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Lettris is a curious tetris-clone game where all the bricks have the same square shape but different content. Each square carries a letter. To make squares disappear and save space for other squares you have to assemble English words (left, right, up, down) from the falling squares.
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|Jmol-3D images||Image 1|
|Molar mass||536.78 g/mol|
| (what is: / ?)
Except where noted otherwise, data are given for materials in their standard state (at 25 °C, 100 kPa)
Hyperforin has only been found in significant amounts in Hypericum perforatum (St. John's wort) with other species such as Hypericum calycinum (Greater St. John's wort or Aaron's beard) containing lower levels of the phytochemical. It is thought to be a monoamine oxidase inhibitor (MAOI). It accumulates in oil glands, pistils, and fruits, probably as a plant defense against herbivory. Other Hypericum species contain low amounts of hyperforin.
The structure of hyperforin was elucidated by a research group from the Shemyakin Institute of Bio-organic Chemistry (USSR Academy of Sciences in Moscow) and published in 1975. Hyperforin is a prenylated phloroglucinol derivative. An enantioselective total synthesis of hyperforin was reported in 2010.
Hyperforin is believed to be the primary active constituent responsible for the antidepressant and anxiolytic properties of the extracts of St. John's wort. It acts as a reuptake inhibitor of monoamines, including serotonin, norepinephrine, dopamine, and of GABA and glutamate, with IC50 values of 0.05-0.10 mcg/mL for all compounds, with the exception of glutamate, which is in the 0.5 mcg/mL range. Hyperforin also inhibits the reuptake of glycine and choline,. It appears to exert these effects by activating the transient receptor potential ion channel TRPC6. Activation of TRPC6 induces the entry of sodium and calcium into the cell which causes inhibition of monoamine reuptake.
Some pharmacokinetic data on hyperforin is available for an extract containing 5% hyperforin. Maximal plasma levels (Cmax) in human volunteers were reached 3.5h after administration of an extract containing 14.8 mg hyperforin. Biological half-life (t½) and mean residence time were 9h and 12h respectively with an estimated steady state plasma concentration of 100 ng/mL (approx. 180 nM/L) for 3 doses/d. Linear plasma concentrations were observed within a normal dosage range and no accumulation occurred.
Hyperforin has been found to be a potent inhibitor of COX-1 and 5-LO with IC50 values of 0.3μM and 90nM respectively. Giving it an anti-inflammatory action of approximately 3-18 times stronger than aspirin.
|5-HT||0.205 ± 0.045|
|Norepinephrine||0.080 ± 0.024|
|Dopamine||0.102 ± 0.019|
|GABA||0.184 ± 0.041|
|L-Glutamate||0.829 ± 0.687|
Hyperforin has antibiotic properties and is active against methicillin-resistant strains of Staphylococcus aureus (MRSA) with a minimal inhibitory concentration (MIC) value of 1.0 μg/mL, as well as against other gram-positive bacteria.
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