Procaine: From Numbing Agent to Cancer-Fighting Repurposed Medication
Can an old anesthetic hold the key to new possibilities in cancer care? Procaine, also known as Novocaine, has been around for well over a century. Discovered in 1905 by German chemist Alfred Einhorn, it was a breakthrough in the field of anesthesia, offering a safer and more manageable alternative to cocaine as a local anesthetic. Einhorn, known for his relentless dedication to creating a safe anesthetic, could hardly have predicted that his invention would someday be studied for its anti-cancer potential. Today, science is uncovering how this simple compound may bring new hope to cancer patients.
Procaine: A "Veteran" Drug with New Potential
Procaine, grandfathered in by the FDA due to its long-standing clinical use, has been utilized for decades primarily in dental and surgical procedures. Now, researchers are turning their attention to this “veteran” drug to explore its surprising role in cancer therapy. Procaine’s anti-cancer effects highlight the potential of repurposing old medications, shining light on novel pathways to target cancer cells.
How Procaine Fights Cancer
1. Anti-Inflammatory & Pain Relief
Beyond its familiar role in numbing, Procaine has powerful anti-inflammatory effects that could benefit cancer patients. Inflammation is not only a hallmark of cancer but also fuels its progression. By reducing inflammation, Procaine may help create a less favorable environment for cancer to thrive. Furthermore, it helps in managing pain—a crucial component of quality of life in cancer care.
2. Antioxidant Properties
Oxidative stress, which involves damage from free radicals, can fuel cancer development and progression. Procaine acts as an antioxidant, working to neutralize these free radicals and reduce oxidative stress, thus potentially slowing down the growth of cancer cells.
3. Anti-Proliferative Action
One of Procaine’s most promising effects is its ability to inhibit cancer cell proliferation. Cancer cells often use a process called DNA methylation to “switch off” tumor-suppressor genes, which would otherwise work to control abnormal growth. Procaine has been shown to reduce DNA methylation in certain cancers, including breast cancer. This action effectively slows down cell division and proliferation, potentially halting the tumor's growth.
4. Pro-Apoptotic Effects
Apoptosis, or programmed cell death, is a natural process that the body uses to eliminate damaged cells. Cancer cells often bypass apoptosis, allowing them to grow uncontrollably. Procaine has been shown to promote apoptosis in cancer cells, essentially reactivating this vital process and enabling the body to get rid of abnormal cells.
5. Anti-Metastatic Properties
Metastasis, the spread of cancer cells to other parts of the body, is one of the biggest challenges in oncology. Procaine has been shown to inhibit metastasis by influencing microRNAs, particularly miR-133b, which plays a role in limiting cancer cell migration. By making it harder for cancer to metastasize, Procaine adds another layer of defence against cancer’s spread.
6. Epigenetic Effects
Epigenetics involves changes in gene expression without altering the DNA itself. Procaine functions as a DNA-demethylating agent, reactivating tumor-suppressor genes that cancer cells often silence. This action supports the body’s natural defenses against cancer, essentially unlocking tools the body already has to combat malignancy.
7. Adjunctive Therapy
Procaine’s effects don’t stop with its own properties. Research suggests that it can work as an adjunct to traditional cancer treatments, such as chemotherapy and radiation. By enhancing the effects of these therapies, Procaine could potentially make these treatments more effective, increasing the impact of each dose and possibly allowing for lower doses that reduce toxic side effects.
Supporting Evidence and Additional Reading
If you’re interested in the research behind Procaine’s anti-cancer properties, here are some key studies:
Hao M, Zhang C, Shi N, Yuan L, Zhang T, Wang X. Procaine induces cell cycle arrest, apoptosis and autophagy through the inhibition of the PI3K/AKT and ERK pathways in human tongue squamous cell carcinoma. Oncol Lett. 2024;28:408.
Li C, Gao S, Li X, Li C, Ma L. Procaine inhibits the proliferation and migration of colon cancer cells through inactivation of the ERK/MAPK/FAK pathways by regulation of RhoA. Oncol Res. 2018;26(2):209-217. doi:10.3727/096504017X14944585873622.
Ali MS, Farah MA, Al-Lohedan HA, Al-Anazi KM. Comprehensive exploration of the anticancer activities of Procaine and its binding with calf thymus DNA: a multi-spectroscopic and molecular modeling study. RSC Advances. 2018;17. doi:10.1039/C7RA13647A.
Wu K-C, Liao K-S, Yeh L-R, Wang Y-K. Drug Repurposing: The Mechanisms and Signaling Pathways of Anti-Cancer Effects of Anesthetics. Biomedicines. 2022;10(7):1589. doi:10.3390/biomedicines10071589.
Villar-Garea A, Fraga MF, Espada J, Esteller M. Procaine is a DNA-demethylating agent with growth-inhibitory effects in human cancer cells. Cancer Res. 2003;63(16):4984-4989.
Ungurianu A, Margina D, Ionesco C, Borsa C. The Radioprotective Effect of Procaine and Procaine-Derived Product Gerovital H3 in Lymphocytes from Young and Aged Individuals. Oxidative Medicine and Cellular Longevity. 2020;4:1-10. doi:10.1155/2020/3580934.
Yau TM, Kim SC. Local anesthetics as hypoxic radiosensitizers, oxic radioprotectors, and potentiators of hyperthermic killing in mammalian cells. Br J Radiol. 1980;53(631):687-692. doi:10.1259/0007-1285-53-631-687.
Chlebowski RT, Block JB, Cundiff D, Dietrich MF. Doxorubicin cytotoxicity enhanced by local anesthetics in a human melanoma cell line. Cancer Treat Rep. 1980;66:121-125.
Viale M, Pastrone I, Pellecchia C, Vannozzi MO, Cafaggi S, et al. Combination of cisplatin-Procaine complex DPR with anticancer drugs increases cytotoxicity against ovarian cancer cell lines. Anticancer Drugs. 1998;9:457-463.