Stephania Tetrandra Extract
Also known as: Han Fang Ji, Stephania root, Stephania tetrandra extract, Stephania tetrandra S. Moore
Overview
Stephania tetrandra is a perennial climbing plant native to China, traditionally used in Traditional Chinese Medicine (TCM) for its anti-inflammatory and analgesic properties. The extract, typically derived from its root, is rich in bioactive alkaloids such as tetrandrine, fangchinoline, cepharanthine, and coclaurine. These compounds are responsible for its observed anti-inflammatory, immunomodulatory, antiviral, and anticancer effects. Primary research areas include its potential in treating rheumatoid arthritis, as an adjunct in cancer therapy, and for antiviral applications. While promising, most evidence is from preclinical studies, with limited large-scale human clinical trials.
Benefits
Stephania tetrandra extract exhibits several evidence-based benefits, primarily driven by its alkaloid content. Its anti-inflammatory properties are well-documented, with studies showing reduction of inflammatory cytokines (TNF-α, IL-6) and nitric oxide in macrophage models, and significant efficacy in animal models of rheumatoid arthritis by inhibiting the PI3K/Akt signaling pathway. For instance, a 28-day treatment with 1.35 g/kg extract in a rat model of rheumatoid arthritis significantly reduced symptoms and modulated metabolomic profiles. In cancer research, coclaurine, an alkaloid from Stephania tetrandra, has shown promise in non-small cell lung cancer (NSCLC) cells by inhibiting EFHD2 expression, which enhances sensitivity to cisplatin chemotherapy. Furthermore, alkaloid-rich fractions have demonstrated potent in vitro antiviral activity against SARS-CoV-2, with IC50 values in the low μg/mL range, suggesting potential as an antiviral agent. Secondary effects include reported in vitro and in vivo antiparasitic activity. While these findings are promising, most evidence is preclinical, and large-scale human trials are needed to confirm efficacy and establish population-specific benefits.
How it works
Stephania tetrandra exerts its effects through multiple biological pathways. Its anti-inflammatory action is primarily mediated by the inhibition of the PI3K/Akt signaling pathway, leading to the suppression of pro-inflammatory mediators. In cancer, specifically non-small cell lung cancer, the alkaloid coclaurine acts by transcriptionally repressing EFHD2, a protein involved in cell signaling, thereby disrupting the NOX4-ABCC1 pathway and enhancing the efficacy of chemotherapy drugs like cisplatin. The antiviral activity, particularly against SARS-CoV-2, is attributed to various alkaloids (tetrandrine, fangchinoline, cepharanthine) which are believed to interfere with viral entry or replication mechanisms. While these molecular targets and pathways are identified, the absorption and bioavailability of these alkaloids in humans may be limited, suggesting that in vitro potency might not directly translate to in vivo effects without optimized formulations.
Side effects
The overall safety profile of Stephania tetrandra extract is not extensively documented in human clinical trials, with most data derived from in vitro and animal studies. At studied doses in these preclinical models, it appears generally well tolerated. Common side effects are not well-established, and traditional use suggests low toxicity at therapeutic doses. However, there is a potential for cytotoxicity at high concentrations, which warrants caution. Specific drug interactions are not fully elucidated, but coclaurine's ability to modulate drug sensitivity, as seen with cisplatin in cancer cells, suggests potential interactions with chemotherapy agents. This requires careful clinical evaluation. Contraindications are not formally established, but due to its alkaloid content, caution is advised for pregnant individuals and those with pre-existing liver or kidney impairment. Further research is needed to comprehensively assess its safety in special populations and to define a maximum safe dose.
Dosage
Optimal dosage ranges for Stephania tetrandra extract in humans are not well-defined due to a lack of clinical trials. In animal models, an effective anti-arthritic dose of approximately 1.35 g/kg of extract was observed in rats over 28 days; however, a human equivalent dose has not been established. The maximum safe dose for human consumption is currently unknown, as toxicity studies are limited. The timing of administration for anti-inflammatory effects in animal studies suggests that effects may become apparent after several weeks of consistent treatment. While aqueous extracts are commonly used traditionally, alkaloid-enriched fractions have been studied for specific effects like antiviral and anticancer activities. It is important to note that the bioavailability of the active alkaloids may be limited, and future formulations might be necessary to improve absorption and efficacy. No specific cofactors are currently established to enhance its effects.
FAQs
Is Stephania tetrandra extract safe?
Preclinical data suggest safety at tested doses, but human safety data are limited, and potential cytotoxicity at high concentrations exists.
Can it be used with chemotherapy?
Coclaurine may enhance cisplatin efficacy in cell studies, but clinical confirmation and evaluation for drug interactions are needed.
How quickly does it work?
Anti-inflammatory effects in animal models were observed after approximately 28 days of consistent treatment.
Is it effective against viruses?
In vitro data show potent antiviral activity against SARS-CoV-2, but clinical efficacy and human relevance are unproven.
Does it have side effects?
Potential for cytotoxicity at high doses exists; traditional use suggests low toxicity at normal therapeutic doses, but human data are scarce.
Research Sources
- https://www.frontiersin.org/journals/pharmacology/articles/10.3389/fphar.2024.1447283/full – This animal study used multi-omics analysis to show that 1.35 g/kg of Stephania tetrandra extract reduced arthritis symptoms in rats over 28 days. It demonstrated the extract's ability to modulate metabolomic profiles and inhibit the PI3K/Akt pathway, supporting its anti-inflammatory effects in rheumatoid arthritis models.
- https://pmc.ncbi.nlm.nih.gov/articles/PMC11510146/ – This in vitro cell study investigated coclaurine's effect on non-small cell lung cancer (NSCLC) cells. It found that coclaurine inhibited EFHD2 expression, which enhanced the sensitivity of NSCLC cells to cisplatin chemotherapy, suggesting a potential role as an adjunct in cancer treatment.
- https://pubs.acs.org/doi/10.1021/acs.jnatprod.3c00159 – This in vitro assay evaluated the antiviral activity of Stephania tetrandra alkaloid fractions against SARS-CoV-2. The study reported potent inhibitory effects with IC50 values in the low μg/mL range, indicating a strong antiviral potential, though clinical translation requires further investigation due to bioavailability concerns.
- https://pmc.ncbi.nlm.nih.gov/articles/PMC7180683/ – This critical review comprehensively summarizes the phytochemistry and pharmacology of Stephania tetrandra, focusing on its alkaloids. It discusses various effects, including anti-inflammatory and antiparasitic activities, consolidating preclinical data but highlighting the lack of extensive clinical trial evidence.
