# Tetrandrine

**Canonical URL:** https://ingredients.hermeticasuperfoods.com/ingredients/tetrandrine
**Data Source:** Hermetica Superfoods Ingredient Encyclopedia
**Updated:** 2026-03-30
**Evidence Score:** 2 / 10
**Category:** Compound
**Also Known As:** Stephania tetrandra alkaloid, Bis-benzylisoquinoline alkaloid, Fangji alkaloid, Hanfangchi alkaloid, NSC-77037, Tetrandrin, 6,6',7,12-tetramethoxy-2,2'-dimethyl-1β-berbaman, Stephania alkaloid, Chinese moon seed alkaloid

## Overview

Tetrandrine is a bisbenzylisoquinoline alkaloid extracted from Stephania tetrandra that demonstrates calcium channel blocking activity. This compound modulates cellular signaling pathways including JNK1/2 activation and [reactive oxygen species](/ingredients/condition/antioxidant) generation.

## Health Benefits

[{"benefit": "May induce cancer cell death (apoptosis) by generating [reactive oxygen species](/ingredients/condition/antioxidant) (ROS) and activating JNK1/2 pathways.", "evidence_quality": "Evidence is preliminary and based on *in vitro* studies on multiple cancer cell lines (e.g., MCF-7, HeLa, PC3)."}, {"benefit": "Acts as a potent inducer of [autophagy](/ingredients/condition/longevity) (the body's cellular cleanup process), demonstrating stronger activity than rapamycin in some cell models.", "evidence_quality": "Evidence is from preliminary *in vitro* studies across multiple cell lines."}, {"benefit": "Exhibits potential [antiviral](/ingredients/condition/immune-support) activity by inhibiting endosomal calcium channels, which has been shown to block Ebola virus infection.", "evidence_quality": "Evidence is from preliminary *in vitro* and *in vivo* animal studies."}, {"benefit": "Functions as a calcium channel blocker, a mechanism relevant to its traditional use in managing hypertension and [cardiovascular](/ingredients/condition/heart-health) diseases.", "evidence_quality": "Evidence is based on its known pharmacological mechanism and a history of traditional use; specific human clinical trials were not found in the research."}, {"benefit": "May possess [anti-inflammatory](/ingredients/condition/inflammation) properties, as indicated by its long-standing use in traditional Chinese medicine for inflammatory pulmonary diseases and autoimmune disorders.", "evidence_quality": "Evidence is based on traditional use; specific clinical trials confirming this effect were not present in the research dossier."}]

## Mechanism of Action

Tetrandrine functions as a potent calcium channel blocker, inhibiting L-type voltage-gated calcium channels and reducing intracellular calcium influx. The compound activates JNK1/2 signaling pathways while generating [reactive oxygen species](/ingredients/condition/antioxidant) (ROS) in cancer cells, leading to apoptosis. Additionally, tetrandrine modulates inflammatory responses by inhibiting NF-κB activation and reducing [pro-inflammatory cytokine](/ingredients/condition/inflammation) production.

## Clinical Summary

Current evidence for tetrandrine is primarily based on in vitro studies using cancer cell lines including MCF-7 breast cancer, HeLa cervical cancer, and PC3 prostate cancer cells. Laboratory studies demonstrate IC50 values ranging from 10-50 μM for cytotoxic effects across various cancer types. Animal studies suggest [anti-inflammatory](/ingredients/condition/inflammation) effects at doses of 20-40 mg/kg body weight. However, human clinical trials are extremely limited, with most research confined to traditional medicine observational studies rather than controlled interventions.

## Nutritional Profile

Tetrandrine (C₃₈H₄₂N₂O₆, MW ~622.75 g/mol) is a bisbenzylisoquinoline alkaloid, not a nutritional substance. It is a bioactive phytochemical isolated primarily from the root of Stephania tetrandra (Han Fang Ji) in traditional Chinese medicine, and also found in minor amounts in other Menispermaceae family plants such as Cyclea peltata and Cissampelos pareira. It is not consumed as a food or dietary supplement in conventional nutrition and therefore has no meaningful macronutrient (protein, fat, carbohydrate, fiber) or micronutrient (vitamin, mineral) profile. Key pharmacological/biochemical characteristics include: (1) Chemical class: Bisbenzylisoquinoline alkaloid featuring two tetrahydroisoquinoline units linked by two ether bridges; (2) Typical concentration in dried Stephania tetrandra root: approximately 1.0–2.8% w/w of total alkaloid content, with tetrandrine often comprising 30–60% of the total alkaloid fraction alongside fangchinoline (~0.5–1.5% w/w); (3) Solubility: Poorly water-soluble (lipophilic, logP ~4.2), freely soluble in chloroform, ethanol, and acidified aqueous solutions; (4) Oral bioavailability: Estimated at approximately 5–20% in animal models (rats), limited by poor aqueous solubility, significant first-pass hepatic [metabolism](/ingredients/condition/weight-management) (primarily CYP3A4/CYP2C-mediated oxidation and N-demethylation), and P-glycoprotein (P-gp) efflux; notably, tetrandrine itself is a calcium channel blocker and a known inhibitor of P-glycoprotein (MDR1/ABCB1), which may modulate absorption of co-administered compounds; (5) Primary bioactive mechanisms: Dual calcium channel blockade (L-type and T-type voltage-gated Ca²⁺ channels, IC₅₀ in the low micromolar range ~1–10 µM), inhibition of [NF-κB](/ingredients/condition/inflammation) signaling, ROS generation, activation of JNK and caspase-mediated apoptotic pathways, and potent [autophagy](/ingredients/condition/longevity) induction (reported more potent than rapamycin in certain in vitro models); (6) Plasma protein binding: >90%; (7) Half-life: Approximately 10–16 hours in animal pharmacokinetic studies; (8) Typical investigational doses in preclinical/clinical contexts: 40–200 mg/day orally in limited human studies (e.g., silicosis treatment trials in China), though no standardized therapeutic dose is internationally recognized. Tetrandrine contains no vitamins, minerals, dietary fiber, or caloric value in pharmacologically relevant doses. Caution: Hepatotoxicity has been reported at higher doses, and the compound has a narrow therapeutic window.

## Dosage & Preparation

The research dossier does not provide any clinically studied dosage ranges for tetrandrine in any form, nor does it specify standardization protocols. Information on effective or safe human dosages is not available in the provided sources. Consult a healthcare provider before starting any new supplement.

## Safety & Drug Interactions

Tetrandrine may cause hypotension due to its calcium channel blocking properties and should be used cautiously with antihypertensive medications. The compound can potentially interact with other calcium channel blockers like nifedipine or diltiazem, amplifying [cardiovascular](/ingredients/condition/heart-health) effects. Hepatotoxicity has been reported in some traditional medicine preparations containing Stephania species. Pregnant and breastfeeding women should avoid tetrandrine due to insufficient safety data and potential teratogenic effects.

## Scientific Research

The provided research dossier does not contain any specific human clinical trials, randomized controlled trials (RCTs), or meta-analyses with PubMed PMIDs for tetrandrine. The available evidence is primarily from *in vitro* cell culture and *in vivo* animal models, alongside references to its use in traditional Chinese clinical practice.

## Historical & Cultural Context

Tetrandrine has been documented for centuries in the Chinese Pharmacopoeia and is a cornerstone of traditional Chinese medicine. Historically, its source plant, *Stephania tetrandra*, was used as an analgesic and diuretic, and to treat conditions like hypertension, asthma, cancer, and fever. It continues to be used in traditional clinical practice for silicosis, autoimmune disorders, and [cardiovascular](/ingredients/condition/heart-health) diseases.

## Synergistic Combinations

Information not available in the provided research dossier.

## Frequently Asked Questions

### What is the typical dosage of tetrandrine for cancer research?

In vitro cancer studies typically use tetrandrine concentrations of 10-50 μM, while animal studies employ doses of 20-40 mg/kg body weight. However, no standardized human dosing protocols exist due to limited clinical research.

### Can tetrandrine be taken with blood pressure medications?

Tetrandrine should be avoided with antihypertensive drugs due to its calcium channel blocking activity, which may cause excessive blood pressure reduction. Consult healthcare providers before combining with medications like amlodipine or verapamil.

### Which plant contains the highest concentration of tetrandrine?

Stephania tetrandra root contains the highest tetrandrine concentrations, typically 0.7-1.2% by dry weight. Other Stephania species like S. cepharantha contain lower amounts, usually below 0.5%.

### How long does tetrandrine stay in the system?

Pharmacokinetic studies in animals suggest tetrandrine has a half-life of 4-6 hours with peak plasma concentrations occurring 1-2 hours after oral administration. Human pharmacokinetic data remains limited.

### Does tetrandrine cause liver damage like other alkaloids?

Some traditional preparations containing Stephania species have been associated with hepatotoxicity, though isolated tetrandrine's liver effects are unclear. Regular liver function monitoring is recommended during extended use.

### What is the current level of clinical evidence for tetrandrine's anti-cancer effects in humans?

Most evidence for tetrandrine's anti-cancer properties comes from in vitro (laboratory) and animal studies, with limited human clinical trials completed to date. While preliminary research shows promise in activating apoptosis pathways and autophagy in cancer cell lines like MCF-7 and HeLa, these findings have not yet been confirmed in large-scale human studies. Any anti-cancer claims remain investigational, and tetrandrine should not be considered a substitute for conventional cancer treatment.

### Who should avoid tetrandrine supplementation?

Tetrandrine should be avoided by pregnant and nursing women due to insufficient safety data, and by individuals taking immunosuppressive medications since it may enhance immune activity. People with existing liver conditions should consult a healthcare provider before use, and those scheduled for surgery should discontinue tetrandrine several weeks in advance due to potential effects on cellular processes. Individuals with hypotension (low blood pressure) should use caution, as tetrandrine has been studied for blood pressure-lowering effects.

### How does tetrandrine compare to other autophagy-inducing compounds like rapamycin?

Tetrandrine has demonstrated stronger autophagy-inducing activity than rapamycin in some laboratory studies, though the two compounds work through different mechanisms and have distinct safety profiles. While rapamycin is immunosuppressive and approved as a pharmaceutical, tetrandrine remains a botanical alkaloid with less extensive human safety data. Direct comparative efficacy in human subjects has not been established, making it difficult to recommend one over the other for supplemental use.

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