Theophylline Topical Has Interesting Properties


Sep 24, 2016
Theophylline is a breakdown-product of Coffeine.

Theophylline exerts complex anti-aging and anti-cytotoxicity effects in human skin ex vivo. - PubMed - NCBI

Theophylline is a phosphodiesterase inhibitor that is being used clinically for asthma therapy. In addition, it is recognized as a cosmetic agent with possible anti-aging and anti-oxidative properties. Nevertheless, how it affects human skin is still poorly examined.

Theophylline (10 or 100 µM) was administer to full-thickness human skin cultures for 24 or 72 hours.

Theophylline stimulated protein expression of the antioxidant metallothionein-1 and mRNA levels of collagen I and III. Assessment of fibrillin-1 immunohistology revealed enhanced structural stability of dermal microfibrils. Theophylline also exerted extracellular matrix-protective effects by decreasing MMP-2 and MMP-9 mRNA levels, partially antagonizing the effects of menadione, the potent, toxic ROS-donor. In addition, it decreased menandione-stimulated epidermal keratinocytes apoptosis. Interestingly, theophylline also increased the level of intracutaneously produced melatonin, i.e. the most potent ROS-protective and DNA damage-repair neuromediator, and tendentially increased protein expression of MT1, the melatonin receptor. Theophylline also increased the expression of keratin 15, the stem cell marker, in the epidermal basal layer but did not change mitochondrial activity or epidermal pigmentation.

This ex vivo pilot study in human skin shows that theophylline possesses several interesting complex skin-protective properties. It encourages further examination of theophylline as a topical candidate for anti-aging treatment.


Nov 14, 2014
Well coffee consumption is well known for protecting against all kinds of skin cancer, and epithelial cancers.
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