Optimisation of artemisinin and scopoletin extraction from Artemisia annua with a new modern pressurised cyclic solid–liquid (PCSL) extraction technique

Abstract

Introduction Artemisia annua is a small herbaceous plant belonging to the Asteraceae family declared therapeutic by the World Health Organisation, in particular for its artemisinin content, an active ingredient at the base of most antimalarial treatments, used every year by over 300 million people. In the last years, owing to low artemisinin content, research of new ways to increase the yield of the plant matrix has led to the use of the total extract taking advantage from the synergic and stabilising effects of the other components. Objective In this work we evaluated and compared the content of artemisinin and scopoletin in extracts of A. annua collected in the Campania Region (southern Italy), by two different extraction processes. Methodology Artemisia annua plants were extracted by traditional maceration (TM) in hydroalcoholic solution as a mother tincture prepared according to the European Pharmacopeia and by pressurised cyclic solid–liquid (PCSL) extraction, a new generation method using the Naviglio extractor. Results The results showed that the PCSL extraction technique is more effective than traditional methods in extracting both phytochemicals, up to 15 times more, reducing the extraction times, without using solvents or having risks for the operators, the environment and the users of the extracts. Conclusion The Naviglio extractor provides extracts with an artemisinin and scopoletin content eight times higher than the daily therapeutic dose, which should be evaluated for its stability over time and biological properties for possible direct use for therapeutic purposes.

Phytochemical Analysis and Anti-Inflammatory Activity of Different Ethanolic Phyto-Extracts of Artemisia annua L.

“…In particular, casticin was found to be able to inhibit IkBs by blocking the phosphorylation activity of IKK and, consequently, the k-kB cascade [55]. The same mechanism could be attributed to scopoletin, a phenolic coumarin, known for its cytotoxicity towards cancer cells, anti-inflammatory activity, and anti-angiogenesis activity [56]. NF-kB is a transcription factor that is usually located in the cytoplasm of the cell and translocated to the nucleus when activated.…”

Role of Plant-Derived Natural Compounds in Experimental Autoimmune Encephalomyelitis: A Review of the Treatment Potential and Development Strategy

“…Scopoletin, a phenolic coumarin derived from various medical or edible plants, possesses various medical properties and exhibits anti-inflammatory, anti-hypotensive ( Balkrishna et al, 2020 ), anti-diabetic ( Choi et al, 2017 ), and anti-aging activities ( Nam and Kim, 2015 ). Supercritical extraction and a new modern pressurized cyclic solid-liquid method are used for scopoletin extraction ( Jokić et al, 2016 ; Zarrelli et al, 2019 ). Under the inflammatory condition of EAE, DCs and antigen-presenting cells play an important role in disease occurrence, which can activate T cells after antigen presentation ( Zozulya et al, 2010 ).…”

Cytotoxicity of an Innovative Pressurised Cyclic Solid–Liquid (PCSL) Extract from Artemisia annua

“…Artemisia annua is a member of the Asteraceae family, with therapeutic properties mainly related to its content in artemisinin, a sesquiterpene lactone produced in the trichomes, which presents an endoperoxide bridge indispensable for its bioactivities [1]. Artemisinin and its derivatives are active ingredients at the basis of most antimalarial treatments [2], as well as present intriguing anticancer properties related to their capability to arrest cell growth, interfere with the cell cycle and/or activate multiple cell death pathways in cancer cells [3][4][5]. An increasing number of evidence suggests that the anticancer properties of A. annua are not exclusively related to a single active component of the plant, but rather to its whole phytochemical complex, including over 600 phytochemicals dominated by sesquiterpenoids, flavonoids, coumarins, enzymes and steroids [6], which may act synergistically [7][8][9].…”

“…It is widely reported that the extraction strategies can significantly affect the potential therapeutic efficacy of obtained samples mainly due to their chemical composition [13][14][15]. In this context, an innovative technique, based on pressurized cyclic solid-liquid (PCSL) extraction, was recently demonstrated to be significantly more efficient than the traditional methodologies used to obtain mother tincture (European Pharmacopeia) in extracting phytochemicals from A. annua [2]. This technique is based on the creation of a pressure gradient, achieved through compressions and immediate decompressions of the plant tissue, which ultimately leads to the extraction of trichomes and avoiding any maceration.…”

“…To date, the biological properties of A. annua PCSL extract have not been fully clarified; nevertheless, it is conceivable to suppose that the high levels of artemisinin and other phytochemicals detected in this product could have a positive impact on its anticancer properties compared to other preparations [2]. In this framework, the present study was mainly focused on assessment of the effects of A. annua PCSL extract, compared to canonical mother tincture, on four different cell lines: 1.…”