On May 10, 2022, a national invention patent launched by Chinese scientists showed that 10uM (micromoles/L) of Cepharanthine can inhibit coronavirus replication by 15393 times.

What is Cepharanthine?

Cepharanthine, a naturally occurring isoquinoline alkaloid extracted from the root block of Stephania Epigaea H.S.Lo, was demonstrated to have anti-inflammatory, immunomodulating, and antiviral effects.

Stephania epigaea H.S.Lo

Product Name Cepharanthine
Synonyms Cepharanthin;(+)-Cepharanthine;O-Methylcepharanoline
Botanical source Stephania epigaea H.S.Lo or Stephania yunnanensis H.S.Lo
CAS NO. 481-49-2
Molecular Formula C37H38N2O6
Molecular Weight 606.71g/mol
Appearance Light yellow to white powder
Specification 98%
Solubility Soluble in ethyl acetate, acetone, methanol, ethanol, insoluble in water
Benefits Increase white blood cells,anti-coronavirus,regulate immune function
Package 1kg/bag, 25kg/drum
Shipment by courier (FedEx, UPS), by air, by sea

Cepharanthine has a CAS number of 481-49-2 and a molecular formula of C37H38N2O6. Cepharanthine is also known by the following synonyms: Cepharanthin, (+)-Cepharanthine, and O-Methylcepharanoline.

Cepharanthine Structure

Cepharanthine natural sources

You can find natural Cepharanthine from Stephania families such as Stephania Epigaea H.S.Lo, Stephania yunnanensis H.S.Lo, Stephania cepharantha Hayata, Stephania japonica (Thunb.) Miers.

Cepharanthine development history

Cepharanthine has been used clinically for over 40 years, and its effect is remarkable. Especially in the recent two years of coronavirus research, it has super anti-new coronavirus activity, bringing new hope for defeating the epidemic.

  • In 1934, firstly found from S. S. cepharantha by Pharmacist Heisaburo Kondo
  • In 1941,1st patent purification process
  • In 1949,1st publications anti-pertussis,tuberculosis
  • In 1951, Cepharanthine was launched in Japan
  • In the 1980s, Cepharanthine showed anticancer activities, anti-inflammation, inhibition of lipid peroxidation, and Membrane-stabilization act.
  • In 1992, Cepharanthine showed anti-HIV activity
  • In 2000, Cepharanthine showed antiparasitic activities
  • In the 2010s, Cepharanthine bound to HSP90 and G4-DNA/RNA and showed potential activity in Alzheimer’s disease
  • In 2018, Cepharanthine inhibited bone resorption
  • In 2020, PharmaDrug Inc. conducted a clinical trial study on Cepharanthine

Cepharanthine covid-19

How to find cepharanthine is effective in inhibiting the spread of the coronavirus?

Dr. tong’s team used a unique drug screening platform to screen out three kinds of drugs from thousands of drugs: cepharanthine, siramectin, and mefloquine hydrochloride and carried out comparative experiments, and finally found that qianjin The effect of geranine is the best, and 10 uM of cepharanthine inhibits the replication of xCoV virus by 15393 times, indicating that cepharanthine is very effective in inhibiting the spread of the new coronavirus.

What is the potential mechanism of cepharanthine in inhibiting the infection of coronavirus?

  1. Inhibit virus entry by inhibiting the binding of S protein to ACE2 and cell membrane Ca2+ ion signaling pathway;
  2. Inhibit new coronavirus infection of cells by inhibiting heat shock protein response;
  3. Inhibit virus infection by up-regulating intracellular cholesterol level
  4. Finally, inhibit virus infection of cells by modulating host immunity. In addition, fenugreek may have other mechanisms for inhibiting the new coronavirus infection.

A summary of the research that cepharanthine can inhibit the coronavirus

country / region Cell experiments Animal experiments
Number of drugs to be screened Number of effective drugs found test drug effective drug
China 2406 3 not carried out
South Korea About 3000* 24 not carried out
Japan 360 2 not carried out
Taiwan, China >3000 15 Mefloquine, nelfinavir, salinomycin, thioguanine Mefloquine, nelfinavir
U.S.A 1900* 20 masitinib masitinib

*Note: The research in South Korea and the United States used a two-step screening method, first screening all drugs with another coronavirus, picking out effective drugs, and then testing the coronavirus.

Combination of nelfinavir and cepharanthine against covid-19

It is reported that Japanese scientists screened out two products with more potent antiviral activity: cepharanthine and nelfinavir. Cepharanthine significantly inhibits the binding of SARS-CoV-2 to cells; Nelfinavir may target major proteases, and Nelfinavir (NFV) inhibits SARS-CoV-2 replication. A combination of cepharanthine and nelfinavir can synergistically augment antiviral activity.

cepharanthine COVID-19

What are the Benefits of Cepharanthine?

Increase white blood cells

The beneficial effects of Cepharanthine on leukopenia were demonstrated as early as the 1980s (Oyaizu et al., 2001). It is a safe and potent method to protect against leukopenia caused by radiotherapy. In addition, it prevents neutropenia, increases the number of peripheral blood leukocytes, and promotes platelet production.

Antiviral effect

Cepharanthine has been shown to have unique antiviral properties against Human Immunodeficiency Virus (HIV).

for HIV-1, cepharanthine inhibits viral replication in U1 monocytic cells; for HTLV-1, cepharanthine inhibits the proliferation of both cell lines; and induces apoptosis of SIT cells; for HBV,cepharanthine inhibits viral replication and suppresses viral HBeAg antigen production; for SARS-CoV-2,cepharanthine inhibits viral entry and replication, suppresses viral infectivity; for GX_P2Vf, cepharanthine inhibits viral replication and cytopathic effects.

mechanism of action of cepharanthine

Cepharanthine hair loss (cepharanthine alopecia)

The anti-hair loss activity of cepharanthine was used earlier in France and Japan. Multiple studies have shown that CEP protects against aminoglycoside-induced hair cell death, stimulates cell proliferation, delays differentiation and keratinization of cultured mouse cells, and promotes the proliferation of hair cells cultured from mouse skin.

Also, cepharanthine has many other effects such as antiparasitic activity, inhibition of bone resorption, antiproliferative activity, Radiosensitization, etc.

Cepharanthine clinical applications

At present,cepharanthine clinical applications mainly treat snake bites, alopecia aerata, xerostomia, and leukopenia. Exploratory studies mainly are on Cancer, Osteoporosis, virus, parasites, infectious disease, and Sepsis.

Cepharanthine safety

FDA has approved CEP for the Treatment of immune thrombocytopenia (ITP).

Cepharanthine FDA

According to the WADA banned substances and the Prohibited list of WADA, cepharanthine is not on the list.

Cepharanthine side effects

Cepharanthine side effects are rarely reported, but overdose is not recommended and may cause discomfort.

Cepharanthine specifications

  • Cepharanthine powder
  • liposomal cepharanthine powder
  • cepharanthine hydrochloride powder

Cepharanthine is available in a variety of forms, including regular powder, liposomal powder, and hydrochloride powder. Each form has its own unique set of benefits and drawbacks. For instance, cepharanthine powder is the most affordable form but has a shorter shelf life than the other two forms. Liposomal cepharanthine powder is more expensive but has a longer shelf life and is more bioavailable than powder. When choosing a cepharanthine product, it is important to consider your needs and budget to find the right form for you.

About Cima Science

Cima Science is a top manufacturer of cepharanthine powder from China, with a capacity of over 10 tons per year. Cima Science is committed to quality and purity, and all ingredients are 100% free of contamination. Cima Science offers high-quality products at competitive prices and is always working to provide the best possible value to its customers. Get a quote now!

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