Cirsiliol

Cirsiliol is a flavonoid compound found in plants like artichoke and certain herbs that exhibits anti-inflammatory and potential anti-cancer properties. Research demonstrates its ability to modulate inflammatory pathways and inhibit tumor cell proliferation in preclinical studies.

Origin & History

Cirsiliol is a trihydroxy-6,7-dimethoxyflavone, a naturally occurring flavonoid compound belonging to the flavone class of polyphenols. It is extracted from Salvia x jamensis (a hybrid sage species) and other plant sources. As a methoxylated flavone, cirsiliol represents a structurally modified flavonoid with enhanced bioactivity compared to non-methylated counterparts.

Historical & Cultural Context

The research provides no information regarding cirsiliol's historical use in traditional medicine systems. Its traditional applications, if any, are not documented in the available literature.

Health Benefits

• May reduce inflammatory bowel disease symptoms - mouse studies showed significant reduction in disease activity index and colon inflammation at 10-30 mg/kg doses (animal evidence only)
• Potential anti-cancer effects - suppressed hepatocellular carcinoma tumor growth in mice and inhibited colon cancer cell proliferation in vitro (preliminary evidence)
• Supports intestinal barrier function - upregulated tight junction proteins Claudin-1, Occludin, and E-cadherin in mouse colitis models (animal evidence only)
• Antioxidant properties - increased glutathione levels while decreasing malondialdehyde in inflammatory conditions (animal evidence only)
• May improve diabetic cardiomyopathy - preliminary evidence suggests benefits through PPAR pathway modulation (very limited evidence)

How It Works

Cirsiliol exerts its anti-inflammatory effects by inhibiting pro-inflammatory cytokines and reducing NF-κB pathway activation. In cancer research, it demonstrates anti-proliferative activity by inducing apoptosis in tumor cells and modulating cell cycle progression. The compound also shows antioxidant properties through free radical scavenging mechanisms.

Scientific Research

Current evidence for cirsiliol consists entirely of preclinical animal studies and in vitro research, with no human clinical trials identified. Key studies include DNBS-induced colitis models in C57BL/6 mice showing efficacy comparable to sulfasalazine, and hepatocellular carcinoma xenograft studies in BALB/c nu/nu mice demonstrating tumor growth suppression. No PMIDs were provided in the research dossier.

Clinical Summary

Current research on cirsiliol is limited to animal and in vitro studies, with no human clinical trials available. Mouse studies for inflammatory bowel disease showed significant improvements at 10-30 mg/kg doses, including reduced disease activity index and colon inflammation. Anti-cancer effects have been observed in hepatocellular carcinoma and colon cancer cell lines in laboratory settings. The evidence remains preliminary and requires human studies to establish clinical efficacy and safety.

Nutritional Profile

Cirsiliol (5,3',4'-trihydroxy-6,7-dimethoxyflavone) is a methoxylated flavone with molecular formula C₁₇H₁₄O₇ and molecular weight ~330.29 g/mol. It is not a macronutrient source and is relevant solely as a bioactive polyphenolic compound. Found naturally in small quantities in plants of the Lamiaceae family, particularly in Leonotis nepetifolia, Salvia species, and Achillea fragrantissima, as well as in certain Compositae species. Typical concentrations in source plants range from trace amounts to approximately 0.01–0.5% of dry weight depending on species, plant part, and extraction conditions. Key structural features include methoxy groups at C-6 and C-7 and hydroxyl groups at C-5, C-3', and C-4', which contribute to its antioxidant and enzyme-inhibitory properties. As a methoxylated flavone, cirsiliol generally exhibits higher metabolic stability and improved membrane permeability compared to unmethylated flavones, potentially conferring moderate oral bioavailability relative to more polar flavonoids. However, like most dietary flavonoids, it is subject to extensive Phase I/II hepatic metabolism (glucuronidation, sulfation, methylation) and gut microbial biotransformation, which may limit systemic bioavailability in its parent form. No significant macronutrient (protein, fat, carbohydrate, fiber), vitamin, or mineral content is associated with cirsiliol itself. Its primary biological activities are attributed to its capacity to modulate NF-κB and STAT3 signaling pathways, inhibit cyclooxygenase (COX) and lipoxygenase (LOX) enzymes, scavenge reactive oxygen species (ROS), and interact with kinase cascades involved in inflammation and cell proliferation. In experimental models, effective concentrations in vitro typically range from 5–50 µM, while in vivo studies in mice have used oral doses of 10–30 mg/kg body weight. No established Recommended Daily Intake exists, and human pharmacokinetic data are currently unavailable.

Preparation & Dosage

Animal studies used 10-30 mg/kg body weight daily for inflammatory conditions and 20 mg/kg every three days for cancer models. In vitro studies employed 10-50 µM concentrations. No human dosage has been established due to absence of clinical trials. Consult a healthcare provider before starting any new supplement.

Synergy & Pairings

Sulfasalazine, Quercetin, Curcumin, Glutathione, Eupatorin

Safety & Interactions

Safety data for cirsiliol in humans is extremely limited due to lack of clinical trials. No specific drug interactions have been documented, though caution is advised with anticoagulant medications due to potential flavonoid interactions. Pregnant and breastfeeding women should avoid cirsiliol supplements due to insufficient safety data. Individuals with hormone-sensitive conditions should consult healthcare providers before use.