Cordycepin benefit and review of studies

Cordyceps militaris, a traditional medicinal mushroom, produces a component compound, cordycepin (3'-deoxyadenosine). Cordycepin has been known to have many pharmacological activities including immunological stimulating, anti-cancer, and anti-infection activities.

Pharmacokinetics of Adenosine and Cordycepin, a Bioactive Constituent of Cordyceps sinensis in Rat.
J Agric Food Chem. 2010. Institute of Traditional Medicine, School of Medicine, National Yang-Ming University, Taipei, Taiwan.
Cordycepin is a bioactive constituent of Cordyceps sinensis that has been shown to regulate homeostatic function. As an adenosine analogue, it is possible cordycepin goes through a similar metabolic pathway to that of adenosine. To investigate this hypothesis, a sensitive liquid chromatography with photodiode-array detector (HPLC-PDA) coupled to a microdialysis sampling system was developed to monitor cordycepin and adenosine in rat blood and liver. Other endogenous nucleosides were simultaneously measured to further understand the downstream metabolic pathway. The experiments were divided into six parallel groups for drug administration: (1) normal saline vehicle, (2) adenosine, (3) cordycepin, (4) normal saline + erythro-9-(2-hydroxy-3-nonyl)adenine (EHNA; a potent adenosine deaminase inhibitor), (5) adenosine + EHNA, and (6) cordycepin + EHNA. The pharmacokinetic results suggest that the levels of both adenosine and cordycepin decreased rapidly in blood around 30 min after drug administration. When adenosine was given, the concentrations of adenosine metabolites, hypoxanthinosine and hypoxanthine, increased in rat blood. This phenomenon was inhibited by EHNA pretreatment. An unidentified peak was observed in the blood and liver samples after cordycepin administration. The decline of this unidentified peak paralleled the decreased of the concentration of cordycepin, and it was not observed in the presence of the adenosine deaminase inhibitor. It is concluded that adenosine and cordycepin had short elimination half-lives and high rates of clearance and their biotransformation was suppressed by EHNA.

Cordycepin Suppresses Expression of Diabetes Regulating Genes by Inhibition of Lipopolysaccharide-induced Inflammation in Macrophages.
Immune Netw. 2009. College of Pharmacy, Sahmyook University, Seoul, Korea.
It has been recently noticed that type 2 diabetes (T2D), one of the most common metabolic diseases, causes a chronic low-grade inflammation and activation of the innate immune system that are closely involved in the pathogenesis of T2D. In the present study, we tested the role of cordycepin on the anti-diabetic effect and anti-inflammatory cascades in LPS-stimulated RAW 264.7 cells. We confirmed the levels of diabetes regulating genes mRNA and protein of cytokines through RT-PCR and western blot analysis and followed by FACS analysis for the surface molecules. Cordycepin inhibited the production of NO and pro-inflammatory cytokines such as IL-1beta, IL-6, and TNF-alpha in LPS-activated macrophages via suppressing protein expression of pro-inflammatory mediators. T2D regulating genes such as 11beta-HSD1 and PPARgamma were decreased as well as expression of co-stimulatory molecules such as ICAM-1 and B7-1/-2 were also decreased with the increment of its concentration. In accordance with suppressed pro-inflammatory cytokine production lead to inhibition of diabetic regulating genes in activated macrophages. Cordycepin suppressed NF-kappaB activation in LPS-activated macrophages. Based on these observations, cordycepin suppressed T2D regulating genes through the inactivation of NF-kappaB dependent inflammatory responses and suggesting that cordycepin will provide potential use as an immunomodulatory agent for treating immunological diseases.