Production Technologies of Pharmacologically Active Sesquiterpene Lactones

Kishkentayeva, A. S.

doi:10.18321/ectj766

Cited by 3 publications

(1 citation statement)

References 15 publications

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“…The structural similarities between Tb and nTb make this compound an obvious starting point for the preparation of 12ADT (7) on a gram scale. Isolation and production technologies of pharmacologically active sesquiterpene lactones [31] were recently reviewed [32,33]. A protocol for isolation of crystalline Tb on a decagram scale by supercritical CO 2 extraction, followed by flash chromatography, is described in Section 2.1.…”

Section: Resultsmentioning

confidence: 99%

Large Scale Conversion of Trilobolide into the Payload of Mipsagargin: 8-O-(12-Aminododecanoyl)-8-O-Debutanoylthapsigargin

et al. 2020

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In spite of the impressing cytotoxicity of thapsigargin (Tg), this compound cannot be used as a chemotherapeutic drug because of general toxicity, causing unacceptable side effects. Instead, a prodrug targeted towards tumors, mipsagargin, was brought into clinical trials. What substantially reduces the clinical potential is the limited access to Tg and its derivatives and cost-inefficient syntheses with unacceptably low yields. Laser trilobum, which contains a structurally related sesquiterpene lactone, trilobolide (Tb), is successfully cultivated. Here, we report scalable isolation of Tb from L. trilobum and a transformation of Tb to 8-O-(12-aminododecanoyl)-8-O-debutanoylthapsigargin in seven steps. The use of cultivated L. trilobum offers an unlimited source of the active principle in mipsagargin.

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Section: Resultsmentioning

confidence: 99%

Large Scale Conversion of Trilobolide into the Payload of Mipsagargin: 8-O-(12-Aminododecanoyl)-8-O-Debutanoylthapsigargin

et al. 2020

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Traditional Use, Phytochemical Profiles and Pharmacological Properties of Artemisia Genus from Central Asia

et al. 2022

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The flora of Kazakhstan is characterized by its wide variety of different types of medicinal plants, many of which can be used on an industrial scale. The Traditional Kazakh Medicine (TKM) was developed during centuries based on the six elements of ancient Kazakh theory, associating different fields such as pharmacology, anatomy, pathology, immunology and food nursing as well as disease prevention. The endemic Artemisia L. species are potential sources of unique and new natural products and new chemical structures, displaying diverse bioactivities and leading to the development of safe and effective phytomedicines against prevailing diseases in Kazakhstan and the Central Asia region. This review provides an overview of Artemisia species from Central Asia, particularly traditional uses in folk medicine and the recent numerous phytochemical and pharmacological studies. The review is done by the methods of literature searches in well-known scientific websites (Scifinder and Pubmed) and data collection in university libraries. Furthermore, our aim is to search for promising and potentially active Artemisia species candidates, encouraging us to analyze Protein Tyrosine Phosphatase 1B (PTP1B), α-glucosidase and bacterial neuraminidase (BNA) inhibition as well as the antioxidant potentials of Artemisia plant extracts, in which endemic species have not been explored for their secondary metabolites and biological activities so far. The main result of the study was that, for the first time, the species Artemisia scopiformis Ledeb. Artemisia albicerata Krasch., Artemisia transiliensis Poljakov, Artemisia schrenkiana Ledeb., Artemisia nitrosa Weber and Artemisia albida Willd. ex Ledeb. due to their special metabolites, showed a high potential for α-glucosidase, PTP1B and BNA inhibition, which is associated with diabetes, obesity and bacterial infections. In addition, we revealed that the methanol extracts of Artemisia were a potent source of polyphenolic compounds. The total polyphenolic contents of Artemisia extracts were correlated with antioxidant potential and varied according to plant origin, the solvent of extraction and the analytical method used. Consequently, oxidative stress caused by reactive oxygen species (ROS) may be managed by the dietary intake of current Artemisia species. The antioxidant potentials of the species A. schrenkiana, A. scopaeformis, A. transiliensis and Artemisia scoparia Waldst. & Kitam. were also promising. In conclusion, the examination of details between different Artemisia species in our research has shown that plant materials are good as an antioxidant and eznyme inhibitory functional natural source.

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Revisiting the Medicinal Value of Terpenes and Terpenoids

Dash¹,

Tyagi²,

Sahu³

et al. 2022

Revisiting Plant Biostimulants

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Nowadays, plant-based chemicals have drawn the attention of pharmacy researchers due to their potent biological activity against various ailments. In this series, terpenes and terpenoids are gaining popularity among drug researchers gradually. Terpenes are naturally occurring large and varied class of hydrocarbons substances produced by a wide variety of plants including fruits, vegetables, flowers and some animals. Their concentration is generally high in plants. A broad range of the biological properties of terpenoids includes cancer chemo-preventive effects, antimicrobial, antifungal, antiviral, anti-hyperglycemic, anti-inflammatory, anti-parasitic activities and memory enhancers. Terpenoids are usually cyclic unsaturated hydrocarbons, with the altered number of oxygen moieties in the constituent groups attached to the basic isoprene skeleton. Terpenoids are a group of substances that occur in nearly every natural food. Terpenoids display a wide range of biological activities against cancer, malaria, inflammation, tuberculosis and a variety of infectious diseases including viral as well as bacterial. In this chapter, we have emphasized the proven and expected medicinal value of both terpenes and terpenoids.

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Production Technologies of Pharmacologically Active Sesquiterpene Lactones

Cited by 3 publications

References 15 publications

Large Scale Conversion of Trilobolide into the Payload of Mipsagargin: 8-O-(12-Aminododecanoyl)-8-O-Debutanoylthapsigargin

Large Scale Conversion of Trilobolide into the Payload of Mipsagargin: 8-O-(12-Aminododecanoyl)-8-O-Debutanoylthapsigargin

Traditional Use, Phytochemical Profiles and Pharmacological Properties of Artemisia Genus from Central Asia

Revisiting the Medicinal Value of Terpenes and Terpenoids

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