Abstract
Glycyrrhizinic acid (GL), also known as glycyrrhizin, is a triterpene saponin, a natural product found on the root of Glycyrrhyza glabra L. ("licquorice"), used worldwide as sweetener and in the traditional eastern medicines. This review is focused on a series of new derivatives synthesized using GL and its aglycon, glycyrrhetinic acid (GLA), as starting materials, the pharmacological activities described for those compounds, as well as new activities reported for GL and GLA themselves.
Highlights
Glycyrrhizinic acid or glycyrrhizin (GL) [1], Figure 1 is a triterpene saponin found in the root of the Leguminosae Glycyrryza glabra L., commonly known as “licquorice” or ‘licorice’ and is used worldwide as a natural sweetener and flavoring additive,1 as well as in the tradicional H O HO2C HO O H HO O O OHGlycyrrhetinic acid 1Chinese, Indian and Tibetan medicines.2 GL, along with its aglycon, glycyrrhetic or glycyrrhetinic acid (GLA), known as “enoxolone” [2], are the most studied and abundant compounds from this plant and are commercially obtained from the crude extract of the licquorice root
Bang and Kim, starting from 2, synthesized the 11-desoxo-3,30-diol which was selectively protected leading to. This protected diol was used as a hairpin loop for two Short hairpin RNA (shRNA), 168 and 169, that acted as gene silencers against the EGFP gene, a gene that codifies the Green Fluorescent Protein (GFP) and is used as a template to measure the activity of small interfering RNA (siRNA) (Scheme 19), indicating that the GLA derivative 166 can act as a hairpin loop for the syntheses of other shRNAs targeting different and clinically relevant genes
Several different synthetic strategies and some pharmacological activities were highlighted in this review, employing GL or its aglycon, GLA, mainly from research groups in Russia, Korea and Japan
Summary
Glycyrrhizinic acid or glycyrrhizin (GL) [1], Figure 1 is a triterpene saponin found in the root of the Leguminosae Glycyrryza glabra L., commonly known as “licquorice” or ‘licorice’ and is used worldwide as a natural sweetener and flavoring additive, as well as in the tradicional. Soc. GL, its aglycon and liquorice extracts are known for its wide range of biological activities, such as anti-inflamatory, anti-allergic, anti-arthritic, antioxidant, hypolipidaemic, antiviral and antitumoral, as well as presenting hepato and imunoprotective effects in humans and animals.. GL, its aglycon and liquorice extracts are known for its wide range of biological activities, such as anti-inflamatory, anti-allergic, anti-arthritic, antioxidant, hypolipidaemic, antiviral and antitumoral, as well as presenting hepato and imunoprotective effects in humans and animals.3,4 Both GL and its aglycon have been employed in the past decades as starting materials for the chemical synthesis of new derivatives, many of them with interesting biological activities. Some reviews have been published reporting new GL and GLA derivatives, as well as their activities.. Some reviews have been published reporting new GL and GLA derivatives, as well as their activities. The current review is focused, in recent data on the syntheses and the synthetic strategies employed for GL and GLA derivatives, published from 2003 onwards, the pharmacological activities of these synthesized derivatives, and new pharmacological activities reported for both GL and GLA
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