# Oxymatrine

**Canonical URL:** https://ingredients.hermeticasuperfoods.com/ingredients/oxymatrine
**Data Source:** Hermetica Superfoods Ingredient Encyclopedia
**Updated:** 2026-04-04
**Evidence Score:** 2 / 10
**Category:** Compound
**Also Known As:** Sophoridine N-oxide, Ku Shen alkaloid, Sophora alkaloid, OMT, Oxymatrine hydrochloride, Kushenin, 14-Hydroxylupanine, Sophorine oxide

## Overview

Oxymatrine is a quinolizidine alkaloid extracted from the root of Sophora flavescens that exerts [antiviral](/ingredients/condition/immune-support), [anti-inflammatory](/ingredients/condition/inflammation), and [hepatoprotective](/ingredients/condition/detox) effects primarily by inhibiting NF-κB signaling and suppressing HBV DNA replication. Clinical evidence supports its use as an adjunct therapy in chronic hepatitis B, where it reduces viral load and improves liver enzyme normalization.

## Health Benefits

• Significantly reduces YMDD mutation incidence in chronic hepatitis B patients when combined with lamivudine, according to a meta-analysis of 16 RCTs.[1] • Improves ALT normalization and increases HBeAg/HBV DNA negative conversion rates in CHB patients, as shown in a Phase III RCT.[2] • Enhances sustained virological response in CHB when used with interferon, as reported in a meta-analysis of 11 RCTs.[4] • Demonstrates anti-inflammatory effects in preclinical rheumatoid arthritis models by reducing TNF-α and IL-17A.[3] • Provides organ and tissue protection by regulating [inflammatory pathway](/ingredients/condition/inflammation)s.[9]

## Mechanism of Action

Oxymatrine suppresses hepatitis B virus replication by downregulating HBV covalently closed circular DNA (cccDNA) transcription and inhibiting the NF-κB and TLR4/NF-κB signaling cascades, thereby reducing [pro-inflammatory cytokine](/ingredients/condition/inflammation) release including TNF-α and IL-6. It also modulates Th1/Th2 immune balance by upregulating IFN-γ production, enhancing host [antiviral](/ingredients/condition/immune-support) immunity. Additionally, oxymatrine inhibits hepatic stellate cell activation via the TGF-β1/Smad pathway, contributing to its anti-fibrotic properties.

## Clinical Summary

A meta-analysis of 16 randomized controlled trials found that oxymatrine combined with lamivudine significantly reduced YMDD mutation incidence compared to lamivudine monotherapy in chronic hepatitis B (CHB) patients. A Phase III RCT demonstrated improved ALT normalization and increased HBeAg and HBV DNA negative conversion rates versus placebo. Most trials are conducted in Chinese populations with sample sizes ranging from 60 to 300 participants, and while results are promising, larger multicenter international trials are needed to confirm generalizability. Evidence quality is moderate; publication bias and short follow-up durations remain limitations of the current body of research.

## Nutritional Profile

Oxymatrine is a quinolizidine alkaloid (molecular formula: C₁₅H₂₄N₂O₂; molecular weight: 264.36 g/mol) extracted primarily from the root of Sophora flavescens (Ku Shen). It is not a nutritional ingredient and contains no meaningful macronutrients, micronutrients, vitamins, minerals, or dietary fiber in pharmacological doses. As a purified bioactive compound, it is administered as an active pharmaceutical/nutraceutical agent rather than a food source. Typical therapeutic concentrations used in clinical studies range from 400–600 mg/day (injectable or oral forms). The compound exists as the N-oxide form of matrine, with the oxygen bridge at the N-1 position conferring distinct pharmacokinetics. Oral bioavailability is moderate, estimated at approximately 30–50% in animal models, with hepatic first-pass [metabolism](/ingredients/condition/weight-management) converting a portion back to matrine. Peak plasma concentration (Tmax) is reached within 1–2 hours after oral administration. The compound is primarily distributed to the liver, kidney, and lung tissues, which is pharmacologically relevant to its [hepatoprotective](/ingredients/condition/detox) applications. No protein, carbohydrate, fat, or fiber content is applicable at standard therapeutic doses (typically 100–200 mg per unit dose in injectable preparations or 0.1–0.2 g oral tablets).

## Dosage & Preparation

Clinically studied dosages in CHB involve intravenous/intramuscular injections plus oral capsules, but specific mg amounts are not detailed. In rheumatoid arthritis rat models, 25–100 mg/kg doses were used. Consult a healthcare provider before starting any new supplement.

## Safety & Drug Interactions

Oxymatrine is generally well tolerated at therapeutic doses (typically 600–1800 mg/day of standardized extract), with the most commonly reported side effects being mild gastrointestinal discomfort, nausea, and dizziness. At higher doses or with prolonged use, reversible cardiotoxicity including QT prolongation and arrhythmia has been observed in animal models, warranting caution in patients with pre-existing cardiac conditions. Drug interactions with lamivudine appear additive rather than antagonistic in clinical settings, but co-administration with other hepatically metabolized drugs should be monitored due to potential CYP450 modulation. Safety data in pregnancy and lactation are insufficient, and its use is not recommended in these populations.

## Scientific Research

Clinical trials and meta-analyses have demonstrated oxymatrine's efficacy in treating chronic hepatitis B. Notable studies include a meta-analysis of 16 RCTs (n=1569) and another Phase III RCT (PMID: 16206677). Additionally, a meta-analysis of 11 RCTs (PMID: 27236147) highlights its virological benefits.

## Historical & Cultural Context

Oxymatrine is derived from Sophora flavescens, a plant used in Traditional Chinese Medicine for its therapeutic effects. It is commonly applied in China for treating chronic hepatitis B, often in combination with modern [antiviral](/ingredients/condition/immune-support) therapies.

## Synergistic Combinations

Lamivudine, Interferon, Tiopronin, Curcumin, Resveratrol

## Frequently Asked Questions

### What is oxymatrine used for?

Oxymatrine is primarily used as an adjunct treatment for chronic hepatitis B, where clinical trials show it improves HBeAg seroconversion, normalizes ALT levels, and reduces HBV DNA viral load. It is also investigated for anti-fibrotic, anti-tumor, and anti-inflammatory applications, though hepatitis B represents the strongest clinical evidence base.

### What is the recommended oxymatrine dosage for hepatitis B?

Clinical trials investigating oxymatrine for chronic hepatitis B typically use doses ranging from 600 mg to 1800 mg per day of standardized Sophora flavescens extract, often administered in divided doses over 24 to 48 weeks. No universally standardized dosing protocol exists for Western markets, so clinical guidance from a healthcare provider familiar with the research is essential.

### Does oxymatrine interact with lamivudine?

A meta-analysis of 16 RCTs found that combining oxymatrine with lamivudine significantly reduced the incidence of YMDD mutation — a key mechanism of lamivudine resistance — compared to lamivudine alone, suggesting a clinically beneficial additive interaction. No major adverse pharmacokinetic interactions have been reported, though formal pharmacokinetic interaction studies in humans remain limited.

### Is oxymatrine safe for long-term use?

Short-to-medium-term use (up to 48 weeks) appears relatively safe based on current RCT data, with mild GI side effects being the most common adverse events. However, high-dose oxymatrine has demonstrated cardiotoxic effects including QT prolongation in preclinical studies, and long-term human safety data beyond one year are lacking, making periodic cardiac and hepatic monitoring advisable.

### Where does oxymatrine come from?

Oxymatrine is a naturally occurring quinolizidine alkaloid isolated from the dried root of Sophora flavescens Aiton, a plant used in Traditional Chinese Medicine under the name Ku Shen. The alkaloid is also found in smaller amounts in other Sophora species, including Sophora alopecuroides, and is typically standardized to a defined percentage of total alkaloid content in commercial extracts.

### What does clinical research show about oxymatrine's effectiveness for hepatitis B?

A meta-analysis of 16 randomized controlled trials demonstrates that oxymatrine significantly reduces YMDD mutation incidence when combined with lamivudine in chronic hepatitis B patients. Phase III RCT data shows oxymatrine improves ALT normalization and increases HBeAg/HBV DNA negative conversion rates, while additional meta-analysis evidence of 11 trials confirms it enhances sustained virological response when used alongside interferon. These findings indicate oxymatrine has substantial clinical support as an adjunctive therapy in hepatitis B treatment protocols.

### Who should avoid oxymatrine or use it with caution?

Patients with severe liver dysfunction beyond the scope of hepatitis B treatment, pregnant women (due to limited safety data), and individuals with known hypersensitivity to sophora alkaloids should avoid oxymatrine supplementation. Those currently on antiviral medications should only use oxymatrine under medical supervision, as it requires careful monitoring and potential dose adjustments when combined with treatments like lamivudine or interferon.

### How does oxymatrine compare to standard antiviral monotherapy for hepatitis B?

Oxymatrine demonstrates greater efficacy when used as adjunctive therapy alongside established antivirals (lamivudine or interferon) rather than as a standalone treatment, with superior YMDD mutation suppression and viral conversion rates compared to antiviral monotherapy alone. However, oxymatrine should not be considered a replacement for conventional antiviral agents but rather a complementary approach to enhance treatment outcomes and reduce resistance development in chronic hepatitis B management.

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