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Planta Med 2019; 85(11/12): 1024-1033
DOI: 10.1055/a-0953-6007
Biological and Pharmacological Activities
Original Papers
Georg Thieme Verlag KG Stuttgart · New York

Halimium halimifolium: From the Chemical and Functional Characterization to a Nutraceutical Ingredient Design[1]

Khawla Kerbab‡
1   Unité de recherche Valorisation des Ressources Naturelles, Molécules Bioactives et Analyses Physicochimiques et Biologiques (VARENBIOMOL), Département de Chimie, Faculté des Sciences Exactes, Université Constantine 1, Constantine, Algérie
,
Francesca Sansone‡
2   Department of Pharmacy, University of Salerno, Fisciano (SA), Italy
,
Lahcene Zaiter
1   Unité de recherche Valorisation des Ressources Naturelles, Molécules Bioactives et Analyses Physicochimiques et Biologiques (VARENBIOMOL), Département de Chimie, Faculté des Sciences Exactes, Université Constantine 1, Constantine, Algérie
,
Tiziana Esposito
2   Department of Pharmacy, University of Salerno, Fisciano (SA), Italy
,
Rita Celano
2   Department of Pharmacy, University of Salerno, Fisciano (SA), Italy
,
Silvia Franceschelli
2   Department of Pharmacy, University of Salerno, Fisciano (SA), Italy
,
Michela Pecoraro
2   Department of Pharmacy, University of Salerno, Fisciano (SA), Italy
,
Fadila Benayache
1   Unité de recherche Valorisation des Ressources Naturelles, Molécules Bioactives et Analyses Physicochimiques et Biologiques (VARENBIOMOL), Département de Chimie, Faculté des Sciences Exactes, Université Constantine 1, Constantine, Algérie
,
Luca Rastrelli
2   Department of Pharmacy, University of Salerno, Fisciano (SA), Italy
,
Patrizia Picerno
2   Department of Pharmacy, University of Salerno, Fisciano (SA), Italy
,
Rita P. Aquino
2   Department of Pharmacy, University of Salerno, Fisciano (SA), Italy
,
Teresa Mencherini
2   Department of Pharmacy, University of Salerno, Fisciano (SA), Italy
› Author Affiliations
Further Information

Publication History

received 22 February 2019
revised 06 June 2019

accepted 07 June 2019

Publication Date:
01 July 2019 (online)

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Abstract

Halimium halimifolium (Hh) is a shrub used in Algerian folk medicine to treat gastrointestinal pain. An UHPLC-PDA-ESI/MSn method was developed to identify the metabolic profile of the traditionally used infusion (Hh-A) from the aerial parts. The structures of flavanols were confirmed by NMR analysis after the isolation procedure from a hydrohalcolic extract (Hh-B) that also allowed for the identification of phenolic acids, an aryl butanol glucoside, and different derivatives of quercetin, myricetin, and kaempferol. Tiliroside isomers were the chemical markers of Hh-A and Hh-B (54.33 and 36.00 mg/g, respectively). Hh-A showed a significant scavenging activity both against the radicals 1,1-diphenyl-2-picrylhydrazyl and 2,2′-Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (EC50 = 10.49 µg/mL and TEAC value = 1.98 mM Trolox/mg infusion) and the lipopolysaccharide-induced reactive oxygen species release in A375 and HeLa cells. Moreover, the antihyperglycemic properties, by inhibiting the α-amylase and α-glucosidase enzymes (IC50 = 0.82 mg/mL and 25.01 µg/mL, respectively), were demonstrated. To upgrade the therapeutic effect, a microencapsulation process is proposed as a strategy to optimize stability, handling, and delivery of bioactive components, avoiding the degradation and loss of the biological efficacy after oral intake. Hh-loaded microparticles were designed using cellulose acetate phthalate as the enteric coating material and spray drying as a production process. The results showed a satisfactory process yield (67.9%), encapsulation efficiency (96.7%), and micrometric characteristics of microparticles (laser-scattering, fluorescent, and scanning electron microscopy). In vitro dissolution studies (USPII-pH change method) showed that Hh-loaded microparticles are able to prevent the release and degradation of the bioactive components in the gastric tract, releasing them into the intestinal environment.

Key words

Halimium halimifolium - Cistaceae - antioxidant activity - antihyperglycemic activity - spray drying - gastro-resistant microparticles - nutraceuticals

1 Dedicated to Professor Dr. Cosimo Pizza 70th birthday in recognition of his outstanding contribution to natural product research.


 

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