Chemistry of Advanced Materials 3(2) (2018) 36-59 Antioxidant, Anti-inflammatory and Neuroprotective Activities of a Plant Extract Derived from Traditional Chinese Medicine: SuHeXiang Wan (AT000)

International audienceIn this paper, we present SuHeXiang Wan, a medicine used in traditional Chinese medicine for the treatment of epilepsy and convulsions. We investigated the antioxidant, anti-inflammatory and neuroprotective activities of the same treatment designated as AT000. The synergy of the two plants, Dryobalanops aromatica and Saussurea lappa, of which the use in alimentary supplements is considered controversial, was evaluated for the first time. The antioxidant activity of the extract was assessed by DPPH and ORAC tests while the anti-inflammatory activity was determined by measuring the capacity of macrophages to generate a strong inflammatory response when stimulated with antigens, inducing NO release. The extract efficacy on the attenuation of the Aβ25-35-induced learning deficits (spatial working memory: spontaneous alternation in the Y-maze and contextual long-term memory: passive avoidance test) was evaluated in vivo in mice seven days after the peptide administration. The impact on lipid peroxidation in the hippocampus, an index of oxidative Chemistry of Advanced Materials (CAM) Journal homepage: http://issrpublishing.com/cam/ Iskandar et al., Chemistry of Advanced Materials 3(2) (2018) 36-59 37 stress, was also evaluated. AT000 extract showed a strong antioxidant activity at 2 mg/mL, 10 mg/mL and 301774 Trolox equivalents according to the DPPH and ORAC tests respectively. The 21-days AT000 treatment dose-dependently alleviated Aβ25-35-induced deficits, with significant prevention at the highest dose tested (250 mg/Kg/day) on the spontaneous alternation, step-through latency and escape latency parameter. 21-days AT000 treatment dose-dependently attenuated also Aβ25-35-induced increase lipid peroxidation, with a significant and complete blockade at the highest doses tested. Synergistic experiments showed that the presence of Dryobalanops aromatica and Saussurea lappa is crucial to obtain a neuroprotective effect. According to these results, AT000 could be a candidate compound in the development of therapeutic drugs for the prevention and treatment of Alzheimer's disease

Study of anti-inflammatory, antioxidant activities and screening by gas chromatography coupled to mass spectrometry of ethanolic extracts of three fabaceae of Benin : isolation of bioactive molecules

Face à la résurgence de pathologies infectieuses, notre étude a porté sur le potentiel thérapeutique de Dialium guineense, Parkia biglobosa et Tamarindus indica afin de rechercher des molécules bioactives pouvant contrer l’antibiorésistance ou ses corolaires. L’état de l’art des molécules bioactives des trois plantes a montré que de nombreuses familles de composés sont identifiées dans différents organes aériens. Toutefois le lien avec les activités biologiques reste non élucidé. Ensuite, nous avons évalué quelques activités biologiques des extraits éthanoliques ou hydro-éthanoliques des feuilles, fruits et écorces. Avec de bons taux de viabilité cellulaires, les extraits de D. guineense (écore) ainsi que ceux de P. biglobosa (feuilles) et T. indica (écorce) ont des ratios d’activités antiinflammatoires de 458,2 ; 161 et 174,6 respectivement. Ces valeurs sont supérieures à celle de la dexaméthasone utilisée comme témoin. Le test KRL a montré une activité antiradicalaire dose dépendante dans la gamme de 0 à 20mg/L. In vitro, 1g de chacun des extraits susmentionnés présente une capacité antioxydante respectivement équivalente à 1585 ; 2092 ; 5071 et 2246 mg de Trolox. Les extraits ont par la suite été analysés par GC-MS révélant pour la première fois la présence de lupéol et de sitostérol dans l’écorce de D. guineense. Enfin, l’étude nutritionnelle des trois fruits révèle, à travers les fortes teneurs en nutriments (80% de sucre pour D. guineense), leur possible contribution à la lutte contre la malnutrition au Bénin et la nécessité d’œuvrer à leur conservation.Mots-clés : Pathologies infectieuses, antibiorésistance, anti-inflammatoire, antioxydant, molécules bioactivesIn a context of infectious diseases resurgence, our study focused on therapeutic potential of Dialium guineense, Parkia biglobosa and Tamarindus indica in order to search for bioactive molecules that can counter antibiotic resistance or its corollaries. The state of the art of on bioactive molecules from the three plants has shown that many families of compounds are identified in different aerial organs. However, the link with biological activities remains unclear. Next, we evaluated some biological activities of ethanolic or hydroethanolic extracts of leaves, fruits and bark. With good cell viability levels, extracts of D. guineense (bark) as well as those of P. biglobosa (leaves) and T. indica (bark) have anti-inflammatory activity ratios of 458.2; 161 and 174.6 respectively. These values are higher than that of dexamethasone used as positive control. The KRL test showed dose-dependent antiradical activity in the range of 0 to 20mg / L. In vitro, 1 g of each of the abovementioned extracts has an antioxidant capacity respectively equivalent to 1585 ; 2092 ; 5071 and 2246 mg of Trolox. The extracts were then analyzed by GC-MS revealing for the first time the presence of lupeol and sitosterol in the bark of D. guineense. Finally, the nutritional study of the three fruits reveals, through the high levels of nutrients (80% sugar for D. guineense), their possible contribution to fight malnutrition in Benin and the need of their conservation. Keywords : Infectious diseases, antimicrobial resistance, anti-inflammatory, antioxidant, bioactive molecule

Antioxidant, Anti-inflammatory and Neuroprotective Activities of a Plant Extract Derived from Traditional Chinese Medicine SuHeXiang Wan (AT000)

International audienceIn this paper, we present SuHeXiang Wan, a medicine used in traditional Chinese medicine for the treatment of epilepsy and convulsions. We investigated the antioxidant, anti-inflammatory and neuroprotective activities of the same treatment designated as AT000. The synergy of the two plants, Dryobalanops aromatica and Saussurea lappa, of which the use in alimentary supplements is considered controversial, was evaluated for the first time. The antioxidant activity of the extract was assessed by DPPH and ORAC tests while the anti-inflammatory activity was determined by measuring the capacity of macrophages to generate a strong inflammatory response when stimulated with antigens, inducing NO release. The extract efficacy on the attenuation of the Aβ25-35-induced learning deficits (spatial working memory: spontaneous alternation in the Y-maze and contextual long-term memory: passive avoidance test) was evaluated in vivo in mice seven days after the peptide administration. The impact on lipid peroxidation in the hippocampus, an index of oxidative Chemistry of Advanced Materials (CAM) Journal homepage: http://issrpublishing.com/cam/ Iskandar et al., Chemistry of Advanced Materials 3(2) (2018) 36-59 37 stress, was also evaluated. AT000 extract showed a strong antioxidant activity at 2 mg/mL, 10 mg/mL and 301774 Trolox equivalents according to the DPPH and ORAC tests respectively. The 21-days AT000 treatment dose-dependently alleviated Aβ25-35-induced deficits, with significant prevention at the highest dose tested (250 mg/Kg/day) on the spontaneous alternation, step-through latency and escape latency parameter. 21-days AT000 treatment dose-dependently attenuated also Aβ25-35-induced increase lipid peroxidation, with a significant and complete blockade at the highest doses tested. Synergistic experiments showed that the presence of Dryobalanops aromatica and Saussurea lappa is crucial to obtain a neuroprotective effect. According to these results, AT000 could be a candidate compound in the development of therapeutic drugs for the prevention and treatment of Alzheimer's disease

Dialium guineense Willd. Parkia biglobosa (Jacq.) R. Br. Ex Benth. and Tamarindus indica L.: Review of known and synergetic bioactive compounds

International audienceNative from Africa, Dialium guineense Willd. Parkia biglobosa R. Br. Ex Benth. And Tamarindus indica L. grow in tropical regions, and are very widespread in West Africa, particularly in Benin. They are simultaneously used in the traditional healing of infectious diseases but there is a lack on their bioactive compounds description. This work places a special emphasis on inventory of known bioactives compounds from the three plants and their mechanism of action in order to identify the need for further research. It emerges from this work that numerous studies confirm the biological activities of the plants extracts. Nevertheless, few bioactive molecules are described as well as the mode of action of the active extracts

GC-MS screening and evaluation of the anti-inflammatory and antioxidant activities of ethanolic leaves and stem barks extracts from Dialium guineense Willd, Parkia biglobosa (Jacq.) R. Br. ex Benth. and Tamarindus indica L

International audienceInflammation has been shown to be greatly involved in the degenerative processes of human skin such as photo aging and atopy. Reduction of low-grade inflammatory reactions by topical products may be necessary in case of skin aggression, to obtain an optimal wound healing and restore the physiological balance of human skin. Present work evaluated the antioxidant, anti-inflammatory and phototoxic properties of ethanolic extracts from leaves and stem barks of Dialium guineense Willd., Parkia biglobosa (Jacq.) R. Br. Ex Benth. and Tamarindus indica L. The antioxidant power of the extracts, measured in vitro by the KRL method, showed that each gram of D. guineense bark extract, P. biglobosa leaves extract and T. indica bark and leaves extracts has an antioxidant capacity equivalent to 1585, 2092, 5071 and 2246 mg of Trolox respectively. Simultaneously with their actions on cell viability, the anti-inflammatory activity of the extracts was monitored measuring their effects on NO production by mouse macrophages submitted to LPS from E. coli to determine the anti-inflammatory ratio of each extract. The bark and leaves of D. guineense Willd., the leaves of P. biglobosa (Jacq.) R. Br. Ex Benth. and the bark of T. indica L. have anti-inflammatory ratios from 161 to 458.2, whereas Dexamethasone (positive control) has a ratio of 37.87. The in vitro 3T3 NRU test was used on mouse fibroblasts to determine the phototoxicity of the six extracts. Only D. guineense Willd. stem bark was photo-toxic with a photo-irritation factor greater than 5 (PIF = 8.39). Our study report some molecules such as lupeol, amaryn, sitosterol for the first time in the extracts and shows that the use of these plants in traditional medicine is justified

Synthesis and Evaluation of the Antibacterial Activities of 13-Substituted Berberine Derivatives

International audienceThe biological activities of berberine, a natural plant molecule, are known to be affected by structural modifications, mostly at position 9 and/or 13. A series of new 13-substituted berberine derivatives were synthesized and evaluated in term of antimicrobial activity using various microorganisms associated to human diseases. Contrarily to the original molecule berberine, several derivatives were found strongly active in microbial sensitivity tests against Mycobacterium, Candida albicans and Gram-positive bacteria, including naïve or resistant Bacillus cereus, Staphylococcus aureus and Streptococcus pyogenes with minimal inhibitory concentration (MIC) of 3.12 to 6.25 µM. Among the various Gram-negative strains tested, berberine's derivatives were only found active on Helicobacter pylori and Vibrio alginolyticus (MIC values of 1.5-3.12 µM). Cytotoxicity assays performed on human cells showed that the antimicrobial berberine derivatives caused low toxicity resulting in good therapeutic index values. In addition, a mechanistic approach demonstrated that, contrarily to already known berberine derivatives causing either membrane permeabilization, DNA fragmentation or interacting with FtsZ protein, active derivatives described in this study act through inhibition of the synthesis of peptidoglycan or RNA. Overall, this study shows that these new berberine derivatives can be considered as potent and safe anti-bacterial agents active on human pathogenic microorganisms, including ones resistant to conventional antibiotics