Scutellarin

Scutellarin at a Glance

Scutellarin is a flavone glucuronide — scutellarein-7-O-glucuronide — and the single most clinically used molecule in the skullcap flavone family. It is the standardised active of breviscapine (Chinese Dengzhan hua su), a flavonoid preparation from the daisy Erigeron breviscapus (Dengzhanhua) that has been used for decades in China, mostly by injection, to treat ischaemic stroke and cardiovascular/cerebrovascular disease ^{1Reference 1Wang L · 2018ReviewClinical benefits and pharmacology of scutellarin: a comprehensive reviewView study →}. Its aglycone is scutellarein, released when the glucuronide is hydrolysed.

Unlike most plant constituents here, scutellarin has a real human clinical footprint rather than only preclinical data — thousands of patients across randomised trials of breviscapine for acute cerebral infarction, unstable angina and diabetic complications ^{3,4,5Reference 3Lyu J et al. · 2020Clinical trialClinical evidence and GRADE assessment for breviscapine injection (DengZhanHuaSu) in patients with acute cerebral infarctionView study →Reference 4Zhi YJ et al. · 2018Meta-analysisZhi YJ, Zhao J, Zhao H, Yu DD (2018). [Efficacy and safety of breviscapine injection in treatment of unstable angina pectoris: systematic review and meta-analysis]. Zhongguo Zhong Yao Za Zhi. https://pubmed.ncbi.nlm.nih.gov/30453722/View study →Reference 5Zhao J et al. · 2019Meta-analysisZhao J, Zhi YJ, Zhao H, Yu DD (2019). [Efficacy and safety of breviscapine injection in treatment of diabetic nephropathy: systematic review and meta-analysis of randomized controlled trials]. Zhongguo Zhong Yao Za Zhi. https://pubmed.ncbi.nlm.nih.gov/30989899/View study →}. The honest caveat is evidence quality, not absence: these trials are mostly Chinese-language, single-region, and rated low-to-moderate on formal GRADE assessment ^{3Reference 3Lyu J et al. · 2020Clinical trialClinical evidence and GRADE assessment for breviscapine injection (DengZhanHuaSu) in patients with acute cerebral infarctionView study →}. The mechanism is deliberately multi-target — antioxidant, anti-inflammatory, vasorelaxant, anti-platelet and anti-coagulant, and directly cytoprotective to neurons and cardiomyocytes ^{1Reference 1Wang L · 2018ReviewClinical benefits and pharmacology of scutellarin: a comprehensive reviewView study →}.

Scutellarin is also one of the skullcap flavones that inhibit 5-HT7 receptor binding, a thread tying the molecule back to Scutellaria lateriflora’s traditional nervine use ^{2Reference 2Gafner S et al. · 2003Inhibition of [3H]-LSD binding to 5-HT7 receptors by flavonoids from Scutellaria laterifloraView study →}. Its recurring weakness runs through everything: poor oral bioavailability, which is exactly why the clinical material is injected ^{1,12Reference 1Wang L · 2018ReviewClinical benefits and pharmacology of scutellarin: a comprehensive reviewView study →Reference 12Hao X et al. · 2005AnimalStudy on the role of hepatic first-pass elimination in the low oral bioavailability of scutellarin in ratsView study →}.

Breviscapine — The Clinical Drug

The point is that scutellarin is not a hypothetical: it is the active principle of an established hospital medicine. Breviscapine (also romanised Dengzhan hua su) is a standardised flavonoid preparation extracted from Erigeron breviscapus in which scutellarin is the principal component ^{1Reference 1Wang L · 2018ReviewClinical benefits and pharmacology of scutellarin: a comprehensive reviewView study →}. It is manufactured as injectable and oral formulations and has been used in Chinese clinical practice since the 1980s for ischaemic stroke, coronary heart disease, angina and diabetic vascular complications ^{1Reference 1Wang L · 2018ReviewClinical benefits and pharmacology of scutellarin: a comprehensive reviewView study →}.

The clinical evidence base is unusually large for a plant flavonoid, though its quality is the load-bearing qualifier:

• Acute cerebral infarction. A systematic review with formal GRADE assessment pooled randomised trials of breviscapine injection (DengZhanHuaSu) in acute cerebral infarction and found signals of benefit on neurological outcome, but rated the certainty of evidence low, citing risk of bias and methodological limitations across the constituent trials ^{3Reference 3Lyu J et al. · 2020Clinical trialClinical evidence and GRADE assessment for breviscapine injection (DengZhanHuaSu) in patients with acute cerebral infarctionView study →}.
• Unstable angina. A systematic review and meta-analysis of breviscapine injection in unstable angina pectoris reported improved symptom and ECG outcomes when added to conventional therapy, again from largely Chinese-language randomised trials of variable quality ^{4Reference 4Zhi YJ et al. · 2018Meta-analysisZhi YJ, Zhao J, Zhao H, Yu DD (2018). [Efficacy and safety of breviscapine injection in treatment of unstable angina pectoris: systematic review and meta-analysis]. Zhongguo Zhong Yao Za Zhi. https://pubmed.ncbi.nlm.nih.gov/30453722/View study →}.
• Diabetic nephropathy. A systematic review and meta-analysis found breviscapine injection, as an adjunct, associated with improved renal markers in diabetic nephropathy ^{5Reference 5Zhao J et al. · 2019Meta-analysisZhao J, Zhi YJ, Zhao H, Yu DD (2019). [Efficacy and safety of breviscapine injection in treatment of diabetic nephropathy: systematic review and meta-analysis of randomized controlled trials]. Zhongguo Zhong Yao Za Zhi. https://pubmed.ncbi.nlm.nih.gov/30989899/View study →}.

Breviscapine is therefore best described as a widely used regional medicine with a genuine but methodologically limited clinical record, not a globally validated drug. The comprehensive pharmacology review of scutellarin frames it exactly this way — an accumulated body of clinical and mechanistic evidence for ischaemia and diabetic complications, tempered by trial-quality and bioavailability caveats ^{1Reference 1Wang L · 2018ReviewClinical benefits and pharmacology of scutellarin: a comprehensive reviewView study →}.

The 5-HT7 & Skullcap Nervine Connection

Scutellarin also links the cardiovascular drug story back to skullcap’s traditional role as a calming nervine. Screening Scutellaria lateriflora (American/mad-dog skullcap) for central activity, Gafner and colleagues found the hot-water and ethanol extracts bound the 5-HT7 serotonin receptor, and identified scutellarin among the flavone glucuronides responsible, inhibiting [³H]-LSD binding to 5-HT7 with an IC50 near 63 µM ^{2Reference 2Gafner S et al. · 2003Inhibition of [3H]-LSD binding to 5-HT7 receptors by flavonoids from Scutellaria laterifloraView study →}. This is an in-vitro binding affinity, not a demonstrated behavioural effect, and 63 µM is a weak interaction — but it is a plausible molecular thread connecting the flavones of American skullcap to that plant’s long nervine reputation, alongside the more-studied GABAergic flavone baicalin ^{2Reference 2Gafner S et al. · 2003Inhibition of [3H]-LSD binding to 5-HT7 receptors by flavonoids from Scutellaria laterifloraView study →}.

What It's Used For

Scutellarin’s evidence is genuinely split between a human clinical layer (breviscapine, in stroke and cardiovascular disease) and a mechanistic preclinical layer (isolated scutellarin in rodent and cell models). The two do not always test the same thing — the trials use the multi-flavonoid breviscapine preparation, while the mechanism studies use the purified molecule.

Evidence by IndicationStrength of support · Beta

Support is an experimental score — weighted by study type (human > animal > in vitro) and volume. A beta, not a validated metric. Human scores rest on breviscapine (the scutellarin-standardised preparation), not always the purified isolate, so read the per-row basis.

01Ischaemic Stroke / Cerebral IschaemiaPromising60%Breviscapine RCTs (GRADE-rated low) + rodent I/R mechanism ^{1,3,6,7,8Reference 1Wang L · 2018ReviewClinical benefits and pharmacology of scutellarin: a comprehensive reviewView study →Reference 3Lyu J et al. · 2020Clinical trialClinical evidence and GRADE assessment for breviscapine injection (DengZhanHuaSu) in patients with acute cerebral infarctionView study →Reference 6Wang S et al. · 2011Neuroprotection of scutellarin is mediated by inhibition of microglial inflammatory activationView study →Reference 7Zhang Y et al. · 2022AnimalScutellarin alleviates cerebral ischemia/reperfusion by suppressing oxidative stress and inflammatory responses via MAPK/NF-κB pathways in ratsView study →Reference 8Chen YJ et al. · 2021Scutellarin reduces cerebral ischemia reperfusion injury involving in vascular endothelium protection and PKG signalView study →}

02Cardiovascular / Myocardial ProtectionPromising48%Unstable-angina meta-analysis + rodent MI-reperfusion isolate work ^{1,4,9Reference 1Wang L · 2018ReviewClinical benefits and pharmacology of scutellarin: a comprehensive reviewView study →Reference 4Zhi YJ et al. · 2018Meta-analysisZhi YJ, Zhao J, Zhao H, Yu DD (2018). [Efficacy and safety of breviscapine injection in treatment of unstable angina pectoris: systematic review and meta-analysis]. Zhongguo Zhong Yao Za Zhi. https://pubmed.ncbi.nlm.nih.gov/30453722/View study →Reference 9Xu LJ et al. · 2020Scutellarin protects against myocardial ischemia-reperfusion injury by suppressing NLRP3 inflammasome activationView study →}

03Diabetic ComplicationsShaky40%Diabetic-nephropathy meta-analysis + preclinical retinopathy/nephropathy ^{1,5,10,11Reference 1Wang L · 2018ReviewClinical benefits and pharmacology of scutellarin: a comprehensive reviewView study →Reference 5Zhao J et al. · 2019Meta-analysisZhao J, Zhi YJ, Zhao H, Yu DD (2019). [Efficacy and safety of breviscapine injection in treatment of diabetic nephropathy: systematic review and meta-analysis of randomized controlled trials]. Zhongguo Zhong Yao Za Zhi. https://pubmed.ncbi.nlm.nih.gov/30989899/View study →Reference 10Long L et al. · 2019Scutellarin prevents angiogenesis in diabetic retinopathy by downregulating VEGF/ERK/FAK/Src pathway signalingView study →Reference 11Huang B et al. · 2024Scutellarin ameliorates diabetic nephropathy via TGF-β1 signaling pathwayView study →}

045-HT7 / Nervine BindingShaky22%Single in-vitro receptor-binding study (IC50 ~63 µM) ^{2Reference 2Gafner S et al. · 2003Inhibition of [3H]-LSD binding to 5-HT7 receptors by flavonoids from Scutellaria laterifloraView study →}

Mechanisms

The unifying read is anti-ischaemic multi-targeting: scutellarin does not act through one receptor but limits oxidative, inflammatory, thrombotic and mitochondrial injury simultaneously — which is both its therapeutic rationale and why any single-mechanism claim understates it ^{1Reference 1Wang L · 2018ReviewClinical benefits and pharmacology of scutellarin: a comprehensive reviewView study →}.

Pharmacokinetics

Scutellarin’s defining pharmacokinetic fact is poor oral bioavailability, and it explains the whole clinical dosage form. In rats, oral bioavailability is low largely because of extensive hepatic first-pass elimination ^{12Reference 12Hao X et al. · 2005AnimalStudy on the role of hepatic first-pass elimination in the low oral bioavailability of scutellarin in ratsView study →}, compounded by efflux-transporter handling in the gut — absorption can be raised by Cremophor EL through activation of MRP3 with concurrent inhibition of MRP2 and BCRP ^{13Reference 13Xiao L et al. · 2016A new mechanism for increasing the oral bioavailability of scutellarin with Cremophor EL: activation of MRP3 with concurrent inhibition of MRP2 and BCRPView study →}, and by triglyceride-mimetic prodrugs that route the molecule through intestinal lymphatic transport to bypass first-pass metabolism ^{14Reference 14Wang X et al. · 2021Triglyceride-mimetic prodrugs of scutellarin enhance oral bioavailability by promoting intestinal lymphatic transport and avoiding first-pass metabolismView study →}. This is why the clinical material (breviscapine) is given by injection, and why much of the scutellarin literature is formulation science — prodrugs, nanoparticles and delivery systems chasing an oral form ^{1,12,13,14Reference 1Wang L · 2018ReviewClinical benefits and pharmacology of scutellarin: a comprehensive reviewView study →Reference 12Hao X et al. · 2005AnimalStudy on the role of hepatic first-pass elimination in the low oral bioavailability of scutellarin in ratsView study →Reference 13Xiao L et al. · 2016A new mechanism for increasing the oral bioavailability of scutellarin with Cremophor EL: activation of MRP3 with concurrent inhibition of MRP2 and BCRPView study →Reference 14Wang X et al. · 2021Triglyceride-mimetic prodrugs of scutellarin enhance oral bioavailability by promoting intestinal lymphatic transport and avoiding first-pass metabolismView study →}. Robust human ADME parameters for a defined oral scutellarin dose (Cmax, half-life, absolute bioavailability of the isolate) are not well established outside the injectable preparation ^{1Reference 1Wang L · 2018ReviewClinical benefits and pharmacology of scutellarin: a comprehensive reviewView study →}.

Clinical Trials

Scutellarin is one of the few plant flavones with a substantial human trial record, via breviscapine: completed randomised trials and meta-analyses in acute cerebral infarction ^{3Reference 3Lyu J et al. · 2020Clinical trialClinical evidence and GRADE assessment for breviscapine injection (DengZhanHuaSu) in patients with acute cerebral infarctionView study →}, unstable angina ^{4Reference 4Zhi YJ et al. · 2018Meta-analysisZhi YJ, Zhao J, Zhao H, Yu DD (2018). [Efficacy and safety of breviscapine injection in treatment of unstable angina pectoris: systematic review and meta-analysis]. Zhongguo Zhong Yao Za Zhi. https://pubmed.ncbi.nlm.nih.gov/30453722/View study →} and diabetic nephropathy ^{5Reference 5Zhao J et al. · 2019Meta-analysisZhao J, Zhi YJ, Zhao H, Yu DD (2019). [Efficacy and safety of breviscapine injection in treatment of diabetic nephropathy: systematic review and meta-analysis of randomized controlled trials]. Zhongguo Zhong Yao Za Zhi. https://pubmed.ncbi.nlm.nih.gov/30989899/View study →}, plus a human pharmacokinetic interaction study in healthy volunteers examining breviscapine against losartan/CYP2C9 ^{15Reference 15Huang HX et al. · 2021Effect of CYP2C9 genetic polymorphism and breviscapine on losartan pharmacokinetics in healthy subjectsView study →}. The persistent limitation is methodological quality and regional concentration, not absence of trials.

Last checked: July 2026.

Isolate vs. Plant Studies

Scutellarin sits in an unusual middle position. The human evidence is a plant preparation — breviscapine is a standardised Erigeron breviscapus flavonoid extract in which scutellarin is the principal, but not the only, active ^{1Reference 1Wang L · 2018ReviewClinical benefits and pharmacology of scutellarin: a comprehensive reviewView study →}; the stroke, angina and nephropathy trials therefore test the preparation, and benefit cannot be assigned to the pure molecule with certainty ^{3,4,5Reference 3Lyu J et al. · 2020Clinical trialClinical evidence and GRADE assessment for breviscapine injection (DengZhanHuaSu) in patients with acute cerebral infarctionView study →Reference 4Zhi YJ et al. · 2018Meta-analysisZhi YJ, Zhao J, Zhao H, Yu DD (2018). [Efficacy and safety of breviscapine injection in treatment of unstable angina pectoris: systematic review and meta-analysis]. Zhongguo Zhong Yao Za Zhi. https://pubmed.ncbi.nlm.nih.gov/30453722/View study →Reference 5Zhao J et al. · 2019Meta-analysisZhao J, Zhi YJ, Zhao H, Yu DD (2019). [Efficacy and safety of breviscapine injection in treatment of diabetic nephropathy: systematic review and meta-analysis of randomized controlled trials]. Zhongguo Zhong Yao Za Zhi. https://pubmed.ncbi.nlm.nih.gov/30989899/View study →}. The mechanistic evidence is the isolate — the cerebral- and myocardial-ischaemia, retinopathy, nephropathy and mitophagy studies use purified scutellarin in rodents and cells ^{6,7,8,9,10,11,16Reference 6Wang S et al. · 2011Neuroprotection of scutellarin is mediated by inhibition of microglial inflammatory activationView study →Reference 7Zhang Y et al. · 2022AnimalScutellarin alleviates cerebral ischemia/reperfusion by suppressing oxidative stress and inflammatory responses via MAPK/NF-κB pathways in ratsView study →Reference 8Chen YJ et al. · 2021Scutellarin reduces cerebral ischemia reperfusion injury involving in vascular endothelium protection and PKG signalView study →Reference 9Xu LJ et al. · 2020Scutellarin protects against myocardial ischemia-reperfusion injury by suppressing NLRP3 inflammasome activationView study →Reference 10Long L et al. · 2019Scutellarin prevents angiogenesis in diabetic retinopathy by downregulating VEGF/ERK/FAK/Src pathway signalingView study →Reference 11Huang B et al. · 2024Scutellarin ameliorates diabetic nephropathy via TGF-β1 signaling pathwayView study →Reference 16Yang L et al. · 2024Scutellarin ameliorates mitochondrial dysfunction and apoptosis in OGD/R-insulted HT22 cells through mitophagy inductionView study →}. The honest framing is: meaningful clinical extract data + a strong isolate mechanism base + no large trial of a defined purified-scutellarin dose. Its aglycone scutellarein has its own, almost entirely preclinical, profile.

Prevalence in Nature

Scutellarin occurs as a flavone 7-O-glucuronide across two plant families of medicinal interest. Its highest-profile source is the daisy Dengzhanhua (Erigeron breviscapus, Compositae/Asteraceae) — the commercial raw material for breviscapine, where scutellarin is the principal flavonoid ^{1Reference 1Wang L · 2018ReviewClinical benefits and pharmacology of scutellarin: a comprehensive reviewView study →}. It is also a characteristic flavone glucuronide of skullcap (Scutellaria, Lamiaceae): it was isolated from the aerial parts of American skullcap (S. lateriflora) during the 5-HT7 bioassay work ^{2Reference 2Gafner S et al. · 2003Inhibition of [3H]-LSD binding to 5-HT7 receptors by flavonoids from Scutellaria laterifloraView study →}, and occurs in Chinese skullcap (S. baicalensis), S. barbata and other Scutellaria species alongside the related flavones baicalin, baicalein and wogonin. In the living plant the compound is stored as the glucuronide rather than the free aglycone scutellarein, and its structure is the 7-O-glucuronide of the apigenin-related flavone scutellarein (6-hydroxyapigenin) — placing it in the same flavone neighbourhood as luteolin.

Major Natural Sources

Source	Family	Plant part	Notes
Dengzhanhua (Erigeron breviscapus)	Asteraceae	aerial parts	Principal flavonoid; the commercial breviscapine source 1Reference 1Wang L · 2018ReviewClinical benefits and pharmacology of scutellarin: a comprehensive reviewView study →
American skullcap (Scutellaria lateriflora)	Lamiaceae	aerial parts	Flavone glucuronide isolated in 5-HT7 work 2Reference 2Gafner S et al. · 2003Inhibition of [3H]-LSD binding to 5-HT7 receptors by flavonoids from Scutellaria laterifloraView study →
Barbed skullcap (Scutellaria barbata)	Lamiaceae	aerial parts	Among its flavone glucuronides 1Reference 1Wang L · 2018ReviewClinical benefits and pharmacology of scutellarin: a comprehensive reviewView study →
Chinese skullcap (Scutellaria baicalensis)	Lamiaceae	root / aerial parts	Minor flavone glucuronide alongside baicalin 1Reference 1Wang L · 2018ReviewClinical benefits and pharmacology of scutellarin: a comprehensive reviewView study →

Quantitative content (percentage dry weight) is rarely reported in the primary literature for scutellarin specifically, so a comparative concentration chart is deferred to the gaps tracker rather than estimated.

Discovery & Synthesis

Scutellarin has no single datable isolation event. It was characterised as a flavone glucuronide of Scutellaria and Erigeron through twentieth-century flavonoid chemistry, and its modern significance dates to the standardisation of breviscapine from Erigeron breviscapus in China in the 1980s, when scutellarin was identified as the preparation’s principal active and the drug entered clinical use for cerebrovascular disease ^{1Reference 1Wang L · 2018ReviewClinical benefits and pharmacology of scutellarin: a comprehensive reviewView study →}. Chemically it is the 7-O-glucuronide of scutellarein (6-hydroxyapigenin); the glucuronide conjugation is what distinguishes it from the free aglycone and drives its poor oral absorption. Manufacture today is by extraction from cultivated Erigeron breviscapus rather than total synthesis, and the active research frontier is not synthesis but delivery — prodrugs, nanoparticles and absorption enhancers aimed at an orally viable form of an otherwise injection-bound molecule ^{1,13,14Reference 1Wang L · 2018ReviewClinical benefits and pharmacology of scutellarin: a comprehensive reviewView study →Reference 13Xiao L et al. · 2016A new mechanism for increasing the oral bioavailability of scutellarin with Cremophor EL: activation of MRP3 with concurrent inhibition of MRP2 and BCRPView study →Reference 14Wang X et al. · 2021Triglyceride-mimetic prodrugs of scutellarin enhance oral bioavailability by promoting intestinal lymphatic transport and avoiding first-pass metabolismView study →}.

Patents: not yet researched.

Toxicity & Safety

Scutellarin carries a low toxicity flag. Across its decades of clinical use as breviscapine and its preclinical record, it is generally well tolerated, and the comprehensive pharmacology review characterises its toxicity as low ^{1Reference 1Wang L · 2018ReviewClinical benefits and pharmacology of scutellarin: a comprehensive reviewView study →}. The safety considerations that do exist are tied to its being a hospital injectable, not a supplement: adverse events reported for breviscapine injection are mostly mild, but injectable herbal preparations carry a recognised risk of infusion/hypersensitivity reactions, so it is used under medical supervision ^{1,3Reference 1Wang L · 2018ReviewClinical benefits and pharmacology of scutellarin: a comprehensive reviewView study →Reference 3Lyu J et al. · 2020Clinical trialClinical evidence and GRADE assessment for breviscapine injection (DengZhanHuaSu) in patients with acute cerebral infarctionView study →}.

On interactions, a human pharmacokinetic study in healthy volunteers dosed breviscapine (120 mg/day) for 14 days and then a single 50 mg losartan dose, and found breviscapine did not significantly alter losartan pharmacokinetics overall, while CYP2C9 genotype (*1/*3 vs *1/*1) drove the expected differences in losartan/E-3174 exposure ^{15Reference 15Huang HX et al. · 2021Effect of CYP2C9 genetic polymorphism and breviscapine on losartan pharmacokinetics in healthy subjectsView study →}. That is reassuring for one CYP2C9 substrate but is a single small study and not a general clearance of interaction risk. Pregnancy and lactation are not adjudicated for an isolated plant constituent — those decisions belong to the herb or product where intake is decided; no dedicated reproductive-toxicity dataset for isolated scutellarin is characterised here.

Safety at a Glance

✅ Low / no toxicity

• Low intrinsic toxicity, long clinical use. Decades of use as breviscapine with a toxicity profile characterised as low ^{1Reference 1Wang L · 2018ReviewClinical benefits and pharmacology of scutellarin: a comprehensive reviewView study →}.
• No significant CYP2C9-substrate interaction in one human study. Breviscapine did not meaningfully change losartan pharmacokinetics in healthy volunteers ^{15Reference 15Huang HX et al. · 2021Effect of CYP2C9 genetic polymorphism and breviscapine on losartan pharmacokinetics in healthy subjectsView study →}.
• It is a supervised injectable medicine, not a supplement. The human product is dosed and monitored in clinical settings; injectable herbal preparations carry infusion/hypersensitivity risk ^{1,3Reference 1Wang L · 2018ReviewClinical benefits and pharmacology of scutellarin: a comprehensive reviewView study →Reference 3Lyu J et al. · 2020Clinical trialClinical evidence and GRADE assessment for breviscapine injection (DengZhanHuaSu) in patients with acute cerebral infarctionView study →}.
• Poor oral bioavailability undercuts oral/self-dosing claims. Heavy first-pass loss means an oral capsule delivers little of the injected drug’s exposure ^{12,13Reference 12Hao X et al. · 2005AnimalStudy on the role of hepatic first-pass elimination in the low oral bioavailability of scutellarin in ratsView study →Reference 13Xiao L et al. · 2016A new mechanism for increasing the oral bioavailability of scutellarin with Cremophor EL: activation of MRP3 with concurrent inhibition of MRP2 and BCRPView study →}.
• Clinical evidence is regionally bounded and low-to-moderate quality. Benefit signals rest largely on single-region trials rated low on GRADE ^{3Reference 3Lyu J et al. · 2020Clinical trialClinical evidence and GRADE assessment for breviscapine injection (DengZhanHuaSu) in patients with acute cerebral infarctionView study →}.

Dosage

There is no established self-administered oral dose for scutellarin. Its human use is as breviscapine, a supervised hospital medicine given largely by injection because oral absorption is poor. The figures below are clinical-study and research doses, not a recommendation:

Oral self-dosing of a scutellarin supplement would not reproduce the injected drug’s exposure, given first-pass loss ^{12,13Reference 12Hao X et al. · 2005AnimalStudy on the role of hepatic first-pass elimination in the low oral bioavailability of scutellarin in ratsView study →Reference 13Xiao L et al. · 2016A new mechanism for increasing the oral bioavailability of scutellarin with Cremophor EL: activation of MRP3 with concurrent inhibition of MRP2 and BCRPView study →}. These are doses studied in research and are not a personal recommendation.

References

1. Wang L, Ma Q (2018). Clinical benefits and pharmacology of scutellarin: a comprehensive review. Pharmacology & Therapeutics. https://pubmed.ncbi.nlm.nih.gov/29742480/
2. Gafner S, et al. (2003). Inhibition of [3H]-LSD binding to 5-HT7 receptors by flavonoids from Scutellaria lateriflora. Journal of Natural Products. https://pubmed.ncbi.nlm.nih.gov/12713409/
3. Lyu J, Xie Y, Sun M, Zhang L (2020). Clinical evidence and GRADE assessment for breviscapine injection (DengZhanHuaSu) in patients with acute cerebral infarction. Journal of Ethnopharmacology. https://pubmed.ncbi.nlm.nih.gov/32726677/
4. Zhi YJ, Zhao J, Zhao H, Yu DD (2018). [Efficacy and safety of breviscapine injection in treatment of unstable angina pectoris: systematic review and meta-analysis]. Zhongguo Zhong Yao Za Zhi. https://pubmed.ncbi.nlm.nih.gov/30453722/
5. Zhao J, Zhi YJ, Zhao H, Yu DD (2019). [Efficacy and safety of breviscapine injection in treatment of diabetic nephropathy: systematic review and meta-analysis of randomized controlled trials]. Zhongguo Zhong Yao Za Zhi. https://pubmed.ncbi.nlm.nih.gov/30989899/
6. Wang S, Wang H, Guo H, Kang L, Gao X, Hu L (2011). Neuroprotection of scutellarin is mediated by inhibition of microglial inflammatory activation. Neuroscience. https://pubmed.ncbi.nlm.nih.gov/21524691/
7. Zhang Y, et al. (2022). Scutellarin alleviates cerebral ischemia/reperfusion by suppressing oxidative stress and inflammatory responses via MAPK/NF-κB pathways in rats. Environmental Toxicology. https://pubmed.ncbi.nlm.nih.gov/36036213/
8. Chen YJ, et al. (2021). Scutellarin reduces cerebral ischemia reperfusion injury involving in vascular endothelium protection and PKG signal. Natural Products and Bioprospecting. https://pubmed.ncbi.nlm.nih.gov/34750765/
9. Xu LJ, Chen RC, Ma XY, Zhu Y, Sun GB, Sun XB (2020). Scutellarin protects against myocardial ischemia-reperfusion injury by suppressing NLRP3 inflammasome activation. Phytomedicine. https://pubmed.ncbi.nlm.nih.gov/31999976/
10. Long L, et al. (2019). Scutellarin prevents angiogenesis in diabetic retinopathy by downregulating VEGF/ERK/FAK/Src pathway signaling. Journal of Diabetes Research. https://pubmed.ncbi.nlm.nih.gov/31976335/
11. Huang B, et al. (2024). Scutellarin ameliorates diabetic nephropathy via TGF-β1 signaling pathway. Natural Products and Bioprospecting. https://pubmed.ncbi.nlm.nih.gov/38656633/
12. Hao X, Cheng G, Yu JE, He Y, An F, Sun J, Cui F (2005). Study on the role of hepatic first-pass elimination in the low oral bioavailability of scutellarin in rats. Pharmazie. https://pubmed.ncbi.nlm.nih.gov/15997843/
13. Xiao L, Yi T, Chen M, Lam CW, Zhou H (2016). A new mechanism for increasing the oral bioavailability of scutellarin with Cremophor EL: activation of MRP3 with concurrent inhibition of MRP2 and BCRP. European Journal of Pharmaceutical Sciences. https://pubmed.ncbi.nlm.nih.gov/27586020/
14. Wang X, et al. (2021). Triglyceride-mimetic prodrugs of scutellarin enhance oral bioavailability by promoting intestinal lymphatic transport and avoiding first-pass metabolism. Drug Delivery. https://pubmed.ncbi.nlm.nih.gov/34338567/
15. Huang HX, et al. (2021). Effect of CYP2C9 genetic polymorphism and breviscapine on losartan pharmacokinetics in healthy subjects. Xenobiotica. https://pubmed.ncbi.nlm.nih.gov/33509019/
16. Yang L, et al. (2024). Scutellarin ameliorates mitochondrial dysfunction and apoptosis in OGD/R-insulted HT22 cells through mitophagy induction. Biomedicine & Pharmacotherapy. https://pubmed.ncbi.nlm.nih.gov/39191025/

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