The venoms of several scorpion species have long been associated with pancreatitis in animal models and humans. Antarease, a Zn-metalloprotease from Tityus serrulatus, is able to penetrate intact ...pancreatic tissue and disrupts the normal vesicular traffic necessary for secretion, so it could play a relevant role in the onset of acute pancreatitis.
The cDNA libraries from five different scorpion species were screened for antarease homologs with specific primers. The amplified PCR products were cloned and sequenced. A structural model was constructed to assess the functionality of the putative metalloproteases. A phylogenetic analysis was performed to identify clustering patterns of these venom components.
Antarease-like sequences were amplified from all the screened cDNA libraries. The complete sequence of the antarease from T. serrulatus was obtained. The structural model of the putative antarease from Tityus trivittatus shows that it may adopt a catalytically active conformation, sharing relevant structural elements with previously reported metalloproteases of the ADAM family. The phylogenetic analysis reveals that the reported sequences cluster in groups that correlate with the geographical localization of the respective species.
Antareases are ubiquitous to a broad range of scorpion species, where they could be catalytically active enzymes. These molecules can be used to describe the evolution of scorpion venoms under different ecogeographic constrains.
For the first time the complete sequence of the antareases is reported. It is demonstrated that antareases are common in the venom of different scorpion species. They are now proposed as targets for antivenom therapies.
Secondary metabolites related to plant defense against natural enemies and enzymes involved in their biosynthesis vary during gall development. We assessed the differential gene expression related to ...defensive metabolites in cynipid wasp galls of Quercus castanea induced by Amphibolips michoacaensis throughout gall development. We assembled de nov
o transcriptomes from galls in three phases of growth and compared the differential expression of phenolic-related genes. We found that (1) Phenylalanine
ammonia
lyase (PAL) enzyme genes were upregulated at the intermediate and late growth stages. (2) Phenylpropanoid genes were upregulated at the intermediate stage and downregulated at the late stage. (3) Lignin genes were upregulated at the late stage. The transcriptomic profile of wasp galls exposes the switches in secondary metabolism during development. Patterns of differential expression shown in wasp galls suggest phenotype manipulation by the wasp larvae and physiological constraints of the host plant for enzyme channeling in different biosynthetic branches of phenolic compounds.
The conjugates of 6-substituted 1-oxoindanoyl carboxylic acids with
L
-isoleucine are mimics of the plant hormone (+)-7-
iso
-JA-
L
-Ile (
3
) that controls and regulates secondary metabolism and ...stress responses. In order to generate ligands that can be used as hormone-like compounds possessing different biological activities, an efficient and short synthesis of 6-bromo-1-oxoindane-4-carboxylic acid opens a general route to 6-Br-1-oxoindanoyl
L
-isoleucine conjugate (Br-In-
L
-Ile) (
9a
) as a key intermediate for several bioactive 6-halogen-In-
L
-Ile analogs (
7a
,
8a
,
10a
). The 6-ethynyl-In-
L
-Ile analog (
11a
) might be a valuable tool to localize macromolecular receptor molecules by click-chemistry. The activities of In-Ile derivatives were evaluated by assays inducing the release of volatile organic compounds (VOCs) in lima bean (
Phaseolus lunatus
). Each compound showed slightly different VOC induction patterns. To correlate such differences with structural features, modeling studies of In-Ile derivatives with COI-JAZa/b/c co-receptors of
P. lunatus
were performed. The modeling profits from the rigid backbone of the 1-oxoindanonoyl conjugates, which allows only well defined interactions with the receptor complex.
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