Physalin pool from Physalis angulata L. leaves and physalin D inhibit P2X7 receptor function in vitro and acute lung injury in vivo.

P2X7 receptor promotes inflammatory response and neuropathic pain. New drugs capable of impairing inflammation and pain-reducing adverse effects extracted from plant extracts have been studied. Physalis angulate L. possesses traditional uses and exhibits antiparasitic, anti-inflammatory, antimicrobial, antinociceptive, antimalarial, antileishmanial, immunosuppressive, antiasthmatic. diuretic, and antitumor activities. The most representative phytochemical constituents identified with medicinal importance are the physalins and withanolides. However, the mechanism of anti-inflammatory action is scarce. Although some physalins and withanolides subtypes have anti-inflammatory activity, only four physalins subtypes (B, D, F, and G) have further studies. Therefore, we evaluated the crude ethanolic extract enriched with physalins B, D, F, and G from P. angulata leaves, a pool containing the physalins B, D, F, G, and the physalins individually, as P2X7 receptor antagonists. For this purpose, we evaluated ATP-induced dye uptake, macroscopic currents, and interleukin 1-ß (IL-1ß) in vitro. The crude extract and pool dose-dependently inhibited P2X7 receptor function. Thus, physalin B, D, F, and G individually evaluated for 5'-triphosphate (ATP)-induced dye uptake assay, whole-cell patch-clamp, and cytokine release showed distinct antagonist levels. Physalin D displayed higher potency and efficacy than physalin B, F, and G for all these parameters. In vivo mice model as ATP-induced paw edema was potently inhibited for physalin D, in contrast to physalin B, F, and G. ATP and lipopolysaccharide (LPS)-induced pleurisy in mice were reversed for physalin D treatment. Molecular modeling and computational simulation predicted the intermolecular interactions between the P2X7 receptor and physalin derivatives. In silico results indicated physalin D and F as a potent allosteric P2X7 receptor antagonist. These data confirm physalin D as a promisor source for developing a new P2X7 receptor antagonist with anti-inflammatory action.

Physalis angulata L. antineoplasic activity, in vitro, evaluation fromit's stems and fruit capsules

Physalis angulata L. (genus Physalis; family Solanaceae) is an herbaceous specimen that grows plentifully at North, Northeast and Middleast Brazilian's regions1. Its fruits are edible, roots and epigeal parts are taken as tea or infusion, all through the world as traditional medicine. Despite of this usefulness not much scientific work has been done on it. This research carried out with plant material (stems and fruit capsules) has the main aim to find out anti-neoplasic activity. The obtained results are described in Table 1. The most significant inhibition values are those for fruit capsules fractions such as 97 percent mouse lymphoma; 93 percent Erlich carcinoma strains when was assayed with MGTS-1-2ai and MGTS-1-1ai respectively. In the course on going studies on the biological response and chemical constituents of P. angulata some fractions were obtained from stems and fruit capsules ethanolic and methanolic extracts. The extract prepared from roots of P. angulata is the most clinically used by physicians for treatment of human hepatic disorders, despite the substance responsible for the efficacy still a matter of argument.