It has been a rather rare event that the Nobel Foundation gave an award
to biomedical scientists who contributed to either discovery or development of
antibiotics (herbal remedy) such as penicillin and streptomycin. Nevertheless, this year three scientists are going to share a Nobel prize in
physiology/medicine for their discovery/development of ivermectin and
artemisinin which kill tropical parasites such as malaria and pathological
nematodes. Youyou Tu (85) in China who
discovered an anti-malaria herbal compound called artemisinin in 1970s shares a
half of this prize, while Satoshi Omura (80) at Kitasato Institute in Japan and
William Campbell (85) at Drew University in US, who
discovered/developed an anti-nematode antibiotic called ivermectin in 1980s,
share the remaining half of this prize.
Quite interestingly, both artemisinin
and ivermectin are PAK1-blockers, and are well known to suppress the growth of
cancers, and many other PAK1-dependent diseases/disorders. However, ivermectin appears not to pass BBB
(blood brain barrier), and therefore would be useless for the therapy of brain
tumors and neuronal diseases such as AD (Alzheimer’s disease). Although the IC50 of artemisinin (AM) against
cancer cells in cell culture is rather high, very recently a far more potent AM
derivative was developed by a German group. This AM derivative kills cancer
cells with IC50 around 10 nM (1). Thus, in the future, not only people living in
tropical zones, but also those in the remaining areas could have a significant benefit
from this potent anti-cancer AM derivative.
References:
1. Reiter C1,
Fröhlich T1,
Zeino M2,
Marschall M3,
Bahsi H3,
Leidenberger
M4, Friedrich O4,
Kappes B4,
Hampel F1,
Efferth T5,
Tsogoeva SB6.
New efficient
artemisinin derived agents against human leukemia cells, human cytomegalovirus
and Plasmodium falciparum: 2nd generation 1,2,4-trioxane-ferrocene hybrids.
Eur J Med Chem. 2015
; 97:164-72.
