Will Emodin be a boon for cancer patients?

Cancer is also known as a malignant tumor rather than a benign tumor. Cancer is a disease caused by the overproliferation of cells in the body due to the loss of normal regulation. The overproliferating cells are called cancer cells, which can invade the surrounding tissues and even metastasize to other body parts through the body’s circulatory system or lymphatic system (cancer metastasis). There are many types of cancer, and the severity of the disease depends on the location of the cancer cells, their malignancy, and whether they have metastasized. Once diagnosed, it is often treated with surgery, chemotherapy, and radiation therapy. If cancer is left untreated, the result is usually death.

People of all ages are at risk of developing cancer, and because DNA damage accumulates with age, the chance of getting cancer increases. Cancer has become one of the leading causes of death in developed countries. Each year, one in four deaths in the United States is due to cancer, ranging from 100,000 to 350,000 worldwide.

Because of the severe impact of cancer on human health, the fight against cancer has been a scorching topic in medicine. In recent years, an emerging drug, Emodin, has attracted medical researchers’ attention, and some even believe that this drug could be a boon for cancer patients. So what exactly is Emodin, and what role does it play in the fight against cancer?

What is Emodin?

Emodin is a naturally occurring anthraquinone found in various plants used in traditional Chinese medicine and occurs primarily as the rhamnoside in rhubarb root. It is a cell-permeable, reversible, substrate-competitive, and potent inhibitor of p56lck tyrosine kinase (IC50 = 18.5 µM). This inhibitor selectively blocked the growth of v-ras-transformed human bronchial epithelial cells (IC50 = 14.8 µM) without affecting normal human bronchial epithelial cells, even at 370 mM. It has been reported to contribute to PHF catabolism in vitro and in vivo as an inhibitor of Tau aggregation. Emodin also inhibits HER2/neu tyrosine kinase activity in HER2/neu overexpressing breast cancer cells.

Source of Emodin

Emodin is an anthraquinone compound that can be isolated from Reynoutria japonica syn. Polygonum cuspidatum. Emodin is particularly abundant in the roots of Rheum palmatum, Polygonum cuspidatum, multiflorum, and Semen. It was isolated exclusively from Rheum palmatum L. It is also produced by many species of fungi, including Aspergillus, Pyrenochaeta, and members of the genus Pestalotiopsis. So we can also understand that Emodin is a natural plant extract.

Physiological effects of Emodin

Emodin is the active ingredient of several plants used in traditional Chinese medicine, such as Rheum palmatum, He Shou Wu, and He Shou Wu. It has been identified as having potential antiviral activity against coronaviruses such as SARS-CoV-2 and is one of the main active ingredients in the antiviral TCM preparation Lianhua Qingwan. Plant-derived and purified Emodin has various effects, including inhibition of inflammation, dyslipidemia, and cancer. Emodin has been shown to inhibit the ion channel of protein 3a, which may play a vital role in releasing viruses from infected cells. Among these effects, the anticancer effect of Emodin is particularly evident.

Prospects and Perspectives

Benchchem scientists have demonstrated through their research that Emodin can directly or selectively inhibit casein kinase II (IC50=0.89 μM). This action inhibits the COP9 signalosome, leading to the stabilization of the tumor suppressor p53. Furthermore, Emodin, as a phytoestrogen, binds to the human estrogen receptor and blocks the binding of 17β-estradiol, with Ki values of 0.77 and 1.5 μM for ERα and ERβ, respectively.

Because Emodin inhibits cancer cell replication and its antiviral activity, more and more scientists are beginning to study its pharmacology in anticancer. It is believed that shortly, Emodin will bring new hope to humanity in the medical field.