Recent enhancement of the immunity in AIDS and other immunocompromised patients by hyperforin an antibiotic from <i>Hypericum perforatum</i> L. (<i>in vitro</i> model) part I

Abstract

Today, <i>Hypericum perforatum</i> L. is probably one of the best-characterized medicinal plants, and hyperforin is its best-characterized constituent. Extracts from <i>H. perforatum</i> are widely used as antidepressants; however, less attention has been given to other properties of hyperforin, such as antitumor, fungicidal, antiviral and antibacterial action, or its possible use as a substance with immunomodulation properties. The present study summarizes results that describe the influence of hyperforin as an immunomodulation agent on phagocytosis and the breakdown of <i>Escherichia coli</i> by human polymorphonuclear neutrophils (PMNs). Hyperforin at 1 - 100 μg/mL concentrations was found to have a major influence on phagocytosis and the breakdown of <i>E. coli</i> by PMNs <i>in vitro</i>. A 100 µg/mL solution of hyperforin increased the uptake of non-opsonized <i>E. coli</i> almost 50-fold, and the uptake of IgG-opsonized <i>E. coli</i> more than threefold; on the other hand, the uptake of serum-opsonized bacteria was reduced to approximately 60% of that of the control. Hyperforin seems to bind to both PMNs and <i>E. coli</i> and acts like an opsonin. The elimination of remnants of IgG-opsonized <i>E. coli</i> from the PMNs was stimulated by hyperforin, while the elimination of remnants from non-op-so nized and serum-opsonized material was unaffected by the drug. Hyperforin exhibited clear immunomodulation ability as a phagocytosisstimulating agent. Hyperforin is probably inactive against human immunodeficiency virus (HIV) and most Gram-negative bacteria. However, it can protect acquired immunodeficiency syndrome (AIDS) patients and other immunocompromised patients by its antibacterial activity against Gram-positive bacteria and by enhancement of phagocytosis of Gram-positive and Gram-negative bacteria; some Gram-negative bacteria, such as <i>Neisseria</i>, are sensitive to hyperforin. Hyperforin has the ability to penetrate the blood-brain barrier (BBB) and blood-testis barrier (BTB) and is a valuable antibacterial agent against meningitis and gonorrhea. These properties of hyperforin are important for an antibiotic with immunomodulation activity in the struggle against the growing mortality in AIDS patients as a result of opportunistic bacteria, as recently shown by Bekondi <i>et al.</i> (2006, Int. J. Infect. Dis. 10, 387-395). It could also help to combat primary and opportunistic pathogens associated with meningitis in adults' relation to HIV serostatus

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“…It is also worth noting that there are substances with the opposite properties that work as immunomodulators and increase immunity [6]- [11].…”

Super Antibiotics, Part I. Hyperforin

“…http://ecdc.europa.eu/en/healthtopics/zika_virus_infection/zika-outbreak/pages/epide miological-situation.aspx#sthash.0cxI6MpK.dpuf. Hyperforin is one such antibiotic, as it can act against penicillin-and multiantibiotic-resistant bacteria, provides immunomodulatory effects, and exhibits the ability to pass through the BTB or BBB [9]- [16].…”

“…Some attempts to use the extracts for medical purposes were done in the former Soviet Union [21], where [22] the structure of the pharmaceutically active substance (PAS) hyperforin was also proposed [22]. was more precisely demonstrated [23] [24]; immunomodulatory activities were demonstrated later [12]- [16].…”

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“…Extracts from the plant Hypericum perforatum L. have been used to preserve food [1], treat infections [2], as immunomodulating agent [3] [4] [5] [6] and for many other medical purposes. One active constituent designated hyperforin, was isolated and characterized in 1971 [7].…”