Abstract
15 extracts of different polarities (dichloromethane, methanol and aqueous extracts) from 5 Yemeni medicinal plants (Aspilia helianthoides, (Schumach. & Thonn.) Oliv. & Hiern subsp. ciliate (Schumach.) C.D. Adams leaves; Ceropegia rupicola, Defl. var. rupicola whole plant; Kniphofia sumarae, Defler whole plant; Pavetta longiflora, Vahl. subsp. longifloraleaves; and Plectranthus cf barbatus (Thulin & Gifri) leaves) were tested for their inhibitory effects against the enzymatic activity of human neutrophil elastase (HNE) (EC 3.4.21.37) in an in vitro human neutrophil elastase inhibition assay. 14 extracts at various concentrations were found able to inhibit the activity of HNE. Among the plants tested,A. helianthoides was the most active inhibitor of HNE. The dichloromethane extracts of all tested plants, exhibited more inhibitory effect on HNE activity than the methanolic and aqueous extracts. The dichloromethane extract of A. helianthoides showed the most active inhibitory effect on the HNE activity (IC50 = 0.4μg/ml). Within the HNE inhibitory active methanolic extracts, those of A. helianthoides and P. cf barbatus were the most active inhibitors with IC50 of about 3μg/ml. These results provide some scientific justification for the use of A. helianthoides in traditional medicine and indicate the presence of HNE inhibitory constituents in the active tested plants.
Highlights
Human neutrophil elastase (HNE) (EC 3.4.21.37), a member of the Chymotrypsin family of serine proteases (SI) is primarily located in the azurophil granules of polymorphonuclear leucocytes
The plants used in this study, with the exception of Aspilia helianthoides that was claimed to be useful for wound healing, are not used in Yemeni traditional medicine such as Kniphofia sumarae, locally named “Bünit”, or utilized for purposes other than inflammatory diseases such as Ceropegia rupicola, locally named “Bukira”, that is applied externally for skin diseases and Pavetta longiflora and Plectranthus cf barbatus, which are used as an anti-malarial agent and as a haemostatic respectively
Investigation the effect of the tested plant extracts on the HNE activity is able to reveal if these plants contain HNE inhibitors and possess anti-inflammatory activity
Summary
Human neutrophil elastase (HNE) (EC 3.4.21.37), a member of the Chymotrypsin family of serine proteases (SI) is primarily located in the azurophil granules of polymorphonuclear leucocytes. It is involved in the degradation of bacteria and immune complexes phagocytosed by the polymorphonuclear leucocytes [1]. The elastase action is modulated by endogenous multiple proteinase inhibitors including α1-proteinase inhibitor (α1-PI) Despite this balance between HNE and proteinase inhibitors activities, there are several human diseases in which a breakdown of this control mechanism is implicated in their pathology. Of the natural elastase inhibitors, three human plasma derived α1- protease inhibitors (Aralast, Prolastin and Zemaira) are used to prevent the progression of emphysema associated with α1- antitrypsin deficiency disorder [15–17). The aim of this study was to investigate the effects of a variety of extracts from some Yemeni plants on the activity of human neutrophil elastase
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