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Product name: Schisandrin A
Synonym name: Deoxyschizandrin; Schizandrin A; Wuweizisu A; Dimethylgomisin J; Deoxyschisandrin
Catalogue No.: BP1261
Cas No.: 61281-38-7
Formula: C24H32O6
Mol Weight: 416.514
Botanical Source: Schisandra chinensis（Turcz.）Baill.
Physical Description:
Type of Compound: Lignans
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 Schisandrin A
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
55.3800
4.9614
4.9620
.0013
6.0309
20.5728
High
89.3584
3.2579
Yes
No
No
No
No
No
0.0
Yes
No
No
Yes
Schisandrin A (CAS No.: 61281-38-7) is an important diphenylcyclohexane lignan compound isolated from the traditional Chinese medicinal material Schisandra chinensis. As one of the most bioactive components in Schisandra, Schisandra methylene has attracted widespread attention in the field of natural product pharmacology. Its unique chemical structure gives it multiple biological activities, especially showing significant effects in liver protection, antioxidant properties, anti-inflammation, and regulation of drug metabolism enzymes. In recent years, with in-depth research into the pathogenesis of liver diseases, Schisandra methyl extract, as a potential liver protectant, has gradually become a research hotspot.
This review aims to systematically summarize the chemical structure and physicochemical properties of Schisandra methylene, plant origin, and extraction methods, with a focus on evaluating its pharmacological activity and mechanism of action, exploring its druggability and pharmacokinetic characteristics, and looking ahead to its potential and challenges in clinical application, with the hope of providing theoretical support and practical guidance for related research.
The chemical name of Schisandra methyl is (±)-3,4,5,6,7,8-hexahydro-1,1-dimethyl-6,7-dimethoxy-2H-benzo[c]chromen-2-one, molecular formula C24H32O7, molecular weight 416.5140. Its structural core is the diphenylcyclohexane lignan backbone, which contains multiple methoxy substituents, giving it strong lipid solubility.
In terms of physicochemical properties, Schisandra methyl has a LogP value of 4.9614, showing high lipid solubility, which helps penetrate cell membranes and the blood-brain barrier (BBB has high permeability). Its polar surface area (TPSA) is 55.38 Ų, and its water solubility is extremely low (0.0013 mg/mL), suggesting limited solubility in the aqueous phase and possibly affecting oral absorption and bioavailability. In terms of safety, Schisandra methyl did not show hERG channel inhibitory activity, and the Ames mutagenicity test was negative, indicating good safety profiles.
Schisandra methyl also exhibited inhibitory effects on the CYP3A subtype of the cytochrome P450 enzyme system, with IC50 at 6.60 μM and Ki at 5.83 μM, suggesting it may affect the metabolic processes of various drugs and requires attention in clinical application.
Schisandra chinensis mainly originates from Schisandra chinensis, a traditional Chinese medicinal herb widely distributed in Northeast China, North China, and the Korean Peninsula. The fruit of Schisandra is rich in various lignan compounds, with a high content of methyl glycosin, which is often used as a quality control indicator.
The extraction process typically uses organic solvent extraction combined with column chromatography separation technology. Common extraction solvents include ethanol, methanol, and their aqueous solutions. Utilizing their lipid solubility, coarse extraction is performed first, followed by purification and separation by silica gel column chromatography, reversed-phase high-performance liquid chromatography (RP-HPLC), and other methods. In recent years, green extraction technologies such as ultrasound-assisted extraction and microwave-assisted extraction have also been applied to improve extraction efficiency and purity.
The optimization of the extraction process not only improves the yield of Schisandra methylene but also provides a stable and reliable raw material guarantee for subsequent pharmacological activity research and drug development.
Schisandra methylene has been the most in-depth research in the field of liver protection. Multiple in vivo and in vitro experiments have shown that Schisandra methyl can significantly reduce pathological conditions such as drug-induced liver injury, alcoholic liver injury, and liver fibrosis. Its hepatoprotective effects mainly manifest as antioxidant, anti-inflammatory, and regulation of hepatocyte apoptosis.
In the drug-induced liver injury model, Schisandra methyl activates the nuclear factor 2-related factor 2 (NRF2) signaling pathway, promoting the expression of downstream antioxidant enzymes such as superoxide dismutase (SOD1, SOD2), catalase (CAT), glutathione peroxidase (GPX1), and NAD(P)H-quinone oxidoreductase 1 (NQO1), significantly enhancing cellular antioxidant defense, reducing reactive oxygen species (ROS) accumulation, and alleviating oxidative stress damage.
Additionally, Schisandra methyl can downregulate the expression of transforming growth factor β1 (TGFB1) and α smooth muscle actin (ACTA2), inhibit hepatic stellate cell activation, and slow down the progression of liver fibrosis. Its regulatory effect on matrix metalloproteinase 9 (MMP9) also helps maintain hepatic stromal homeostasis and prevents excessive fibrosis.
Schisandra methyl hormone induces the expression of various antioxidant enzymes by modulating the NRF2/ARE signaling pathway, significantly enhancing cellular resistance to oxidative damage. Its anti-inflammatory effect is related to inhibiting the activation of nuclear factor κB (NF-κB) and the expression of downstream pro-inflammatory cytokines, effectively reducing inflammatory responses.
Schisandra methyl extract has a significant inhibitory effect on the hepatic drug-metabolizing enzyme CYP3A, with IC50 and Ki values of 6.60 μM and 5.83 μM, respectively. As one of the most important drug-metabolizing enzymes in the human body, CYP3A participates in the metabolic transformation of various drugs. The inhibitory effect of Schisandra methyl suggests it may cause drug interactions, affecting the metabolic kinetics and efficacy of concomitant drugs.
The biological effects of Schisandra methyl are mainly realized through multiple signaling pathways and molecular targets:
NRF2/ARE signaling pathway: Schisandra methyl activates NRF2, promotes its nuclear translocation, enhances antioxidant enzyme gene expression, improves cellular antioxidant capacity, and reduces oxidative stress.
Anti-inflammatory signaling regulation: By inhibiting the NF-κB pathway, it reduces the release of pro-inflammatory cytokines (such as TNF-α, IL-6), alleviating inflammatory responses.
Targets related to liver fibrosis: downregulate TGFB1 and ACTA2 expression, inhibit hepatic stellate cell activation, reduce collagen deposition, and alleviate liver fibrosis.
Matrix metalloproteinase regulation: modulates MMP9 expression, maintains dynamic liver matrix balance, and prevents excessive fibrosis.
Drug metabolism enzyme inhibition: Directly inhibits CYP3A enzyme activity, affecting drug metabolism and suggesting potential risks in combination therapy.
These multi-target and multi-pathway mechanisms together form the basis of the multiple pharmacological effects of Schisandra methylene.
The drug-making evaluation of Schisandra Jiasu shows that it has certain advantages and challenges:
Lipid solubility and bioavailability: High LogP value (4.96) and low water solubility (0.0013 mg/mL) indicate strong lipid solubility, but poor water solubility may limit oral absorption efficiency. Formulation technology is needed to improve its solubility and bioavailability.
Blood-brain barrier permeability: High blood-brain barrier permeability suggests it may act in the central nervous system, broadening its indication range.
Safety: No hERG inhibition and no mutagenicity (Ames test negative), indicating good safety.
Pharmacokinetic characteristics: Current studies show that Schisandra methyl extract is absorbed quickly after oral administration, widely distributed in the body, and significantly enriched in the liver, meeting the targeted requirements for its hepatoprotective effects. Its inhibitory effect on CYP3A suggests possible drug interaction risks, requiring further study of its metabolic pathways and clearance mechanisms.
Overall, Schisandra Methyl has good safety and bioactivity, but its pharmacokinetic properties need to be optimized to enhance its clinical application potential.
As a natural product, Schisandra methyl extract has broad clinical application prospects due to its significant hepatoprotective effects and good safety. Its potential therapeutic value in various liver diseases such as drug-induced liver injury, alcoholic liver disease, non-alcoholic fatty liver, and liver fibrosis has been confirmed by extensive basic research.
Future clinical translation should focus on the following aspects:
Dosage form development and administration route optimization: To address its poor water solubility, new dosage forms such as nanoformulations, liposomes, and solid dispersions are developed to improve oral bioavailability.
Drug interaction research: In-depth evaluation of its effects on CYP3A and other drug-metabolizing enzymes, guiding rational combination therapy to avoid adverse reactions.
Clinical trial design: Conduct systematic clinical safety and efficacy evaluations to clarify indication scope and dosage.
Multi-target mechanism research: Combining modern molecular biology techniques, further elucidating its mechanism of action and exploring new indications.
Combination therapy strategies: Explore synergistic effects with other liver-protective drugs or antioxidants to enhance treatment outcomes.
In summary, as a natural product with multiple pharmacological activities, Schisandra methyl extract has the potential to become a new drug for treating liver diseases, but its clinical application still requires overcoming challenges in pharmacokinetics and drug interactions.
As the main active ingredient in Schisandra, Schisandra methyl extract demonstrates significant pharmacological activity in liver protection and antioxidant fields due to its unique chemical structure and multi-target mechanism. By activating the NRF2 signaling pathway, regulating antioxidant enzyme expression, suppressing inflammatory responses, and modulating molecules related to liver fibrosis, it achieves multi-layered protection for the liver. At the same time, the inhibitory effect of Schisandra methyl acid on CYP3A suggests that drug interactions should be considered in clinical applications.
In the future, by integrating modern drug formulation technologies and systematic pharmacokinetic research, optimizing the druggability of Schisandra Jiasu will provide a solid foundation for its clinical translation. With deeper analysis of its mechanism of action and advances clinical research, Schisandra Methyl Extract is expected to become an effective natural medicine for treating liver diseases, contributing new strength to pharmacological research of natural products and liver disease treatment.
Shenshuai
Wenjing
Hedandan
