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| 5mg |
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| Other Sizes |
| Targets |
Hydrastinine targets several biological systems. It exerts a strong stimulating action on the uterus of all species studied, including humans, acting both directly on the smooth muscle and through its sympathetic innervation. As a result, hydrastinine and the closely related alkaloid cotarnine have been used as hemostatics, particularly in abnormal uterine conditions such as menorrhagia or postpartum hemorrhage. Hydrastinine also modulates major human liver microsomal cytochromes P450, particularly CYP2C9, CYP2D6, and CYP3A4/5, acting as a time-dependent inhibitor. It may also influence tyrosine hydroxylase activity and affect intracellular calcium levels, though these activities are better characterized for its parent compound hydrastine.
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| ln Vitro |
Goldenseal has been utilized to treat a broad range of illnesses, such as inflammation, urinary tract issues, and gastrointestinal issues. Goldenseal contains five main alkaloid constituents: canadine, hydroxystinine, palmatine, berberine, and hydrastine[1].
In vitro, hydrastinine has been shown to modulate cytochrome P450 enzyme activity, specifically CYP2C9, CYP2D6, and CYP3A4/5. Studies on goldenseal alkaloids have revealed that hydrastinine can inhibit these major drug-metabolizing enzymes, suggesting potential for herb-drug interactions. In uterine smooth muscle preparations from various species, including humans, hydrastinine induces contraction, which underlies its historical use as a uterotonic and hemostatic agent. In PC12 cells, hydrastine (a related alkaloid) inhibits tyrosine hydroxylase (IC50=20.7 microM) and reduces dopamine biosynthesis, effects that may also be partially shared by hydrastinine. Additionally, hydrastine decreases basal intracellular Ca2+ concentration in PC12 cells through L-type Ca2+ channels and caffeine-sensitive channels. The specific IC50 values for hydrastinine for these targets have not been extensively quantified. |
| ln Vivo |
In vivo, hydrastinine has been studied for its uterotonic and hemostatic effects in animal models and historically in humans. In non-pregnant animals, hydrastinine increases uterine tone and contractility, effects that are mediated both directly on smooth muscle and through sympathetic pathways. These effects were utilized historically to manage abnormal uterine bleeding (menorrhagia, postpartum hemorrhage). In terms of its pharmacokinetic and drug interaction potential, in vivo studies suggest that oral consumption of goldenseal (containing hydrastinine) can modulate CYP450 enzyme activity, although the specific contribution of hydrastinine versus other alkaloids is not fully delineated. Hydrastinine may also affect blood pressure and peripheral circulation due to its vasoconstrictor effects, but this has not been systematically studied.
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| Enzyme Assay |
A typical non-cellular (cell-free) protocol for evaluating hydrastinine's effect on cytochrome P450 enzymes uses human liver microsomes (HLMs). HLMs (0.5 mg/mL protein) are pre-incubated with various concentrations of hydrastinine (0.1-100 microM) in potassium phosphate buffer (100 mM, pH 7.4) containing MgCl2 (3.3 mM) and NADPH (1 mM) for 0-30 minutes at 37degC. After pre-incubation, isoform-specific probe substrates are added (e.g., diclofenac for CYP2C9, bufuralol for CYP2D6, midazolam for CYP3A4/5), and the reaction is continued for 10-30 minutes. The reaction is terminated by adding acetonitrile containing an internal standard. After centrifugation, the metabolites are analyzed by LC-MS/MS. The remaining enzyme activity is calculated relative to control incubations without hydrastinine. Time-dependent inhibition is assessed by comparing IC50 values with and without pre-incubation.
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| Cell Assay |
A typical in vitro cellular protocol for evaluating hydrastinine's effect on uterine contractility uses isolated rat or human uterine smooth muscle strips. Uterine tissue is obtained from female animals in the estrus phase or from surgical patients. The tissue is dissected, and longitudinal muscle strips (approximately 2×10 mm) are prepared and mounted in organ baths containing oxygenated Krebs-Ringer bicarbonate solution maintained at 37degC. After equilibration under 1-2 g tension for 60 minutes, the strips are exposed to increasing concentrations of hydrastinine (1-100 microM) in a cumulative manner. Contractile responses (amplitude and frequency) are recorded isometrically using force transducers. To determine the mechanism, the strips are pre-incubated with receptor antagonists (e.g., atropine for muscarinic receptors, propranolol for beta-adrenoceptors) before hydrastinine addition. A positive control (e.g., oxytocin or carbachol) is used to verify tissue responsiveness. The EC50 for hydrastinine-induced contraction is calculated from the concentration-response curve.
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| Animal Protocol |
An in vivo animal protocol for evaluating the uterotonic effects of hydrastinine uses female Sprague-Dawley rats (200-250 g) in the estrus phase. Rats are anesthetized with urethane (1.5 g/kg, ip). A midline laparotomy is performed to expose the uterus, and a catheter is inserted into the jugular vein for drug administration. A force transducer is attached to the uterine horn to measure intrauterine pressure or isometric tension. After a stabilization period of 30 minutes, hydrastinine is administered intravenously at incremental doses (0.1, 0.3, 1, 3, 10 mg/kg). Uterine contractions (amplitude, frequency, and baseline tone) are recorded continuously for 30-60 minutes post-dose. Separate groups receive vehicle (saline) or positive control (oxytocin, 0.01-1 IU/kg). To evaluate hemostatic effects, a separate cohort of animals is used to measure blood loss in a uterine incision model: after hydrastinine administration, a standardized uterine incision is made, and the amount of blood loss is measured gravimetrically over 10 minutes.
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| ADME/Pharmacokinetics |
Limited pharmacokinetic data are available for hydrastinine as a pure compound. Historically, hydrastinine has been administered intravenously or orally for its hemostatic effects. Based on historical reports and studies on goldenseal extracts (which contain hydrastinine and other alkaloids), the oral bioavailability of hydrastinine is likely moderate. As a small-molecule alkaloid, it is expected to be absorbed from the gastrointestinal tract, but may undergo first-pass metabolism. Hydrastinine is known to interact with cytochrome P450 enzymes, particularly CYP2C9, CYP2D6, and CYP3A4/5, as an inhibitor. This suggests that it may have the potential to alter the metabolism of co-administered drugs. The compound has a plasma half-life that is likely short (hours), based on the duration of its pharmacological effects. Comprehensive PK studies have not been published.
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| Toxicity/Toxicokinetics |
Toxicity data for hydrastinine are limited. Historically, hydrastinine has been used in low doses as a hemostatic agent and was generally considered safe at therapeutic doses. However, high doses may cause uterine hyperstimulation, which could lead to uterine rupture or fetal distress, particularly in pregnant women. Other potential adverse effects include nausea, vomiting, diarrhea, and central nervous system effects. As a modulator of cytochrome P450 enzymes, there is a theoretical risk of herb-drug interactions when taken with medications metabolized by CYP2C9, CYP2D6, or CYP3A4/5 (e.g., warfarin, antidepressants, statins). Standard laboratory safety precautions should be followed when handling hydrastinine. It is for research use only and is not approved for clinical use in humans. The compound should be stored at -20degC, protected from light.
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| References | |
| Additional Infomation |
Reports indicate that myricetin has been found in Canadian Coptis chinensis, rhododendron, and Celandine maize, and relevant data is available for reference.
Hydrastinine (CAS 6592-85-4) is a naturally occurring alkaloid derived from the hydrolysis of hydrastine. It has the molecular formula C11H13NO3 and a molecular weight of 207.23. Historically, hydrastinine and cotarnine have been used as hemostatic agents, particularly in the management of abnormal uterine bleeding (menorrhagia, postpartum hemorrhage). The compound exerts a strong stimulating action on the uterus, increasing uterine tone and contractility, which helps reduce bleeding. Hydrastinine also modulates major human liver cytochrome P450 enzymes (CYP2C9, CYP2D6, CYP3A4/5), indicating potential for herb-drug interactions. It is a minor alkaloid component of goldenseal (Hydrastis canadensis). As of 2026, hydrastinine is not an FDA-approved drug and is available primarily as a research chemical. It is not intended for human use without appropriate regulatory approval. |
| Molecular Formula |
C11H13NO3
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|---|---|
| Molecular Weight |
207.23
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| Exact Mass |
207.09
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| Elemental Analysis |
C, 63.76; H, 6.32; N, 6.76; O, 23.16
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| CAS # |
6592-85-4
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| Related CAS # |
Hydrastinine hydrochloride; 4884-68-8
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| PubChem CID |
3638
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| Appearance |
Off-white to light brown solid powder
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| Density |
1.332g/cm3
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| Boiling Point |
342.5ºC at 760 mmHg
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| Flash Point |
161ºC
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| Index of Refraction |
1.617
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| LogP |
0.832
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
15
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| Complexity |
248
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN1CCc2cc3c(cc2C1O)OCO3
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| InChi Key |
YOJQZPVUNUQTDF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H13NO3/c1-12-3-2-7-4-9-10(15-6-14-9)5-8(7)11(12)13/h4-5,11,13H,2-3,6H2,1H3
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| Chemical Name |
6-methyl-7,8-dihydro-5H-[1,3]dioxolo[4,5-g]isoquinolin-5-ol
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| Synonyms |
Hydraztinine; Hydrastinine
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 250 mg/mL (1206.39 mM)
H2O: 16.67 mg/mL (80.44 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (10.04 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (10.04 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (10.04 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.8256 mL | 24.1278 mL | 48.2556 mL | |
| 5 mM | 0.9651 mL | 4.8256 mL | 9.6511 mL | |
| 10 mM | 0.4826 mL | 2.4128 mL | 4.8256 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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