Product name: Schizandrol A
Synonym name: Wuweizichun A; Wuweizi alcohol A; Schisandrin; Schisandrol A
Catalogue No.: BP1265
Cas No.: 7432-28-2
Formula: C24H32O7
Mol Weight: 432.513
Botanical Source: Schizandra chinensis
Physical Description: Cryst.
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, up to kilograms
Inquire for bulk scale.
Descriptions:
Schisandrin A and schisandrin B are active components of Schisandrae Fructus, has anti-inflammatory action, may act differentially on activating GST/ depleting cellular GSH and inducing an antioxidant response. [1]
Schisandrin A and Schisandrin B inhibit CYP3A activity by a mixed noncompetitive and complete inhibition, with IC(50) values of 6.60 and 5.51 microM and K(i) values of 5.83 and 4.24 microM, respectively.[2]
Schisandrin A is an MDR-reversing agent in chemotherapy for osteosarcoma, the mechanism is associated with reducing the IC50 of DOX , and increasing cleaved-PARP and cleaved-Caspase-7 levels in MG-63 cells transfected with the MDR1 expression vector.[3]
Schisandrin A and B induce OATP1B1 expression and increase its transporter activity in HepG2 cells..[4]
Schisandrin A, B, and C have certain protective effects on the oxidative damage of HaCat cells induced by H2O2. [5]
References:
[1] Kuan L P, Shan W H, Chen J, et al. Plos One, 2016, 11(5).
[2] Li W L, Xin H W, Su M W, et al. Method Find in Exp Clin, 2010, 32(3):163-9.
[3] Xia Y Z, Yang L, Wang Z D, et al. Rsc Adv, 2015, 5(18):13972-84.
[4] Guo C X, Deng S, Yin J Y, et al. Pharmazie, 2015, 70(1):29-32.
[5] Wei H. Journal of Anhui Agricultural Sciences, 2013, 41(3):1047-9.
[6] Xu XM, Li J P, Yan C, et al. Journal of Northeast Agricultural University, 2007, 14(4):323-6.
HPLC of Schizandrol A
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
Schizandrol A, CAS number 7432-28-2, is a typical diterpene natural product isolated from the traditional Chinese medicinal herb Schisandra chinensis. Schisandra, as a widely used tonic herb in traditional Chinese medicine, has attracted attention for its multiple pharmacological effects, including regulating nervous system function, antioxidant properties, anti-inflammation, and liver protection. As one of its main active ingredients, Schisandra Alcohol A has been increasingly studied in recent years in neurological diseases, especially its sedative effects, showing good pharmacological activity and drug potential.
This review aims to systematically summarize the chemical structure and physicochemical properties of Schisandra Alcohol A, plant origins and extraction methods, with a focus on evaluating its pharmacological activity and mechanism of action. Combining druggability parameters and pharmacokinetic characteristics, it explores its clinical application prospects and development direction as a nervous system regulator, providing a theoretical basis and reference for subsequent basic research and drug development.
Schizandrol A has the molecular formula C_24H_32O_6 and a molecular weight of 432.5130, belonging to the pentacyclic diterpene compounds. Its structural features include a typical pentacyclic framework containing multiple hydroxyl and methoxy groups, giving it certain polarity and biological activity. Hydroxyl groups present in the molecular structure may participate in hydrogen bonding, affecting their ability to bind to biological targets.
In terms of physicochemical properties, the LogP value of Schisandra Alcohol A is 3.58, indicating moderate hydrophobicity, which facilitates cell membrane penetration and blood-brain barrier passage. Its topological pole surface area (TPSA) is 75.61 Ų, and moderate polarity facilitates interaction with target proteins. Low water solubility (0.0079 mg/mL) suggests that appropriate formulation modifications may be needed in vivo to enhance bioavailability. It is worth noting that Schisandra Alcohol A has good permeability to the blood-brain barrier, supporting its pharmacological effects in the central nervous system. The hERG channel inhibition test was negative, indicating a low risk of cardiotoxicity. The Ames mutagenic test was 0.0, indicating that this compound poses no significant genotoxicity risk.
Schisandra Alcohol A is mainly found in the fruit of Schisandra chinensis, a plant in the Schisandra family, distributed in Northeast China, North China, and the Korean Peninsula. Schisandra is named for its unique five flavors—sour, sweet, bitter, spicy, and salty—and has long been used in traditional Chinese medicine to tonify the kidneys and boost qi, astringe the lungs, and relieve cough.
Traditional methods for extracting schisandra alcohol methyl mostly use organic solvent extraction combined with liquid-liquid separation and column chromatography for separation and purification. Common solvents include ethanol, methanol, and ethyl acetate. Modern extraction technologies such as ultrasound-assisted extraction, microwave-assisted extraction, and high-performance liquid chromatography (HPLC) purification methods have improved extraction efficiency and purity. The specific steps usually include:
In recent years, the combination of mass spectrometry and nuclear magnetic resonance techniques has made structural identification and purity analysis of Schisandra Alcohol A increasingly precise, laying the foundation for pharmacological research and quality control.
Research on the pharmacological activity of Schisandol A mainly focuses on its central nervous system regulation, especially its sedative and anxiolytic effects. In addition, its antioxidant, anti-inflammatory, and liver-protective effects have also been gradually reported.
Multiple in vivo and in vitro experiments have shown that Schisandra Alcohol A has a significant sedative effect. In mouse models, schisandra alcohol A can prolong sleep duration induced by sodium pentobarbital, reduce excitatory behavior, and suggest its inhibitory effect on the central nervous system. This sedative effect is closely related to regulating the neurotransmitter system, especially the γ-aminobutyric acid (GABA) receptor system.
Schisandol A demonstrated anti-anxiety and antidepressant activities in behavioral models such as open-field experiments and forced swimming experiments. Its mechanism involves regulating the 5-hydroxytryptamine (5-HT) system, especially activation of the 5-HT1A receptor, to improve neurotransmitter imbalance.
Schisandol A has the ability to scavenge free radicals and suppress oxidative stress, reducing nerve cell damage and protecting brain tissue from oxidative damage, demonstrating potential neuroprotective effects.
Some studies report that Schisandra Alcohol A has anti-inflammatory effects, alleviating neuroinflammatory responses by inhibiting the release of inflammatory mediators. In addition, its protective effects on the liver have also been confirmed, possibly achieved by regulating hepatocyte metabolism and antioxidant pathways.
The sedative and neuromodulatory effects of Schisandra Alcohol A are mainly achieved through multi-target coordinated regulation, involving the regulation of neurotransmitter transporters and receptors.
GABA, as the main inhibitory neurotransmitter of the central nervous system, has receptor subtypes GABRA1, GABRB2, and GABRG2 as important targets of Schisandra Alcohol A. Research shows that schisandra alcohol methyl can enhance GABA receptor-mediated chloride channel activity, promote neuronal hyperpolarization, and exert sedative and anti-anxiety effects.
Schisandra Alcohol A binds to the 5-HT1A receptor (HTR1A), regulates neurotransmission of serotonin, and improves mood and behavioral abnormalities. This mechanism helps exert its antidepressant and anti-anxiety effects.
SLC6A4 (serotonin transporter) is a key protein regulating 5-HT levels. Schisandra Alcohol A may regulate SLC6A4 function, maintain neurotransmitter balance, and further regulate the excitation and inhibition states of the central nervous system.
In summary, Schisandra Alcohol A regulates the neurotransmitter system through the synergistic action of multiple targets and pathways, achieving sedative and neuroprotective effects.
Druggability evaluation of pentoschinol A shows it has good potential for drug development.
The molecular weight is 432.5130, which falls within the Lipinski rule range, and the LogP value is moderate at 3.58, indicating good membrane permeability. TPSA is 75.61 Ų, suitable for crossing the blood-brain barrier and matching the physicochemical characteristics of central nervous system drugs. Low water solubility suggests that dosage formulation optimization is needed to improve oral bioavailability.
Both experimental and computational predictions show that schisandra alcohol has high blood-brain barrier permeability, supporting its pharmacological activity in the central nervous system.
The hERG channel inhibition test was negative, indicating a low risk of cardiotoxicity. The Ames mutagenic test result was 0.0, indicating no obvious genotoxicity and good safety.
Currently, pharmacokinetic studies on schisandra alcohol alpha are limited. Preliminary data indicate good oral absorption, wide distribution in the body, and especially enrichment in brain tissue. Metabolic pathways may involve the hepatic cytochrome P450 enzyme system, with excretion mainly via bile and urine. Future studies are needed to systematically study its absorption, distribution, metabolism, and excretion (ADME) characteristics to provide a basis for clinical application.
With its remarkable sedating, anxiolytic, and neuroprotective effects, Schisandra Alcohol A shows broad clinical application prospects. As a central nervous system regulator, it is expected to be used to treat various neuropsychiatric disorders such as insomnia, anxiety, depression, and neurodegenerative disorders.
Currently, Schisandol A is still in basic research and early pharmacological evaluation stages, and has not yet entered large-scale clinical trials. Future research should focus on the following aspects:
Dosage form development and drug delivery route optimization: Developing new dosage forms such as nanoformulations and solid dispersions to improve bioavailability and in vivo stability based on their low water solubility.
Systematic pharmacokinetics and toxicology research: In-depth analysis of in vivo metabolic pathways, drug interactions, and long-term safety.
Preclinical and clinical research: Conduct multicenter, randomized controlled clinical trials to verify efficacy and safety, and clarify indications.
Deepening Mechanism Research: Using modern molecular biology and pharmacological techniques, further elucidating its multi-target mechanisms of action to guide precise drug administration.
Exploration of combined compound applications: Combining traditional Chinese medicine compound theory, the synergistic effects of Schisandra Alcohol A and other active ingredients are explored to enhance efficacy.
In summary, as a natural product with good druggability and multiple neuroprotective functions, Schisandra Alcohol A has the potential to become a novel central nervous system drug and warrants further research and development.
As an important active ingredient in Schisandra, Schisandra Alcohol A, due to its unique chemical structure and excellent physicochemical properties, demonstrates significant pharmacological activity in the central nervous system for sedation, anti-anxiety, and neuroprotection. Its mechanism of action involves multiple targets including GABA receptor, 5-HT1A receptor, and serotonin transporter, demonstrating the advantages of multi-target regulation by natural products. Druggability evaluations have shown good blood-brain barrier permeability and safety, laying a foundation for the development of central nervous system drugs.
In the future, with the advancement of pharmacokinetics, toxicology, and clinical research, Schisandra Alcohol A is expected to become a new drug for treating neuropsychiatric diseases. Its development not only enriches the research content of natural product pharmacology but also provides scientific support for the modernization of traditional Chinese medicine. Ongoing multidisciplinary collaboration and technological innovation will drive Schisandol A from the laboratory to clinical practice, benefiting a wide range of patients.
(Full text approximately 4,500 words)
