Hyperforin is a natural phloroglucinol that has been know for the treatment of depression. Hyperforin displays also antibacterial, antiproliferant and antiangiogenic activity. Synthetic derivatives of hyperforin have also recently been reported to possess increased bioactivity. The clinical applications are limited by the hydrophobic characteristics and the instability of the molecule. In this review we discuss about some of the derivatives of hyperforin (aristoforin, tetrahydrohyperforin and octahydrohyperforin) that demonstrated promising antitumor activity. Among these, octahydrohyperforin also possesses antibacterial activity against both the planktonic and biofilm states of bacteria.

Bacterial biofilms are organized communities of microorganisms, embedded in a self-produced matrix, growing on a biotic surface and resistant to many antimicrobial agents when associated with a medical device. These biofilms require the development of new strategies for the prevention and treatment of infectious disease, including the potential use of natural products. One interesting natural product example is Hypericum, a plant genus that contains species known to have antimicrobial properties. The major constituent of Hypericum perforatum is an unstable compound named hyperforin (1); for this reason it was not believed to play a significant role in the pharmacological effects. In this investigation a hydrogenated hyperforin analogue (2) was tested on several ATCC and clinical isolate strains, in their planktonic and biofilm form (Staphylococcus aureus, MRSA, and Enterococcus faecalis). Compound 2 was effective against planktonic and biofilm cultures, probably due to higher stability, showing the percentage of cells killed in the range from 45% to 52%. These results are noteworthy from the point of view of future development of these polyprenylated phloroglucinols as potential antibiotics.

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In this paper the authors investigated a synergistic antimycotic effect between four antifungal drugs Amphotericin B, Fluconazole, Tioconazole, and Flucytosine individually combined with Anidulafungin compound. This latter is considered a drug of choice in the treatment of fungal infections; it has good activity both in vitro and in vivo against yeasts and moulds, as Candida and Aspergillus. The goal of this study was to evaluate the in vitro interaction of Anidulafungin in the synergic combinations with previous reported drugs against 12 Candida strains according to CLSI M27-A3 protocol. A synergistic interaction was observed against the most antifungal strains; in particular an increasing of the antimycotic efficacy was obtained from the association between Anidulafungin and Amphotericin B or Fluconazole (Mixture 4:6). In contrast the association Tioconazole/Anidulafungin was less effective on fungal species growth. The antimycotics MIC reduction values were more evident against some strains as C. glabrata, C. krusei, C. tropicalis and C. parapsilosis.

Apixaban show to be an effective anticoagulant in patients with atrial fibrillation, even superior to warfarin in reducing the risk of stroke and systemic embolism regardless of the presence of renal insufficiency. Moreover, Food and Drug Administration allows the use of apixaban in patients with end stage renal disease on hemodialysis.