Hispidulin

Hispidulin have antioxidant, antifungal, anti-inflammatory, antimutagenic, and antineoplastic properties.

Hispidulin is a naturally occurring flavonoid found in various plants, including the herb Salvia officinalis (sage) and Sphaeranthus indicus.

Chemical Properties

Hispidulin, chemically known as 4',5,7-trihydroxy-6-methoxyflavone, belongs to the flavone subclass of flavonoids. Its molecular formula is C16H12O6, and it has a molecular weight of 300.26 g/mol. The structure of hispidulin includes three hydroxyl groups and one methoxy group, which contribute to its biological activity.

Natural Sources

Hispidulin is found in various plants, particularly those used in traditional medicine. Some notable sources include:

• Salvia officinalis (sage)
• Sphaeranthus indicus
• Artemisia annua (sweet wormwood)
• Eupatorium perfoliatum (boneset)

These plants have been used for centuries in traditional medicine systems, such as Ayurveda and Traditional Chinese Medicine, for their therapeutic properties.

Biological Activities

Hispidulin exhibits a wide range of biological activities, making it a compound of interest for various therapeutic applications. Some of the key biological activities include:

Antioxidant Activity

Hispidulin has been shown to possess strong antioxidant properties. It can scavenge free radicals and reduce oxidative stress, which is implicated in the pathogenesis of numerous chronic diseases, including cancer, cardiovascular diseases, and neurodegenerative disorders.

Anti-inflammatory Activity

Inflammation is a common underlying factor in many chronic diseases. Hispidulin has demonstrated significant anti-inflammatory effects by inhibiting the production of pro-inflammatory cytokines and enzymes, such as TNF-α, IL-6, and COX-2.

Anticancer Activity

Research has indicated that hispidulin exhibits anticancer properties against various cancer cell lines, including breast, lung, and colon cancer. It induces apoptosis (programmed cell death) and inhibits cell proliferation, migration, and invasion. These effects are mediated through multiple signaling pathways, including the PI3K/Akt and MAPK pathways.

Neuroprotective Effects

Hispidulin has shown promise in protecting against neurodegenerative diseases, such as Alzheimer's and Parkinson's disease. It exerts neuroprotective effects by reducing oxidative stress, inhibiting neuroinflammation, and modulating neurotransmitter systems.

Antimicrobial Activity

Hispidulin has demonstrated antimicrobial properties against a range of pathogens, including bacteria, fungi, and viruses. This makes it a potential candidate for developing new antimicrobial agents, particularly in the face of rising antibiotic resistance.

Potential Health Benefits

Given its diverse biological activities, hispidulin holds potential for various health benefits. Some of the potential therapeutic applications include:

Cardiovascular Health

Hispidulin's antioxidant and anti-inflammatory properties may contribute to cardiovascular health by reducing oxidative stress and inflammation, which are key factors in the development of atherosclerosis and other cardiovascular diseases.

Cancer Prevention and Treatment

The anticancer properties of hispidulin make it a promising candidate for cancer prevention and treatment. Its ability to induce apoptosis and inhibit cancer cell proliferation and migration could be harnessed in developing new anticancer therapies.

Neuroprotection

Hispidulin's neuroprotective effects suggest potential benefits in preventing and treating neurodegenerative diseases. By reducing oxidative stress and neuroinflammation, hispidulin may help preserve cognitive function and slow disease progression.

Anti-inflammatory and Antimicrobial Applications

Hispidulin's anti-inflammatory and antimicrobial properties could be beneficial in treating various inflammatory and infectious diseases. Its ability to modulate the immune response and inhibit pathogen growth makes it a versatile compound for therapeutic use.

Articles/Studies

PHARMACOLOGICAL ASSESSMENT OF HISPIDULIN--A NATURAL BIOACTIVE FLAVONE.

Clerodendrum petasites S. Moore: The therapeutic potential of phytochemicals, hispidulin, vanillic acid, verbascoside, and apigenin.

Medicinal importance, pharmacological activities, and analytical aspects of hispidulin: A concise report.

Dyslipidemia

Study:

Hispidulin is a naturally occurring flavonoid isolated from a traditional Chinese medicinal herb, Saussurea involucrata. In this study, the regulating role of hispidulin on the mRNA expression level of enzymes involved in lipid metabolism was examined in vitro and in vivo. Moreover, the in vivo lipid-modulating effect of hispidulin was compared with that of fenofibrate, a classical PPARα agonist. Our results in present study demonstrated that hispidulin can directly bind to and activate PPARα as an agonist and thus modulate the downstream lipid-metabolizing genes. Moreover, hispidulin could attenuate dyslipidemia in high fat diet induced dyslipidemia rat model. Although further studies are needed, this study provided evidence for the potential use of hispidulin in dyslipidemia management.

Allergies

• Immunosuppressive effect of hispidulin in allergic contact dermatitis.
• Hispidulin Inhibits Mast Cell-Mediated Allergic Inflammation through Down-Regulation of Histamine Release and Inflammatory Cytokines.

Anticonvulsive

The flavone hispidulin, a benzodiazepine receptor ligand with positive allosteric properties, traverses the blood-brain barrier and exhibits anticonvulsive effects.

Cancer

• Hispidulin suppresses the angiogenesis and growth of human pancreatic cancer by targeting vascular endothelial growth factor receptor 2-mediated PI3K/Akt/mTOR signaling pathway.
• Potential Therapeutic Role of Hispidulin in Gastric Cancer through Induction of Apoptosis via NAG-1 Signaling.
• Dual properties of hispidulin: antiproliferative effects on HepG2 cancer cells and selective inhibition of ABCG2 transport activity.
• Hispidulin Enhances TRAIL-Mediated Apoptosis via CaMKK/AMPK/USP51 Axis-Mediated Bim Stabilization.
• Hispidulin, a small flavonoid molecule, suppresses the angiogenesis and growth of human pancreatic cancer by targeting vascular endothelial growth factor receptor 2-mediated PI3K/Akt/mTOR signaling pathway.
• Hispidulin exhibits potent anticancer activity in vitro and in vivo through activating ER stress in non-small-cell lung cancer cells.
• Hispidulin mediates apoptosis in human renal cell carcinoma by inducing ceramide accumulation.
• Hispidulin induces ER stress-mediated apoptosis in human hepatocellular carcinoma cells in vitro and in vivo by activating AMPK signaling pathway.
• Hispidulin suppresses cell growth and metastasis by targeting PIM1 through JAK2/STAT3 signaling in colorectal cancer.
• Hispidulin suppresses tumor growth and metastasis in renal cell carcinoma by modulating ceramide-sphingosine 1-phosphate rheostat.
• Hispidulin induces mitochondrial apoptosis in acute myeloid leukemia cells by targeting extracellular matrix metalloproteinase inducer.

Cardiovascular

Hispidulin Attenuates Cardiac Hypertrophy by Improving Mitochondrial Dysfunction.

Other Effects

• Hispidulin prevents sevoflurane- Induced memory dysfunction in aged rats.
• Activation of Nrf2 Reduces UVA-Mediated MMP-1 Upregulation via MAPK/AP-1 Signaling Cascades: The Photoprotective Effects of Sulforaphane and Hispidulin.