Schaftoside

• Antioxidant
• Anti-inflammatory
• Neuroprotective
• Hepatoprotective

• Antiviral
• Antimicrobial
• Antidiabetic
• Skin barrier protection
• Anticancer

Schaftoside (apigenin-6-C-glucoside-8-C-arabinoside) exerts its diverse biological effects through multiple molecular pathways. As a di-C-glycosylflavone, schaftoside possesses a unique structural feature where two sugar molecules—a glucose at the C-6 position and an arabinose at the C-8 position—are directly attached to the apigenin backbone via carbon-carbon bonds, rather than through oxygen atoms as in O-glycosides. These C-glycosidic bonds are resistant to hydrolysis by glycosidases, contributing to schaftoside’s distinct pharmacokinetic profile and biological activities. One of schaftoside’s most extensively studied mechanisms is its antioxidant activity.

Schaftoside scavenges reactive oxygen species (ROS) and free radicals through its hydroxyl groups on the flavone structure. It neutralizes superoxide anions, hydroxyl radicals, and other reactive species, preventing oxidative damage to cellular components including lipids, proteins, and DNA. Beyond direct scavenging, schaftoside enhances endogenous antioxidant defenses by activating the nuclear factor erythroid 2-related factor 2 (Nrf2) pathway. By promoting Nrf2 nuclear translocation and binding to antioxidant response elements (AREs), schaftoside upregulates the expression of antioxidant enzymes including superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GPx), and heme oxygenase-1 (HO-1).

This dual approach to antioxidant protection—direct scavenging and enhancement of endogenous antioxidant systems—provides comprehensive defense against oxidative stress. As an anti-inflammatory agent, schaftoside inhibits the nuclear factor-kappa B (NF-κB) signaling pathway by preventing IκB kinase (IKK) activation and subsequent nuclear translocation of NF-κB, thereby reducing the expression of pro-inflammatory genes. It suppresses the production of inflammatory cytokines including tumor necrosis factor-alpha (TNF-α), interleukin-1β (IL-1β), and interleukin-6 (IL-6), while inhibiting cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) expression. Schaftoside also modulates the mitogen-activated protein kinase (MAPK) signaling pathways, including p38 MAPK, extracellular signal-regulated kinase (ERK), and c-Jun N-terminal kinase (JNK), further contributing to its anti-inflammatory properties.

A particularly significant anti-inflammatory mechanism of schaftoside is its ability to inhibit the NLRP3 inflammasome, a multiprotein complex involved in the processing and secretion of pro-inflammatory cytokines IL-1β and IL-18. By suppressing NLRP3 inflammasome activation, schaftoside reduces the production of these potent inflammatory mediators, providing additional anti-inflammatory benefits beyond NF-κB inhibition. In the central nervous system, schaftoside exhibits neuroprotective effects through multiple mechanisms. It protects neurons from oxidative stress and excitotoxicity by reducing glutamate-induced calcium influx and maintaining mitochondrial function.

Schaftoside also inhibits neuroinflammation by suppressing microglial activation and reducing the production of pro-inflammatory mediators in the brain. Furthermore, it has been shown to enhance brain-derived neurotrophic factor (BDNF) expression and activate the phosphatidylinositol 3-kinase (PI3K)/Akt signaling pathway, promoting neuronal survival and synaptic plasticity. Recent studies have demonstrated schaftoside’s ability to protect against cerebral ischemia-reperfusion injury by regulating autophagy and reducing oxidative stress, suggesting potential applications in stroke and other cerebrovascular conditions. In the liver, schaftoside demonstrates hepatoprotective effects through multiple mechanisms.

It reduces oxidative stress and inflammation in hepatocytes, protecting against various hepatotoxic agents. Schaftoside also modulates lipid metabolism by activating AMP-activated protein kinase (AMPK), potentially benefiting conditions like non-alcoholic fatty liver disease (NAFLD). Additionally, it has been shown to inhibit hepatic stellate cell activation and reduce collagen production, suggesting potential anti-fibrotic effects in chronic liver diseases. Schaftoside has demonstrated antiviral properties against several viruses, including influenza virus and dengue virus.

The antiviral mechanisms include direct inhibition of viral entry, interference with viral replication machinery, and modulation of host immune responses. The presence of two different sugar moieties at different positions on the apigenin backbone may contribute to schaftoside’s ability to interact with viral proteins and disrupt their function. In skin cells, schaftoside has been shown to improve barrier function and hydration. It enhances the expression of filaggrin, involucrin, and other proteins essential for skin barrier integrity.

Schaftoside also activates the aryl hydrocarbon receptor (AhR) pathway, which plays a role in skin homeostasis and protection against environmental stressors. Additionally, it reduces inflammation and oxidative stress in keratinocytes, potentially benefiting various skin conditions. In cancer cells, schaftoside demonstrates antiproliferative and pro-apoptotic effects. It induces cell cycle arrest by modulating the expression and activity of cell cycle regulators, including cyclins and cyclin-dependent kinases (CDKs).

Schaftoside also triggers apoptosis through both intrinsic (mitochondrial) and extrinsic (death receptor) pathways. It modulates the expression of Bcl-2 family proteins, decreasing anti-apoptotic proteins (Bcl-2, Bcl-xL) and increasing pro-apoptotic proteins (Bax, Bad), leading to mitochondrial membrane permeabilization, cytochrome c release, and activation of caspase cascades. Furthermore, schaftoside has been shown to inhibit angiogenesis and metastasis by reducing vascular endothelial growth factor (VEGF) expression and matrix metalloproteinase (MMP) activity. The unique di-C-glycosidic structure of schaftoside, with different sugar moieties at different positions, contributes to its distinct pharmacological profile compared to mono-C-glycosides like vitexin or isovitexin.

This structural feature affects its bioavailability, metabolism, and tissue distribution, potentially leading to different biological activities and therapeutic applications. The presence of both glucose and arabinose moieties may allow schaftoside to interact with a broader range of molecular targets, potentially explaining its diverse biological effects.

Optimal dosage ranges for schaftoside in humans have not been well established through clinical trials. Most research has focused on schaftoside as a component of herbal extracts, particularly from passion flower (Passiflora species), bamboo leaves, and wheat leaves, rather than as an isolated compound. Based on preclinical studies and limited human research with herbal extracts containing schaftoside, estimated effective doses would range from 5-30 mg of schaftoside daily. For passion flower extracts, typical daily doses range from 300-800 mg of standardized extract containing 0.1-0.5% schaftoside, corresponding to approximately 0.3-4 mg of schaftoside daily.

For bamboo leaf extracts, typical daily doses range from 200-600 mg of standardized extract containing 0.1-0.4% schaftoside, corresponding to approximately 0.2-2.4 mg of schaftoside daily. For wheat leaf extracts, typical daily doses range from 250-750 mg of standardized extract containing 0.1-0.3% schaftoside, corresponding to approximately 0.25-2.25 mg of schaftoside daily. It’s important to note that schaftoside’s bioactivity may be influenced by other compounds present in herbal extracts, potentially leading to synergistic effects that allow for lower effective doses compared to isolated schaftoside.

Schaftoside has relatively low oral bioavailability, estimated at approximately 1-5% in animal studies. This limited bioavailability is primarily due to its di-C-glycosidic structure, which affects its absorption and metabolism. Unlike O-glycosides, the C-glycosidic bonds in schaftoside (where glucose is directly attached to the C-6 position and arabinose to the C-8 position of apigenin via carbon-carbon bonds) are resistant to hydrolysis by intestinal and hepatic glycosidases. This means that schaftoside is primarily absorbed intact rather than being converted to its aglycone (apigenin) in the gastrointestinal tract.

The presence of two sugar moieties—glucose and arabinose—further increases the molecular weight and hydrophilicity of schaftoside, reducing passive diffusion across cell membranes. Absorption occurs primarily through active transport mechanisms, including sodium-dependent glucose transporters (SGLTs) and possibly other transporters, though the efficiency of this process is limited due to the complex structure. Once absorbed, schaftoside undergoes limited phase II metabolism, primarily glucuronidation and sulfation, though to a lesser extent than many other flavonoids due to its already glycosylated structure. The C-glycosidic bonds also make schaftoside less susceptible to efflux by P-glycoprotein transporters in the intestine, which may partially compensate for its limited passive diffusion.

In animal studies, schaftoside has demonstrated tissue distribution to various organs, including the liver, kidneys, and brain, though brain penetration is limited due to its hydrophilicity and relatively large molecular size. The presence of other compounds in herbal extracts, particularly from passion flower, bamboo leaves, and wheat leaves, may influence schaftoside’s bioavailability through various mechanisms, including competitive inhibition of metabolic enzymes or transporters.

Nanoemulsion formulations – can increase bioavailability by 3-10 fold by improving solubility and enhancing intestinal permeability, Liposomal encapsulation – protects schaftoside from degradation and enhances cellular uptake, Self-emulsifying drug delivery systems (SEDDS) – improve dissolution and absorption in the gastrointestinal tract, Phospholipid complexes – enhance lipid solubility and membrane permeability, Microemulsions – provide a stable delivery system with enhanced solubility, Combination with piperine – inhibits P-glycoprotein efflux and intestinal metabolism, Cyclodextrin inclusion complexes – improve aqueous solubility while maintaining stability, Solid dispersion techniques – enhance dissolution rate and solubility, Co-administration with other flavonoids that may compete for metabolic enzymes, potentially extending schaftoside’s half-life, Nanoparticle formulations – improve stability and targeted delivery, particularly relevant for hepatoprotective and neuroprotective applications

Schaftoside is best absorbed when taken with meals containing some fat, which can enhance solubility and stimulate bile secretion, improving dissolution and absorption. The presence of other flavonoids may enhance schaftoside’s bioavailability through competitive inhibition of metabolic enzymes or transporters. For antioxidant and anti-inflammatory effects, timing is less critical than consistency of use, though divided doses throughout the day may maintain more consistent blood levels due to schaftoside’s relatively short half-life (approximately 2-4 hours in animal studies). For neuroprotective effects, consistent daily dosing is important for maintaining protective mechanisms against oxidative stress and neuroinflammation.

For hepatoprotective effects, taking schaftoside with meals may enhance its delivery to the liver through the portal circulation. For skin barrier support, both oral and topical applications may be beneficial. Oral supplementation should be consistent daily dosing, while topical applications may be applied 1-2 times daily to affected areas. Enhanced delivery formulations like nanoemulsions or liposomes may have different optimal timing recommendations based on their specific pharmacokinetic profiles, but generally follow the same principles of taking with food for optimal absorption.

Traditional use of herbs containing schaftoside often involves preparing them as teas or tinctures, which may have different absorption characteristics compared to modern extract formulations. When consumed as a tea, the hot water extraction efficiently extracts schaftoside due to its good water solubility, but the absence of lipids may limit absorption compared to when taken with a meal.

• Gastrointestinal discomfort (mild, uncommon)
• Nausea (rare)
• Dizziness (rare)
• Headache (rare)
• Allergic reactions (rare)
• Mild drowsiness (uncommon, primarily when taken with passion flower extracts)

• Pregnancy and breastfeeding (due to insufficient safety data)
• Scheduled surgery (discontinue 2 weeks before due to potential mild sedative effects when present in passion flower extracts)
• Individuals with known allergies to plants in the Passifloraceae family (for passion flower-derived schaftoside), Poaceae family (for bamboo or wheat-derived schaftoside), or Pennisetum genus (for pearl millet-derived schaftoside)
• Individuals with severe liver or kidney disease (due to limited data on metabolism and excretion in these populations)
• Individuals taking medications that act on the central nervous system (due to potential additive effects when present in passion flower extracts)

• Sedatives and hypnotics (potential for additive sedative effects when schaftoside is present in passion flower extracts)
• Anticoagulant and antiplatelet medications (may enhance antiplatelet effects, potentially increasing bleeding risk, though this effect appears to be mild)
• Cytochrome P450 substrates (limited evidence suggests potential mild inhibition of certain CYP enzymes)
• Antioxidant medications (potential for additive effects with other antioxidants)
• Hepatoprotective medications (potential for additive effects with other hepatoprotective agents)
• Drugs requiring active transport for absorption (potential competition for transporters)
• Immunomodulatory drugs (potential for interaction due to schaftoside’s effects on inflammatory pathways)
• Topical medications (potential for interaction when schaftoside is applied topically alongside other active ingredients)

Due to limited human clinical data on isolated schaftoside, a definitive upper limit has not been established. Based on safety data for passion flower, bamboo leaf, and wheat leaf extracts (which contain schaftoside) and animal toxicity studies, doses up to 30 mg of schaftoside daily or 800 mg of standardized extract daily appear to be well-tolerated in most individuals. For general supplementation, doses exceeding these levels are not recommended without medical supervision due to potential drug interactions and limited long-term safety data at higher doses. It’s important to note that schaftoside has demonstrated a favorable safety profile in both preclinical and limited clinical studies, with a wide therapeutic window.

Acute toxicity studies in animals have shown very low toxicity, with LD50 values well above any reasonable supplemental dose. The presence of other bioactive compounds in herbal extracts may contribute to the overall safety profile, making it difficult to establish precise upper limits for isolated schaftoside. Traditional use of herbs containing schaftoside in moderate doses has a long history of safe use, further supporting the generally favorable safety profile of schaftoside-containing preparations.

Schaftoside itself is not approved as a drug by the FDA and is not commonly available as an isolated supplement. Plant extracts containing schaftoside, such as passion flower, bamboo leaf, and wheat leaf extracts, are regulated as dietary supplements under the Dietary Supplement Health and Education Act (DSHEA) of 1994. Manufacturers cannot make specific disease treatment claims but may make general structure/function claims with appropriate disclaimers. The FDA has not evaluated the safety or efficacy of schaftoside specifically.

Passion flower and bamboo leaves are generally recognized as safe (GRAS) when used in traditional amounts as herbs or supplements.

Eu: In the European Union, schaftoside is not approved as a medicinal product. However, passion flower extracts containing schaftoside are regulated as traditional herbal medicinal products under Directive 2004/24/EC in several EU countries, allowing them to be sold with specific health claims related to traditional use. The European Medicines Agency (EMA) has published a community herbal monograph on passion flower, recognizing its traditional medicinal use for relief of mild symptoms of mental stress and to aid sleep. Bamboo leaf and wheat leaf extracts are primarily regulated as food supplements in the EU.

Germany: In Germany, passion flower extracts are approved by Commission E (the German regulatory authority for herbs) for nervousness and sleep disorders. They are available as registered herbal medicinal products with specific therapeutic indications. Bamboo leaf and wheat leaf extracts are primarily available as food supplements.

Uk: In the United Kingdom, passion flower products may be registered as Traditional Herbal Medicinal Products (THMPs) under the Traditional Herbal Medicines Registration Scheme, allowing them to be sold with specific health claims based on traditional use. Bamboo leaf and wheat leaf extracts are primarily regulated as food supplements.

Canada: Health Canada regulates passion flower, bamboo leaf, and wheat leaf extracts as Natural Health Products (NHPs). Several products containing these extracts have been issued Natural Product Numbers (NPNs), allowing them to be sold with specific health claims. For passion flower, these include ‘traditionally used in Herbal Medicine as a sleep aid’ and ‘helps relieve restlessness and nervousness.’ Isolated schaftoside is not specifically approved as a standalone ingredient.

Australia: The Therapeutic Goods Administration (TGA) regulates passion flower, bamboo leaf, and wheat leaf extracts as complementary medicines. Several products containing these extracts are listed on the Australian Register of Therapeutic Goods (ARTG). Traditional use claims are permitted with appropriate evidence of traditional use. Schaftoside as an isolated compound is not specifically regulated.

China: In China, bamboo leaves (Zhu Ye) are officially listed in the Chinese Pharmacopoeia as a traditional Chinese medicine. They are approved for clearing heat, resolving phlegm, and calming the spirit. Various formulations containing bamboo leaves are approved for medicinal use. Passion flower and wheat leaves are less commonly used in traditional Chinese medicine. Schaftoside as an isolated compound is primarily used in research rather than as an approved therapeutic agent.

Japan: In Japan, bamboo leaves are recognized as medicinal plants and are included in some traditional Japanese medicine formulations. Passion flower and wheat leaves are less commonly used in Japanese traditional medicine. Schaftoside as an isolated compound is not specifically regulated for therapeutic use.

Medium to high

Isolated schaftoside is rarely available commercially for supplementation and is primarily sold as a research chemical at prices ranging from $300-$800 per 10-25 mg, making it prohibitively expensive for regular supplementation. Standardized passion flower extracts containing schaftoside along with other flavonoids typically cost $0.25-$1.00 per day for basic extracts and $1.00-$2.50 per day for premium, highly standardized formulations. Standardized bamboo leaf extracts containing schaftoside typically cost $0.30-$1.20 per day for basic extracts and $1.20-$3.00 per day for premium formulations. Standardized wheat leaf extracts containing schaftoside typically cost $0.25-$1.00 per day for basic extracts and $1.00-$2.50 per day for premium formulations.

Dried herbs for tea preparation (passion flower) are the most cost-effective option, typically costing $0.15-$0.50 per day, though they provide less consistent and potentially lower amounts of schaftoside.

The cost-effectiveness of schaftoside must be evaluated in the context of herbal extracts containing it, as isolated schaftoside is not practically available for regular supplementation due to its high cost and limited commercial availability. For antioxidant and anti-inflammatory benefits, there are likely more cost-effective options than schaftoside-containing extracts, as many other botanical antioxidants have similar potency at lower costs. For neuroprotective effects, particularly in the context of cerebral ischemia-reperfusion injury, the value proposition is promising based on preclinical studies, but clinical evidence is still lacking. The long-term benefits for neurodegenerative conditions would need to be substantial to justify ongoing supplementation costs.

For hepatoprotective effects, schaftoside-containing extracts offer moderate value compared to other liver-protective supplements. The preclinical evidence is promising, particularly for conditions like drug-induced liver injury and non-alcoholic fatty liver disease, but more clinical studies are needed to fully establish their efficacy in humans. For skin barrier support, schaftoside-containing extracts and topical formulations offer potential value for individuals with compromised skin barrier function, such as those with atopic dermatitis or aging skin. The emerging evidence for schaftoside’s effects on filaggrin and other skin barrier proteins suggests unique benefits that may justify its cost for specific skin conditions.

When comparing the cost-effectiveness of passion flower, bamboo leaf, and wheat leaf extracts containing schaftoside to other supplements with similar indications: For neuroprotection, they are comparably priced to other neuroprotective botanicals like Bacopa monnieri or Ginkgo biloba, but with less clinical evidence supporting their use. For hepatoprotection, they are generally more expensive than milk thistle (silymarin) extracts, which have more extensive clinical evidence for liver conditions. For skin barrier support, topical formulations containing schaftoside may offer unique benefits compared to conventional moisturizers, potentially justifying their higher cost for specific skin conditions. The most cost-effective way to consume schaftoside is through traditional passion flower tea, which can be prepared from dried herb at a fraction of the cost of processed extracts.

However, the concentration of schaftoside and other active compounds may be lower and less consistent in tea preparations compared to standardized extracts. Enhanced delivery systems such as nanoemulsions, liposomes, or SEDDS offer better bioavailability and potentially superior therapeutic outcomes, which may justify their higher cost for specific health conditions, particularly those requiring significant tissue penetration of schaftoside.

Pure schaftoside is moderately stable, with a typical shelf life of 2-3 years when properly stored. The C-glycosidic bonds (where glucose is directly attached to the C-6 position and arabinose to the C-8 position of apigenin via carbon-carbon bonds) provide better stability compared to O-glycosides, as they are resistant to hydrolysis by acids and enzymes. Standardized herbal extracts containing schaftoside, such as passion flower, bamboo leaf, or wheat leaf extracts, typically have a shelf life of 1-2 years from the date of manufacture. Dried herb material (e.g., passion flower, bamboo leaves, wheat leaves) properly stored can maintain acceptable schaftoside content for 1-2 years.

Tea preparations have a much shorter shelf life, with optimal potency maintained for only a few hours after preparation. Enhanced delivery formulations such as nanoemulsions or liposomes generally have shorter shelf lives of 1-2 years, depending on the specific formulation and preservative system. Topical formulations containing schaftoside typically have a shelf life of 1-2 years, though this can be extended with proper preservative systems and packaging.

Store in a cool, dry place away from direct sunlight in airtight, opaque containers. Refrigeration is recommended for liquid formulations and can extend shelf life of extracts containing schaftoside. Protect from moisture, heat, oxygen, and light exposure, which can accelerate degradation. For research-grade pure schaftoside, storage under inert gas (nitrogen or argon) at -20°C is recommended for maximum stability.

For dried herb material (e.g., passion flower, bamboo leaves, wheat leaves), store in airtight containers away from light and moisture to preserve the schaftoside content. The addition of antioxidants such as vitamin E or ascorbic acid to formulations can help prevent oxidation and extend shelf life. Enhanced delivery formulations may have specific storage requirements provided by the manufacturer, which should be followed carefully to maintain stability and potency. Topical formulations should be stored in airless pumps or tubes rather than jars to minimize exposure to air and potential contamination.

Avoid repeated freeze-thaw cycles, particularly for liquid formulations, as this can destabilize the product.

Exposure to UV light and sunlight – causes photodegradation, High temperatures (above 30°C) – accelerates decomposition, Moisture – can promote hydrolysis (though to a lesser extent than with O-glycosides) and microbial growth, particularly in liquid formulations, Oxygen exposure – leads to oxidation, pH extremes – schaftoside is most stable at slightly acidic to neutral pH (5-7), with increased degradation in strongly acidic or alkaline conditions, Metal ions (particularly iron and copper) – can catalyze oxidation reactions, Enzymatic activity – while the C-glycosidic bonds are resistant to glycosidases, other enzymes may affect the flavone structure, Incompatible excipients in formulations – certain preservatives or other ingredients may interact negatively with schaftoside, Repeated freeze-thaw cycles – can destabilize enhanced delivery formulations such as nanoemulsions or liposomes, Microbial contamination – particularly relevant for liquid and topical formulations, can lead to degradation of active compounds

Synthesis Methods

Natural Sources

Quality Considerations

Schaftoside itself was not identified or isolated until the modern era, but it is a constituent of several plants that have been used in traditional medicine systems for centuries. While the specific contribution of schaftoside to the traditional uses of these plants was unknown to ancient practitioners, it is now recognized as one of the bioactive compounds in these historically important medicinal materials. Schaftoside is primarily found in passion flower (Passiflora species), bamboo leaves, wheat leaves, and pearl millet, all of which have rich histories in traditional medicine across various cultures. Passion flower has been used by indigenous peoples of the Americas for centuries before European contact.

Native American tribes, including the Aztecs, Maya, and various North American groups, used passion flower for its calming and sedative properties. The Aztecs used passion flower as a sedative and to treat insomnia, nervousness, and epilepsy. Various indigenous tribes in North America used passion flower to treat wounds, earaches, liver problems, and as a mild pain reliever. When European explorers arrived in the Americas in the 16th century, they quickly learned about passion flower from indigenous peoples and brought it back to Europe.

The plant was named ‘passion flower’ by Spanish missionaries who saw in its unique flower structure symbols of the Passion of Christ. By the 17th century, passion flower was being used in European herbal medicine for its calming and sleep-promoting effects. In the 19th and early 20th centuries, passion flower was included in various pharmacopeias and was commonly prescribed for nervousness, insomnia, and epilepsy. It was officially listed in the United States National Formulary from 1916 to 1936 and in the British Herbal Pharmacopoeia.

Bamboo has been used in traditional Asian medicine, particularly in China, Korea, and Japan, for thousands of years. In Traditional Chinese Medicine (TCM), bamboo leaves (Zhu Ye) were first documented in the ‘Shennong Bencao Jing’ (Divine Farmer’s Classic of Materia Medica) around 200-300 CE. They were classified as herbs that clear heat, resolve phlegm, and calm the spirit. Bamboo leaves were traditionally used to treat fevers, coughs, phlegm, and irritability.

The cooling properties of bamboo leaves made them particularly valuable for treating conditions associated with ‘heat’ in TCM theory, including inflammatory conditions, fevers, and thirst. In Korean traditional medicine, bamboo leaves were used for similar purposes as in TCM, with additional applications for treating hypertension and diabetes. In Japanese Kampo medicine, bamboo leaves were included in various formulations for treating respiratory conditions and fevers. Wheat, one of the world’s oldest cultivated crops, has been used not only as a staple food but also for medicinal purposes in various cultures.

In ancient Egypt, Greece, and Rome, wheat was used in poultices for wounds and inflammatory conditions. The young wheat leaves, which contain schaftoside, were used in traditional European folk medicine for their nutritive and healing properties. In some traditional systems, wheat grass juice, derived from young wheat leaves, was used for detoxification, improving digestion, and enhancing overall health. Pearl millet, one of the oldest cultivated cereals in the world, has been a staple food in arid regions of Africa and Asia for thousands of years.

Beyond its nutritional value, pearl millet was used in traditional African medicine for its strengthening and revitalizing properties. In some traditional systems, pearl millet was believed to have cooling properties and was used to treat conditions associated with heat and inflammation. Corn silk, another source of schaftoside, has been used in traditional medicine systems worldwide. Native American tribes used corn silk tea for treating urinary tract infections, kidney stones, and as a diuretic.

In TCM, corn silk (Yu Mi Xu) was used to promote urination, reduce edema, and treat urinary tract infections. Schaftoside was first isolated and characterized in the mid-20th century as part of the scientific investigation into the active components of these traditional medicinal plants. Its structure was elucidated as apigenin-6-C-glucoside-8-C-arabinoside, identifying it as a di-C-glycosylflavone with unique carbon-carbon bonds between the flavone backbone and the sugar moieties. Modern scientific interest in schaftoside began to grow in the late 20th and early 21st centuries as research revealed its antioxidant, anti-inflammatory, neuroprotective, and hepatoprotective properties.

The discovery of schaftoside’s effects on oxidative stress, inflammatory pathways, and autophagy regulation has provided scientific explanations for some of the traditional uses of plants containing schaftoside, particularly their applications in inflammatory conditions, neurological disorders, and liver health.

No meta-analyses specifically on schaftoside are currently available; most analyses focus on herbal extracts containing schaftoside or flavonoids as a group.

Limited ongoing trials specifically investigating schaftoside; most research remains at the preclinical stage, Several preclinical studies investigating schaftoside’s potential in neurodegenerative diseases, particularly focusing on its neuroprotective properties in cerebral ischemia-reperfusion injury, Research on schaftoside’s hepatoprotective effects in various liver disease models, including non-alcoholic fatty liver disease and drug-induced liver injury, Investigations into schaftoside’s skin barrier-enhancing effects for potential applications in dermatology, Studies on schaftoside’s antiviral properties against respiratory viruses, including influenza and potentially coronaviruses, Research on novel delivery systems to enhance schaftoside’s bioavailability and targeted delivery