In this series of papers, we will present the appearance of antibiotics in general, from the original animal and microbial natural peptides and proteins, metabolites of molds and yeasts, and bacterial metabolites, to a new generation of plant-based antibiotics. The focus will be on the discovery of hyperforin and its curative properties as a new multitarget antibiotic with unique properties and possibilities for the development of a multitarget medical tool. Chromatography and mass spectrometry of hyperforin, together with its antibiotic, antiprotozoal, and anticancer activities, will be presented in this series. A description of chromatographic/mass spectrometric evidence of the passage of hyperforin through the blood-testis barrier (BTB) and the blood-brain barrier (BBB) will be provided in part II. This antibiotic is a useful tool in the struggle against Neisseria gonorrhea and Neisseria meningitides because of its free passage through the BTB and BBB and its immunomodulatory effects, together with antibacterial and detoxification effects. This paper is the first in a series that addresses the problems of using antibiotics in general and the need for the development of a new generation of antibiotics. The advantages and disadvantages of using antibiotics in human and veterinary medicine will be discussed, as will the possible associated epidemics in general and the epidemics of methicillin-resistant Staphylococcus aureus (MRSA) in particular.