The South American social spider Parawixia bistriata produces a venom containing complex organic compounds with intriguing biological activities. The crude venom leads to paralysis in termites and stimulates l-glutamate uptake and inhibits GABA uptake in rat brain synaptosomes. Glutamate is the major neurotransmitter at the insect neuromuscular junction and at the mammalian central nervous system, suggesting a modulation of the glutamatergic system by the venom. Parawixin1, 2, and 10 (Pwx1, 2 and 10) are HPLC fractions that demonstrate this bioactivity. Pwx1 stimulates l-glutamate uptake through the main transporter in the brain, EAAT2, and is neuroprotective in in vivo glaucoma models. Pxw2 inhibits GABA and glycine uptake in synaptosomes and inhibits seizures and neurodegeneration, and Pwx10 increases l-glutamate uptake in synaptosomes and is neuroprotective and anticonvulsant, shown in in vivo epilepsy models. Herein, we investigated the low molecular mass compounds in this venom and have found over 20 small compounds and 36 unique acylpolyamines with and without amino acid linkers. The active substances in fractions Pwx1 and Pwx2 require further investigation. We elucidated and confirmed the structure of the active acylpolyamine in Pwx10. Both fraction Pwx10 and the synthesized component enhance the activity of transporters EAAT1 and EAAT2, and, importantly, offer in vitro neuroprotection against excitotoxicity in primary cultures. These data suggest that compounds with this mechanism could be developed into therapies for disorders in which l-glutamate excitotoxicity is involved.

Anti-inflammatory and anxiolytic properties of Lactuca sativa L extract was evaluated by formalin induced mice paw edema test, and elevated plus maze animal model respectively. Solid microspheres containing dispersed extract were obtained by water-in-oil-in-water multiple emulsion system followed by solvent evaporation method. Optimization was carried out using MINITAB 16 and optimized microspheres were loaded into a gel base. Anti-oxidant activity of optimized microspheres loaded gel was evaluated using DPPH (2,2-diphenyl-1-picrylhydrazyl) assay. The gel was also evaluated for its physical properties, drug release kinetics and anti-inflammatory activity using formalin induced mice-paw edema test where the anti-inflammatory potential was compared to marketed diclofenac gel (1.16% w/w). All doses of extract as well as microsphere loaded sustained release anti-inflammatory gel showed a dose and time dependent inhibition of edema (P<0.05), the extract also showed a dose dependent inhibition of level of anxiety (P<0.001). Potential anti-oxidant activity was seen with different concentration of crude extract and microsphere loaded gel. The anti-oxidant potential was compared using IC50 value which was 5.62 µg/mL, 6.34 µg/ml, 8.25 µg/mL for ascorbic acid, methanolic extract of L. sativa and microspheres loaded gel respectively.

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