected to serve as an adjunct therapy, reducing the side effects of traditional drugs.

In addition, the application of hydrated catechins in diseases related to antioxidant damage is also significant, such as neurodegenerative diseases, diabetes, and liver diseases. By regulating the NFE2L2/NRF2 pathway, it enhances cellular antioxidant defenses and may slow disease progression.

In the future, with further research into the pharmacological mechanisms of hydrated catechin and the progress of clinical trials, its potential as a novel natural drug or health supplement will become even more apparent. By combining nanotechnology with drug carrier systems, it is expected to improve bioavailability and targeting, expanding its clinical application scope.

Conclusion

As an important natural polyphenolic compound, hydrated catechins demonstrate excellent pharmacological effects and pharmaceutical potential due to their remarkable antioxidant and anti-inflammatory activities. It regulates intracellular oxidative stress and inflammatory responses through multiple targets and pathways, exerting cellular protective effects. Physicochemical properties and safety evaluations support its development as a candidate drug. In the future, systematic research on its pharmacokinetic properties and clinical efficacy should be strengthened to promote its translational application across various diseases. In summary, hydrated catechins are highly promising natural product drugs worthy of in-depth exploration and utilization in natural drug development and disease treatment.