scholarly journals Centellosides in Centella Asiatica: Bioconversion (Ratios), Elite Lines, Biomarkers

Author(s):  
Renju Kunjumon ◽  
Anil John Johnson ◽  
Rajani Kurup ◽  
Sabulal Baby

Abstract Centellosides viz., asiatic acid (ASA), madecassic acid (MDA), asiaticoside (ASI), madecassoside (MAD), are the major bioactive molecules in Centella asiatica (CA). In this study MDA:ASA, MAD:ASI (C6-hydroxylation versus non-hydroxylation) and ASI:ASA, MAD:MDA (C28-glycoside versus aglycone) ratios in 50 CA accessions originally collected from wild locations in south India and grown under identical ecological conditions for six generations were determined using validated HPTLC-densitometry protocol(s). ASA, MDA, ASI and MAD ranged from 0.01-0.29% (average 0.06 ± 0.08%, n = 22; 28 accessions recorded ASA content as zero), 0.02-0.72% (0.12 ± 0.13%), 0.04-2.41% (0.44 ± 0.52%) and 0.15%-5.27% (1.59 ± 1.26%, n = 50), respectively. Distinctly, C6-hydroxylated (MDA:ASA 4.00, MAD:ASI 3.61) and C28-glycosylated (ASI:ASA 7.33, MAD:MDA 13.25) centellosides dominated over the respective non-derivatized entities. Our results infer that both C6-hydroxylation by P450-dependent monooxygenases and C28-glycosylation by UDP-Glc glucosyltransferases (UGTs) are dominant biosynthetic steps in CA. This study also discovered six elite clones of CA from south India with their (ASI+MAD) contents above the industrial benchmark (≥ 4%). Two elite clones with ASI contents ≥ 2% were also identified. These elite lines can be multiplied and utilized for the industrial applications of CA. Besides, this study emphasizes the need for standardizing all four centellosides as biomarkers in CA raw drugs, pharmaceutical and cosmetic products.

2019 ◽  
Vol 19 (2) ◽  
pp. 114-118
Author(s):  
Gian Luigi Mariottini ◽  
Irwin Darren Grice

Natural compounds extracted from organisms and microorganisms are an important resource for the development of drugs and bioactive molecules. Many such compounds have made valuable contributions in diverse fields such as human health, pharmaceutics and industrial applications. Presently, however, research on investigating natural compounds from marine organisms is scarce. This is somewhat surprising considering that the marine environment makes a major contribution to Earth's ecosystems and consequently possesses a vast storehouse of diverse marine species. Interestingly, of the marine bioactive natural compounds identified to date, many are venoms, coming from Cnidarians (jellyfish, sea anemones, corals). Cnidarians are therefore particularly interesting marine species, producing important biological compounds that warrant further investigation for their development as possible therapeutic agents. From an experimental aspect, this review aims to emphasize and update the current scientific knowledge reported on selected biological activity (antiinflammatory, antimicrobial, antitumoral, anticoagulant, along with several less studied effects) of Cnidarian venoms/extracts, highlighting potential aspects for ongoing research towards their utilization in human therapeutic approaches.


Plants ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 1219
Author(s):  
Marek Bunse ◽  
Peter Lorenz ◽  
Florian C. Stintzing ◽  
Dietmar R. Kammerer

The present study aimed at the identification and quantitation of phenolic compounds, fatty acids, and further characteristic substances in the seeds of Geum urbanum L. and Geum rivale L. For this purpose, individual components of extracts recovered with MeOH, CH2Cl2, and by cold-pressing, respectively, were characterized by HPLC-DAD/ESI-MSn and GC/MS and compared with reference compounds. For both Geum species, phenolic compounds, such as flavonoids and gallic acid derivatives, and triterpenes, such as saponins and their aglycones, were detected. Surprisingly, both Geum species revealed the presence of derivatives of the triterpenoid aglycons asiatic acid and madecassic acid, which were characterized for the first time in the genus Geum. Furthermore, the fatty acids of both species were characterized by GC–MS after derivatization. Both species showed a promising fatty-acid profile in terms of nutritional properties because of high proportions of unsaturated fatty acids. Linoleic acid and linolenic acid were most abundant, among other compounds such as palmitic acid and stearic acid. In summary, the present study demonstrates the seeds of G. urbanum and G. rivale to be a valuable source of unsaturated fatty acids and bioactive phenolics, which might be exploited for nutritional and cosmetic products and for phytotherapeutic purposes.


2012 ◽  
Vol 78 (13) ◽  
pp. 4654-4658 ◽  
Author(s):  
Claudio Gardana ◽  
Andrea Barbieri ◽  
Paolo Simonetti ◽  
Simone Guglielmetti

ABSTRACTPropolis (bee glue) is a resinous, sticky, dark-colored material produced by honeybees. Propolis today, due to its medicinal properties, is increasingly popular and is extensively used in food, beverages, and cosmetic products. Besides its numerous positive properties, propolis may also have adverse effects, such as, principally, allergic eczematous contact dermatitis in apiarists and in consumers with an allergic predisposition. In this study, we found appropriate conditions for removing caffeate esters, which are the main allergenic components, from raw propolis. The proposed method consists of the resuspension of propolis in a food grade solvent, followed by a biotransformation based on the cinnamoyl esterase activity ofLactobacillus helveticus. We showed that the reduction of caffeate esters byL. helveticusdid not affect the content of flavonoids, which are the main bioactive molecules of propolis. Furthermore, we verified that the biotransformation of propolis did not cause a loss of antimicrobial activity. Finally, we demonstrated that the ability ofL. helveticusto hydrolyze caffeate esters in propolis is strain specific. In conclusion, the proposed strategy is simple, employs food grade materials, and is effective in selectively removing allergenic molecules without affecting the bioactive fraction of propolis. This is the first study demonstrating that the allergenic caffeate esters of propolis can be eliminated by means of a bacterial biotransformation procedure.


2017 ◽  
Vol 4 (02) ◽  
pp. e66-e73 ◽  
Author(s):  
Tosapol Anukunwithaya ◽  
Mayuree Tantisira ◽  
Tsutomu Shimada ◽  
Yoshimichi Sai ◽  
Phisit Khemawoot

AbstractECa 233 is a standardized extract of Centella asiatica, characterized as a white powder containing triterpenoid glycosides not less than 80% with a ratio of madecassoside to asiaticoside of 1.5±0.5:1. Although pharmacological and toxicological profiles of ECa 233 have been successively reported, the pharmacokinetic data needed for further therapeutic development are not fully elucidated. This study aimed to investigate the pharmacokinetics of multiple oral dosing of ECa 233 at 100 mg/kg/day for 7 days in rats. Plasma, tissues, urine, and feces were collected from 0 to 24 h after dosing on days 1 and 7. The concentrations of asiaticoside, madecassoside, asiatic acid, and madecassic acid were simultaneously analyzed by liquid chromatography-tandem mass spectrometry. No significant change was observed in physical and blood biochemical parameters of the animals treated with ECa 233 for 7 days. The maximum plasma concentration and area under the curve at day 7 of madecassoside and asiaticoside decreased by 70–80% from day 1. However, both triterpenoid glycosides were extensively distributed and accumulated, resulting in significantly higher concentrations at pharmacologically relevant organs. Madecasssic acid and asiatic acid are major metabolites mainly found in and excreted via feces. Moreover, multiple dosing of ECa 233 increased mRNA expression of Abcb1a and Abcc2 in the small intestine by approximately 2- to 3-fold. This is the first study to identify an inductive effect of a standardized extract of C. asiatica after multiple oral dosing in rats. Potential drug-herb interactions when ECa 233 is coadministered with Abcb1a and Abcc2 substrates calls for further investigations.


2021 ◽  
Vol 12 ◽  
Author(s):  
Jia Hui Wong ◽  
Anna M. Barron ◽  
Jafri Malin Abdullah

Natural products remain a crucial source of drug discovery for accessible and affordable solutions for healthy aging. Centella asiatica (L.) Urb. (CA) is an important medicinal plant with a wide range of ethnomedicinal uses. Past in vivo and in vitro studies have shown that the plant extract and its key components, such as asiatic acid, asiaticoside, madecassic acid and madecassoside, exhibit a range of anti-inflammatory, neuroprotective, and cognitive benefits mechanistically linked to mitoprotective and antioxidant properties of the plant. Mitochondrial dysfunction and oxidative stress are key drivers of aging and neurodegenerative disease, including Alzheimer’s disease and Parkinson’s disease. Here we appraise the growing body of evidence that the mitoprotective and antioxidative effects of CA may potentially be harnessed for the treatment of brain aging and neurodegenerative disease.


Plants ◽  
2022 ◽  
Vol 11 (2) ◽  
pp. 148
Author(s):  
Seungeun Baek ◽  
Jong-Eun Han ◽  
Thanh-Tam Ho ◽  
So-Young Park

Centella asiatica (Apiaceae) is a tropical/subtropical medicinal plant, which contains a variety of triterpenoids, including madecassoside, asiaticoside, madecassic acid, and asiatic acid. In this study, we tested the efficiency of hairy root (HR) induction in C. asiatica from leaf and petiole explants. Leaves and petioles collected from C. asiatica plants were suspended in agro-stock for 30 min and co-cultured with Agrobacterium rhizogenes for 3 days to induce HR formation. The transformation efficiency of leaf and petiole explants was approximately 27% and 12%, respectively. A total of 36 HR lines were identified by PCR-based amplification of rol genes, and eight of these lines were selected for further analysis. Among all eight HR lines, the petiole-derived lines HP4 and HP2 displayed the highest growth index (37.8) and the highest triterpenoids concentration (46.57 mg∙g−1), respectively. Although triterpenoid concentration was >2-fold higher in leaves than in petioles of C. asiatica plants, the accumulation of triterpenoids in petiole-derived HR cultures was 1.4-fold higher than that in leaf-derived HR cultures. Additionally, in both leaf- and petiole-derived HR cultures, terpenoid production was higher in HRs than in adventitious roots. These results demonstrate that the triterpenoid content in the explant does not affect the triterpenoid content in the resultant HRs. The HR culture of C. asiatica could be scaled up to enable the mass production of triterpenoids in bioreactors for the pharmaceutical and cosmetic industries.


2018 ◽  
Vol 5 (02) ◽  
pp. e39-e47 ◽  
Author(s):  
Phisit Khemawoot ◽  
Patcharaporn Hengjumrut ◽  
Tosapol Anukunwithaya ◽  
Leng Chang ◽  
Supakit Wongwiwatthananukit ◽  
...  

Abstract Centella asiatica is a tropical plant commonly used as an herbal remedy in traditional medicines in many countries. In an attempt to establish an herbal extract with well-defined characteristics, a standardized extract of C. Asiatica, ECa 233, was developed. This extract contains at least 80% triterpenoid glycosides with the major constituents madecassoside and asiaticoside at a ratio of 1.5±0.5:1. In the present study, comparative pharmacokinetics of ECa 233 with its mixture of madecassoside and asiaticoside were conducted in rats. Following intravenous or oral administration of the test compounds, blood, tissues, urine, and feces were collected for the determination of madecassoside, asiaticoside, and their metabolite levels using liquid chromatography tandem mass spectrometry. Plasma levels of madecassoside and asiaticoside in the ECa 233-treated group were found to be higher than their respective counterparts in the mixture. Madecassoside and asiaticoside in both test formulae appeared to be widely distributed in several organs, and more than 50% of the administered doses were recovered as madecassic acid and asiatic acid in the feces within 24 to 48 h. The results clearly demonstrated the pharmacokinetic advantage of a standardized extract of C. Asiatica, ECa 233, compared with a mixture of madecassoside and asiaticoside at an equivalent amount. Other minor constituents that naturally exist in ECa 233 appeared to positively modulate the pharmacokinetics of its major constituents, resulting in relatively better pharmacokinetic profiles than those from a mixture of pure compounds.


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