What is Icaritin?
Icaritin powder (Anhydroicaritin) is a prenylflavonoid compound derived from Epimedium brevicornu Maxim, a traditional Chinese herbal medicine used for thousands of years.
Icaritin Sources
Icaritin naturally occurs in the Epimedium Genus, extracted from dried stems and leaves of Epimedium arrophylum, Epimedium pubescent, Epimedium Wushan, or Epimedium Korean.
Epimedium is a flowering plant that belongs to the Berberidaceae family. The Epimedium is also known as fairy wings, horny goat weed, and yin yang huo. Most of these herbs are found in China, and a few are prevalent in Asia and the Mediterranean. Most species have ‘spider-like’ four-parted flowers in the spring. They are naturally deciduous. One specie of Epimedium is used as a dietary supplement.
Constituents of epimedium plant Extract
Epimedium herb, commonly named Yinyanghuo in Chinese, originates in the Berberidaceae family, including Epimedium koreanum Nakai, Epimedium brevicornum Maxim, Epimedium pubescens Maxim, Epimedium sagittatum Maxim. and Epimedium wushanense .
Many chemical studies have shown that more than 260 components have been isolated from Epimedium, such as flavonoids, essential oils, phytosterols, polysaccharides, phenolic acids, and alkaloids. Pharmacological studies have shown that ingredients in Epimedium possess various attributes. For example, flavonoids, the significant components in Epimedium, which including baohuoside II, hyperoside, icariside I, icariin and astragalin, baohuoside I, epimedin A, epimedin B, quercitrin, sagittatoside A, sagittatoside B, epimedin C, have been widely used to improve cardiovascular and promote sexual function. They also offer anti-inflammation, anti-cancer, anti-osteoporosis, and anti-oxidation effects. Phenolic acids such as chlorogenic acid, neochlorogenic acid, and cryptochlorogenic acid have a wide range of pharmacological effects such as anti-inflammatory, anti-fatigue, and anti-tumor. In addition, alkaloids have been found to have anti glycemic and antioxidant activities.
Icaritin VS icariin
Icaritin, cas#118525-40-9, Molecular formula: C21H20O6, yellow powder.
Icariin, cas#489-32-7, Molecular formula: C33H40O15, Light yellow crystalline powder.
Icaritin is an unconjugated form of icariin hydroxylated at the 3,7-positions. Both icariin (ICA) and icaritin (ICT) are the primary active flavonoids extracted from traditional Chinese medicine epimedium that have been regarded as neuroprotective agents in disease models. Icaritin is the aglycone form of icariin.
Icariin (ICA) and icaritin (ICT) exhibit many pharmacological functions, including anti-osteoporosis, anti-cardiovascular, and anti-cancer activities.
Studies have found that icaritin has stronger pharmacological activity than icariin; icaritin can also promote osteogenic differentiation of bone marrow stromal cells and play an essential role in bone protection.
Icaritin VS artemisinin
Artemisinin, extracted from sweet wormwood (Artemisia annua), has been identified for treating malaria, including highly resistant strains.
Like artemisinin, Icaritin is a monomeric compound with 98.0%~102.0% obtained by enzymolysis from Epimedium II. It is a small-molecule drug.
Icaritin is a new paradigm based on modernizing traditional Chinese medicine after artemisinin.
How does Icaritin work?
Icaritin induces apoptosis through multiple and differential signaling pathways. Icaritin induces apoptosis by inhibiting the PI3K-AKT pathway in AML and CML cells;
PI3K-AKT is considered a major signaling pathway in cancer development. Studies have shown that icaritin inhibited the activation of PI3K-AKT, which partially inhibits tumor cell growth in AML and CML.
Icaritin inhibits the cell cycle of hematological cancer cells
The cell cycle has four distinct phases, namely, G0, G1, S, and G2/M. Previous studies proved that icaritin arrested the cell cycle and blocked the proliferation of blood tumor cells. For different cancer cells, icaritin arrests cells at different cell cycle phases. This effect is related to the action of icaritin on the specific cyclins and CDKs.
The study of the improvement effect of icaritin on hematopoietic function in cyclophosphamide-induced myelosuppression mice indicated that icaritin could protect against chemotherapy-induced bone marrow injury. In other words, icaritin might be an ideal agent that protects normal hematopoietic stem cells and damages hematologic malignancy cells simultaneously.
Icaritin Manufacturing process
Icaritin Benefits
Neuroprotection
Glutamate and glutamine are excitatory amino acids at a high level in the brain, take part in the glutamate-glutamine cycle, and are essential for maintaining normal brain health. Icaritin Increases levels of Antioxidant Molecules and Regulates Glutamate–Glutamine Cycle in the Substantia Nigra (a motor nucleus in the midbrain), further supporting that icaritin exerts neuroprotective effects.
Regulates estrogen
Several in vitro studies have shown that Icaritin has estrogen-like activity. Icaritin regulates the expression of estrogen-responsive genes through its unique mechanism of action in activating the ER.
Anti-cancer
The anticancer activity of icariin has been reported in breast, lung, esophageal, glioblastoma, leukemia, and HCC. Some studies found that icariin promotes HCC cell apoptosis and inhibits liver cancer cells by activating the caspase pathway and inhibiting the interleukin-6/Janus kinase (JNK) 2/signaling sensor and transcription activator 3 signaling pathway.
Icaritin reduces prostate cancer progression by inhibiting high-fat diet-induced serum adipokine in the TRAMP mice model.
Icariin inhibits multiple myeloma by inhibiting IL-6/JAK2/STAT3.
Icaritin s thought to be a novel immune modulator that could prolong survival in patients with hepatocellular carcinoma (HCC). Some studies found that icariin promotes HCC cell apoptosis and inhibits liver cancer cells by activating the caspase pathway and inhibiting the interleukin-6/Janus kinase (JNK) 2/signaling sensor and transcription activator 3 signaling pathway.
Icaritin side effects
There is currently no data on the serious side effects of Icaritin. However, high doses may cause side effects such as dizziness, vomiting, dry mouth, muscle cramps, and breathing problems.
Icaritin dosage
Some clinical trial data shows the recommended doses of Icaritin are between 400 and 1800mg for cancer treatment.
Icaritin Prices
Icaritin is very expensive in the market. The average price range is about USD 11000-13300/kg for different quantities. Wholesale icaritin powder from Cima will provide the most competitive price for you.
Where to buy bulk Icaritin powder
Wuxi Cima Science Co., Ltd is a nutritional raw material manufacturer. Cima is committed to quality, purity, and integrity. With the opening of our new factory, we now have three plants and one R&D center in China, and we have an office and warehouse in the USA.
Icaritin, 98% powder, is our star product. Our package is 1kg/aluminum foil bag, 25kg/drum; please email us if you want to know the price and technical documents, such as COA and MSDS; A free sample is available.
Reference:
- Wu, H., Liu, X., Gao, Z.-Y., Lin, M., Zhao, X., Sun, Y., & Pu, X.-P. (2021). Icaritin Provides Neuroprotection in Parkinson’s Disease by Attenuating Neuroinflammation, Oxidative Stress, and Energy Deficiency. In Antioxidants (Vol. 10, Issue 4, p. 529). MDPI AG. https://doi.org/10.3390/antiox10040529
- Wu, C.-T., Chen, M.-C., Liu, S.-H., Yang, T.-H., Long, L.-H., Guan, S.-S., & Chen, C.-M. (2021). Bioactive Flavonoids Icaritin and Icariin Protect against Cerebral Ischemia–Reperfusion-Associated Apoptosis and Extracellular Matrix Accumulation in an Ischemic Stroke Mouse Model. In Biomedicines (Vol. 9, Issue 11, p. 1719). MDPI AG. https://doi.org/10.3390/biomedicines9111719
- Icaritin reduces tert-butylhydroperoxide-induced cell damage through activation of Nrf2 and Akt in H9c2 cardiomyoblasts https://library.um.edu.mo/etheses/b25903226_toc.pdf