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Product name: Catalpol
Synonym name: Catalpinoside
Catalogue No.: BP0321
Cas No.: 2415-24-9
Formula: C15H22O10
Mol Weight: 362.331
Botanical Source: Plantago lanceolata, Buddleia globosa, Buddleia variabilis and Lagotis brevituba
Physical Description: Powder
Type of Compound: Iridoids
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:
Catalpol, an iridoid glucoside, has been reported to inhibit apoptosis of neuron and endothelial cells; the pretreatment of H9c2 cells with catalpol can be against H 2 O 2 -induced apoptosis, and the protective effect of catalpol involves the mitochondrial-dependent caspase pathway and is associated with increased Bcl-2 and decreased Bax expression.[1]
Catalpol has the neuroprotective effects of in lipopolysaccharide (LPS)-induced inflammatory models, it can prevent mesencephalic neuron death and ameliorate cognitive ability animals; catalpol can exert inhibitory effects on the inflammatory reaction in astrocytes and that inactivation of NF-κB could be the major determinant for its anti-inflammatory mechanism, therefore, it may potentially be a highly effective therapeutic agent in treating neurodegenerative diseases associated with inflammation.[2]
Catalpol exerts the most significant cytoprotective effect on astrocytes by suppressing the production of free radicals and elevating antioxidant capacity.[3]
Catalpol can increase presynaptic proteins and up-regulate relative signaling molecules in the hippocampus of the aged rats, it seems to indicate that catalpol might ameliorate age-related neuroplasticity loss by “normalizing” presynaptic proteins and their relative signaling pathways in the aged rats.[4]
References:
[1] Hu L A, Sun Y K, Zhang H S, et al. Bioscience Reports, 2016,36(3).
[2] Bi J, Jiang B, Zorn A, et al. Toxicol in Vitro, 2013, 27(2):543-50.
[3] Li Y, Bao Y, Bo J, et al. Int J Dev Neurosci, 2008, 26(3–4):309-17.
[4] Liu J, He Q J, Zou W, et al. Brain Res, 2006, 1123(1):68-79.
[5] Sun L L, Ren Y H, Chen H L, et al. China Pharmacy, 2013(04):374-5.
HPLC of Catalpol
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
189.9000
-2.5000
-2.5000
Low
No
No
No
No
No
No
Catalpol (CAS number 2415-24-9) is an active ingredient mainly found in the Rehmannia glutinosa plant, belonging to the iris glycoside class. As a typical monosaccharide, zichul has attracted significant attention in traditional Chinese medicine due to its remarkable pharmacological activity. In recent years, with the deepening development of natural product pharmacology, zichul has been widely studied for its multi-target and multi-pathway biological activity, especially showing promising application potential in neuroprotection, antidiabetic, anti-inflammatory, antioxidant, anticancer, and anti-hepatitis B virus (HBV) areas. This paper systematically reviews the chemical structure and physicochemical properties of azinol, plant origin and extraction methods, pharmacological activity, mechanism of action, druggability evaluation, and clinical application prospects, aiming to provide theoretical basis and research directions for the in-depth development and utilization of this natural product.
The chemical name of catalpinoside is Catalpinoside, with the molecular formula C15H22O10 and a molecular weight of 362.33. Its structural feature is that a cyclic monosaccharide partially connects to a terpenoid skeleton, making it a typical iris glycoside compound. The LogP value of azitrinol is about -2.5, indicating strong hydrophilicity and good water solubility. Its topological polar surface area (TPSA) reaches 189.9 Ų, and the number of hydrogen bond acceptors reaches 10, indicating that the molecule has strong polarity and a large number of hydrogen bond donors/acceptors, which may affect membrane permeability and bioavailability.
In terms of physicochemical properties, azinol has high polarity and good water solubility, but its blood-brain barrier penetration ability (BBB has low permeability), suggesting its direct role in the central nervous system is limited. Additionally, zifenol showed no significant hepatotoxicity, cardiotoxicity, or hERG channel inhibition, and the Ames mutagenic test was negative, indicating good safety and a solid druggability.
Zichun is mainly distributed in Rehmannia glutinosa plants, especially the roots of Rehmannia glutinosa. Prepared Rehmannia is a traditional Chinese medicinal herb, widely used for nourishing yin and blood, regulating endocrine function, and anti-inflammatory effects. As one of its main active ingredients, the content of azitol varies depending on the plant's growth stage and processing method.
In terms of extraction methods, the commonly used water extraction and alcohol precipitation method is to extract from the dried roots of prepared Rehmannia. The specific steps include: crushing dried Rehmannia glutinosa, refluxing with water or 70% ethanol for extraction, concentrating the filtrate, adding ethanol to precipitate impurities, and then purifying it through multiple column chromatography (such as silica gel columns, reversed-phase C18 columns) to obtain high-purity cathanol. In recent years, purification technologies combining ultrasound-assisted extraction, microwave-assisted extraction, and high-performance liquid chromatography (HPLC) have been applied to improve extraction efficiency and purity.
Zijunol demonstrates significant neuroprotective effects in various neurodegenerative disease models. Both in vitro and in vivo studies show that catalpa alcohol can reduce oxidative stress in nerve cells, inhibit neuroinflammatory responses, and promote nerve regeneration. Its mechanism involves regulating apoptosis-related signaling pathways, inhibiting the release of inflammatory factors, and enhancing antioxidant enzyme activity. For example, in a Parkinson's disease model, cathol reduces dopaminergic neuron damage by inhibiting reactive oxygen species (ROS) production and modulating mitochondrial function.
Research on zichun in the anti-diabetes field is particularly in-depth. By activating the AMPK pathway, it enhances insulin sensitivity, promotes glucose uptake and metabolism, and lowers blood sugar levels. Additionally, azolin can inhibit DPP4 activity, prolonging the half-life of GLP-1 and thereby promoting insulin secretion. Its regulatory effect on SGLT2 also helps increase urinary glucose excretion, improving diabetes symptoms. Multiple animal studies have shown that zisol significantly reduces fasting blood glucose and glycated hemoglobin levels in diabetic rats, while also improving the function of islet β cells.
Zijunol can significantly inhibit the expression of inflammatory mediators such as TNF-α, IL-1β, and IL-6, reducing inflammatory responses. Its antioxidant effects mainly work by scavenging free radicals and increasing the activity of antioxidant enzymes such as superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px). Such actions give zijin the potential therapeutic value of various inflammatory disease models.
Zi alcohol exhibits effects on various tumor cell lines by inhibiting proliferation, inducing apoptosis, and blocking the cell cycle. Its anticancer mechanism involves regulating signaling pathways such as PI3K/AKT, MAPK, and NF-κB, inhibiting tumor cell migration and invasion capabilities. Some studies have also found that caterol can enhance the sensitivity of chemotherapy drugs and has potential adjunctive therapeutic effects.
The antispasmodic effects of zijin in neurological diseases have also been reported, possibly related to its regulation of neurotransmitter release and neuronal excitability. Animal experiments have shown that ziol can prolong the latency period of seizures and reduce their intensity.
Zijin inhibits HBV replication and can reduce the expression of HBV DNA and related antigens. Its antiviral mechanism may involve modulating host immune responses and directly inhibiting viral replicase activity, providing new natural drug candidates for hepatitis B treatment.
The multiple pharmacological effects of zichul are attributed to its regulation of various molecular targets, with particular performance in its antidiabetic effects. The main targets include:
AMPK (PRKAA1): As a cellular energy sensor, AMPK activation promotes glucose uptake and lipid metabolism; azolol improves metabolic disorders by activating the AMPK pathway.
SGLT2 (Sodium-Glucose Co-Transporter 2): Ziol inhibits SGLT2, reduces renal glucose reabsorption, promotes urinary glucose excretion, and lowers blood sugar.
GCK (Glucose Kinase): Zybol promotes GCK activity, enhancing the utilization of glucose by liver and islet cells.
PPARG (Peroxisome Proliferator-Activated Receptor γ): Regulates lipid metabolism and insulin sensitivity; Zijin improves insulin resistance by activating PPARG.
AKT1: Involved in insulin signaling, aziol activates AKT1 to promote glucose transport and metabolism.
DPP4 (peptidyl dipeptidase 4): Zi alcohol inhibits DPP4 activity, prolongs the action of glucagon-like peptide-1 (GLP-1), and enhances insulin secretion.
IRS1 (insulin receptor substrate 1): Ziol promotes IRS1 phosphorylation and enhances insulin signaling.
SLC2A4 (GLUT4): Zisol promotes the transport of GLUT4 to cell membranes, increasing glucose uptake.
PIK3R1 (phospholipidyl-inositol 3-kinase regulatory subunit): Involved in insulin signaling pathways, zidanol regulates PI3K activity and promotes glucose metabolism.
Additionally, azinol exerts anti-inflammatory and antioxidant effects by regulating signaling pathways such as NF-κB and MAPK. In terms of neuroprotection, catinol regulates the expression of apoptosis-related proteins (such as Bcl-2, Caspase-3), reducing nerve cell damage.
Druggability evaluations of zisol indicate good safety and a low risk of toxic side effects. Its molecular weight is moderate and water solubility is good, but its low LogP value suggests insufficient lipid solubility, which may limit oral absorption and cell membrane penetration. High TPSA and a high number of hydrogen bond receptors may further affect its bioavailability.
The low permeability of the blood-brain barrier limits its direct application in central nervous system diseases, but its intrabrain distribution is expected to improve through structural modification or nanocarrier technology. In vivo pharmacokinetic studies show that zinitol is absorbed quickly after oral administration, but its bioavailability is limited, mainly metabolized and excreted by the liver, with no significant hepatotoxicity or cardiotoxicity observed.
Modern pharmaceutical technologies, such as liposomes, nanoparticles, and solid dispersions, are expected to improve the solubility and bioavailability of aziol, promoting its clinical translation.
As a multi-target natural active ingredient, Zichul possesses broad pharmacological activity and good safety, showing potential as a new natural medicine. It is particularly outstanding in the prevention and treatment of diabetes and its complications, and in the future may be used as an adjunct therapy or in combination with existing drugs. In addition, the potential of zidulin in neurodegenerative diseases, tumors, and chronic inflammatory diseases is also worth further exploration.
Future research should focus on:
Zichuol, a natural product of iris glycosides derived from plants of the genus Rehmannia, demonstrates broad research and application prospects due to its diverse pharmacological activities and good safety profile. Its potential in anti-diabetic, neuroprotective, anti-inflammatory, antioxidant, and anti-cancer fields has been confirmed by extensive basic research. In the future, with advances in pharmaceutics technology and deepening clinical research, zijunol is expected to become an important candidate for natural drug development, providing new strategies and options for the treatment of related diseases. Ongoing multidisciplinary collaboration and innovative research will drive zichul from the laboratory to clinical practice, realizing its value in modern medicine.
Shenshuai
Wenjing
Hedandan
