Caffeic Acid Derivatives Research Articles

Brief Communication: Caffeic Acid Derivatives and Polymethoxylated Flavonoids from Cat’s Whiskers (Orthosiphon stamineus) Form Stable Complexes with SARS-CoV Molecular Targets: An In silico Analysis

Cat’s whiskers or the ‘misai kucing’ is an herbal plant native to the Southeast Asian region. The polyphenol enriched leaf extract contains numerous medicinal properties of major pharmaceutical interest. In this study, selected cat’s whiskers polyphenols were screened computationally to predict the minimum binding affinities with severe acute respiratory syndrome coronavirus (SARS-CoV) molecular targets. Molecular docking analysis showed that the caffeic acid derivatives and polymethoxylated flavonoids from cat’s whiskers bound stably to the binding pocket regions of SARS-CoV molecular targets at – 4.2 to – 7.1 kcal/mol. Furthermore, these cat’s whiskers polyphenol-bound SARS-CoV complexes were held fairly strongly by hydrophobic interactions, hydrogen bonds, and electrostatic interactions at various extents.

Characterization of chemical constituents in Shuanghuanglian oral dosage forms by ultra-high performance liquid chromatography coupled with time-of-flight mass spectrometry.

Shuanghuanglian is a common traditional Chinese medicine prescription. It is an herbal formula composed of Lonicerae Japonicae Flos, Scutellariae Radix, and Forsythiae Fructus. A comprehensive understanding of Shuanghuanglian oral dosage forms components was obtained using a method based on ultra-high performance liquid chromatography coupled with time-of-flight mass spectrometry for the separation and characterization of Shuanghuanglian oral liquids, granules, soft capsules, and effervescent tablets. A total of 358 components were chemically defined or tentatively identified, including flavonoids, caffeic acid derivatives, lignans, coumarins, iridoids, triterpenes, and anthraquinones. The results will provide a basis for the general study of Shuanghuanglian and be meaningful for the composition identification of traditional Chinese medicine prescriptions.

Mint (Mentha spp.) Honey: Analysis of the Phenolic Profile and Antioxidant Activity.

The composition of honey is influenced by the botanical source and geographical area of the nectar from which it is derived. Unifloral honeys reach higher market value than multifloral honeys due to their specific aromas, which result from volatile and phenolic compounds. The aim of our study is to characterize the phenolic composition of a rare unifloral variety of honey - mint (Mentha spp.) honey. For this purpose, we performed standard physicochemical analyses, pollen analysis, determined total phenolic and flavonoid content, analysed antioxidant activity and performed qualitative and quantitative analyses of phenolic compounds for five mint honeys. Our results indicate that mint honey samples have high phenolic content, expressed in gallic acid equivalents, from (76.7±0.6) to (90.1±1.1) mg/100 g, and flavonoid content, expressed as quercetin equivalents, from (6.7±0.6) to (12.5±0.8) mg/100 g. These honey samples also exhibit strong antioxidant activity, expressed as Trolox equivalents, from (33.6±2.8) to (51.3±1.2) mg/100 g and from (14.4±0.8) to (55.1±2.4) mg/100 g when analysed with DPPH and ABTS assays, respectively. Quantitative LC-MS/MS analysis revealed that the most abundant phenols in all samples were chrysin, apigenin and p-coumaric acid. Qualitative LC-MS/MS analysis identified the presence of kaempferide, diosmetin, acacetin and several caffeic acid derivatives. Our study indicates that mint honey contains unique phenolic profiles, which likely contribute to its distinctive aroma and strong antioxidant activity. A detailed description of the rare honey varieties gives beekeepers greater visibility and easier access to the demanding natural product market.

Russian market of fermented kombucha beverages

Fermented beverages based on kombucha contain a wide range of minor biologically active substances (flavonoids, caffeic acid derivatives, B vitamins, and others). The inclusion of these beverages in the diet helps to increase its nutritional value due to the content of biologically active substances, including essential ones. To develop beverages (kombucha) with a certain content of biologically active substances, it is necessary to study the composition of these products sold on the Russian market. The aim of the work was to analyze the Russian market of fermented beverages based on kombucha. Material and methods. More than 100 different marketed products were selected, positioned as non-alcoholic fermented beverages based on kombucha. Results. It was revealed that black tea (~28%), green tea (~24%) and Blooming Sally (~13%) are most often used as the basis for kombucha. In other cases, various types of tea, coffee, as well as special varieties of tea are used. Sugar (~55%), stevia extract (~24%), as well as honey, fructose, glucose-fructose syrup are used as sweeteners. The formation of the flavor profile of kombucha is achieved by using additional ingredients. A variety of fruits (lemon, orange, mango, apple, etc.), vegetables (cucumber, beetroot, etc.), berries (cranberries, lingonberries, chokeberry, raspberries, etc.) are used in the form of juices or purees; herbs and spices (mint, nutmeg, star anise, cloves, lavender, vanilla, etc.), as well as functional ingredients (vitamins, prebiotics, probiotics, chlorophyll) are applied as such additives. Conclusion. The analysis of the range of fermented drinks (kombucha) marketed in trading network was carried out. A list of main and auxiliary ingredients has been formed to assess the possibility of using these drinks to modify eating patterns.

Сравнительный фитохимический анализ настоев травы манжетки обыкновенной и травы манжетки мягкой

The research data revealed the existence of various pharmacological effects of Alchemilla vulgaris herb infusions and confirmed the prospects of introducing these infusions into medical practice. Biologically active substances (BAS) in the Alchemilla herb are of high variability, which adversely affects the phytochemical composition of the infusion and its pharmacological properties. The expansion of the raw material base of Alchemilla is possible due to Alchemilla mollis, which is a micro-specie with a stable chemical composition. Objective: a comparative analysis of the phytochemical composition of infusions of A. mollis and A. vulgaris herbs to assess the possibility of expanding the raw material base of the aerial part due to the cultivated micro-specie A. mollis. Materials and Methods. The objects of the study are A. vulgaris herb infusion (AVI) and A. mollis herb infusion (AMI). The harvesting of raw materials was being produced during the period of mass flowering from cultivated Alchemilla mollis (Buuser) Rothm and wild-growing Alchemilla vulgaris L. s. I. Preliminary qualitative analysis was performed by conventional methods. The content of tannins, polysaccharides, ascorbic acid, and flavonoids were quantified. Results. A preliminary qualitative analysis showed the similarity of the studied infusions, including the presence of phenolic compounds, markers of the genus Alchemilla (caffeic acid, luteolin and quercetin derivatives). The peculiarity of AMI is the predominant content of condensed tannins, which is consistent with the data on the accumulation of this group of biologically active substances in A. mollis herb. Significant higher amounts of tannins (p<0.05) and ascorbic acid (p<0.05) were found in BAS; no differences were found in the amount of polysaccharides and flavonoids. Conclusion. The conducted study indicates the similarity of the chemical composition of the studied infusions, which allows the use of AMI similarly to AVI, and A. mollis herb to expand the raw material base of the herb.

Synthesis of Caffeic Acid Derivatives: Identification of (E)-N-(4-Cyanobenzyl)-3-(3,4-dihydroxyphenyl)acrylamide as an Anticancer Agent against Human Cervical Cancer Cells

A novel series of natural compound-caffeic acid derivatives were synthesized by coupling with different substituted amines and alkyl halides in an effort to enhance the anticancer activity and explore the structure-activity relationship. The structures of the compounds were determined by 1H NMR and mass spectroscopy analysis. Compounds were evaluated for inhibition against HeLa-cervical cancer cell proliferation and results revealed that compound (E)-N-(4-cyanobenzyl)-3-(3,4- dihydroxyphenyl)acrylamide (SHC5) exhibited potent antiproliferative activity with 5.2 μM concentration and it is further confirmed by Hoechst/PI double staining and Annexin V/PI double staining assay. Further, compound SHC5 was screened against other cancer cell lines namely K562, Jurkat, HCT116 and MiaPaCa2 to test the specificity of the molecule and found to be ineffective.

Design and synthesis of caffeic acid derivatives and evaluation of their inhibitory activity against Pseudomonas aeruginosa

Design and synthesis of caffeic acid derivatives and evaluation of their inhibitory activity against Pseudomonas aeruginosa

Chemical analysis of some Ocimum basilicum medicinal teas

Objectives. Ocimum basilicum is one of the widespread medicinal plants, widely used due to its multiple therapeutic properties (antimicrobial, antiviral, hypoglycemic, antispasmodic, anti-inflammatory, carminative, stomachic, antioxidant, analgesic, etc.), as well as its specific aromatic character. The aim of this study was to comparatively investigate the chemical composition (flavonoids, caffeic acid derivatives, tannins, essential oil) of the aerial parts of some Romanian medicinal teas of Ocimum basilicum. Materials and methods. The content of flavonoids, phenolic acids and tannins in three samples of O. basilicum tea were determined spectrophotometrically. Identification of important phenolic compounds (rutin, isoquercitrin chlorogenic acid and caffeic acid) was performed by thin layer chromatography (TLC). The essential oils were obtained by hydrodistillation method. Outcomes and conclusions. Following the quantitative determinations performed, it can be seen that the basil samples are rich in active principles, and their use for the treatment of some diseases can be justified.

Polyscias filicifolia (Araliaceae) Hairy Roots with Antigenotoxic and Anti-Photogenotoxic Activity.

Hairy root cultures are considered as a valuable source of bioactive phytoconstituents with expanding applicability for their production. In the present study, hairy root cultures of Polyscias filicifolia (Araliaceae), a traditional Southeast Asian medicinal plant, were established. The transformation with Agrobacterium rhizogenes ATCC 15834 allowed to obtain 15 root lines. The K-1 line, demonstrating the highest growth capabilities, was subjected to further investigations. To enhance the biosynthetic potential of hairy roots, methyl jasmonate elicitation approach was applied (MeJA; at different doses and exposure time), with subsequent transfer of elicited roots to control medium. This strategy resulted in chlorogenic acid production up to 1.59 mg/g dry weight. HPLC-PDA-ESI-MS analysis demonstrated variation in extracts composition and allowed to identify different caffeic and ferulic acid derivatives. Next, cytotoxic, antigenotoxic, and anti-photogenotoxic properties of hairy roots extracts were determined. None of the tested extracts were cytotoxic. In addition, they demonstrated significant antigenotoxic activity with the highest protective potential; up to 52% and 49% of inhibition of induction ratio (IR) induced by the 2-aminoanthracene was revealed for extracts derived from hairy roots elicited for 3 days with 50 µM MeJA and roots elicited for 7 days with 100 µM MeJA and then transferred for 30 days to control medium, respectively. These same extracts exhibited the highest anti-photogenotoxic potential, up to 36% of inhibition of chloropromazine-induced genotoxicity.

Tentative qualitative and quantitative analysis of phenolic compounds in leaf extract from Carica papaya Linn. plant growing in Uganda

Summary Introduction Carica papaya L. belongs to Caricaceae family. It is an evergreen tree or shrub with usually unbranched trunk. Previous studies on the methanolic leaf extract of this plant proved the antibacterial, cytotoxic, anticancer and antioxidant effects indicative of promising therapeutic potentials. Methods Chromatographic and spectroscopic techniques along with high performance liquid chromatography quantitative analysis were performed to isolate, tentatively identify and quantify polyphenolic compounds in MeOH extract of C. papaya leaves. UHPLC-DAD-ESI-MS/MS and UHPLC-DAD methods were adopted for qualitative and quantitative analysis respectively. In the case of polyphenol separation, some reference substances were isolated by preparative HPLC. Results Six polyphenols were isolated and quantified from C. papaya leaf extract, including three phenolic acids: derivatives of caffeic acid, p-coumaric acid, ferulic acid and three flavonoids: quercetin dirhamnosylhexoside, kaempferol dirhamnosyl-hexoside, quercetin 3-O-rutinoside. Among them quercetin dirhamnosyl-hexoside was significantly higher (1.9 mg/g extract) than other identified compounds. Conclusion The results of present study provide a new data on polyphenols composition of C. papaya plant derived from Uganda and promote research on its possible standardization and use as a dietary supplement and/or herbal medicine.

Ilex paraguariensisA. St.-Hil. (Yerba Mate) Differently Regulates the Lipid Mobilization and, Irisin and Lactate Levels in Sedentary and Chronic Swimming Mice

Healthy mice were submitted or not to daily chronic swimming and/or daily yerba mate (YM) infusion intake and had their bloods analyzed after four weeks. We hypothesized that daily intake of YM may act differently on lipid mobilization and, on the creatine, lactate and irisin levels in sedentary mice and those submitted to chronic exercise. The groups were (n=48): YM-non-treated control (NTC), YM-non-treated swimming control (NSC), non-roasted YM (NRY), roasted YM (RY), swimming plus non-roasted YM (SNRY), swimming plus roasted YM (SRY). No significant (P>0.05) difference was observed concerning creatine phosphoskinase (CPK) value. Lactate level decreased significantly (P<0.05) for SNRY and SRY, suggesting accelerated lipid mobilization and glycogen sparing potential. There was significant (P<0.05) body weight loss in all, except for NTC. Higher weight loss in NRY, RY, SNR and SRY indicated greater lipid mobilization. Thiobarbituric acid reactive substances (TBARS) and irisin had significantly (P<0.05) higher values for RY. This is first report that deals with the effect of YM consumption on serum irisin level. Major amounts of caffeic acid derivatives, slightly increased caffeine and less amount of rutin may be responsible by accelerated lipoperoxidation in sedentary healthy mices chronically treated with roasted YM. Chronically consumed YM plus swimming aid in healthy weight loss. Sedentary lifestyle plus roasted YM chronic consumption may cause accelerated lipid mobilization and increased TBARS production via irisin overexpression leading to an increase in lipoperoxidation.

The Effect of Hydrothermal Treatment on Metabolite Composition of Hass Avocados Stored in a Controlled Atmosphere.

Avocado cv. Hass consumption has expanded worldwide given its nutritional, sensory, and functional attributes. In this work, avocado fruit from two harvests was subjected to hydrothermal treatment (38 °C for 1 h) or left untreated (control) and then stored for 30 and 50 days in a controlled atmosphere (4 kPa O2 and 6 kPa CO2 at 7 °C) (HTCA and CA, respectively) with subsequent ripening at ~20 °C. The fruit was evaluated for primary and secondary metabolites at harvest, after storage, and after reaching edible ripeness. A decrease from harvest to edible ripeness in mannoheptulose and perseitol was observed while β-sitosterol, hydrophilic and lipophilic antioxidant activity (H-AOX, L-AOX), abscisic acid, and total phenolics (composed of p-coumaric and caffeic acids such as aglycones or their derivatives) increased. HTCA fruit at edible ripeness displayed higher contents of mannoheptulose, perseitol, β-sitosterol, L-AOX, caffeic acid, and p-coumaric acid derivatives, while CA fruit presented higher contents of α-tocopherol, H-AOX, and syringic acid glycoside for both harvests and storage times. The results indicate that a hydrothermal treatment prior to CA enables fruit of high nutritional value characterized by enhanced content of phenolic compounds at edible ripeness to reach distant markets.

Red Clover HDT, a BAHD Hydroxycinnamoyl-Coenzyme A:L-3,4-Dihydroxyphenylalanine (L-DOPA) Hydroxycinnamoyl Transferase That Synthesizes Clovamide and Other N-Hydroxycinnamoyl-Aromatic Amino Acid Amides.

Red clover leaves accumulate high levels (up to 1 to 2% of dry matter) of two caffeic acid derivatives: phaselic acid (2-O-caffeoyl-L-malate) and clovamide [N-caffeoyl-L-3,4-dihydroxyphenylalanine (L-DOPA)]. These likely play roles in protecting the plant from biotic and abiotic stresses but can also help preserve protein during harvest and storage of the forage via oxidation by an endogenous polyphenol oxidase. We previously identified and characterized, a hydroxycinnamoyl-coenzyme A (CoA):malate hydroxycinnamoyl transferase (HMT) from red clover. Here, we identified a hydroxycinnamoyl-CoA:L-DOPA hydroxycinnamoyl transferase (HDT) activity in unexpanded red clover leaves. Silencing of the previously cloned HMT gene reduced both HMT and HDT activities in red clover, even though the HMT enzyme lacks HDT activity. A combination of PCR with degenerate primers based on BAHD hydroxycinnamoyl-CoA transferase sequences and 5′ and 3′ rapid amplification of cDNA ends was used to clone two nearly identical cDNAs from red clover. When expressed in Escherichia coli, the encoded proteins were capable of transferring hydroxycinnamic acids (p-coumaric, caffeic, or ferulic) from the corresponding CoA thioesters to the aromatic amino acids L-Phe, L-Tyr, L-DOPA, or L-Trp. Kinetic parameters for these substrates were determined. Stable expression of HDT in transgenic alfalfa resulted in foliar accumulation of p-coumaroyl- and feruloyl-L-Tyr that are not normally present in alfalfa, but not derivatives containing caffeoyl or L-DOPA moieties. Transient expression of HDT in Nicotiana benthamiana resulted in the production of caffeoyl-L-Tyr, but not clovamide. Coexpression of HDT with a tyrosine hydroxylase resulted in clovamide accumulation, indicating the host species’ pool of available amino acid (and hydroxycinnamoyl-CoA) substrates likely plays a major role in determining HDT product accumulation in planta. Finally, that HDT and HMT proteins share a high degree of identity (72%), but differ substantially in substrate specificity, is promising for further investigation of structure-function relationships of this class of enzymes, which could allow the rational design of BAHD enzymes with specific and desirable activities.

Akkermansia muciniphila in inflammatory bowel disease and colorectal cancer.

Akkermansia muciniphila in inflammatory bowel disease and colorectal cancer.

Calystegia soldanella Extract Exerts Anti-Oxidative and Anti-Inflammatory Effects via the Regulation of the NF-κB/Nrf-2 Pathways in Mouse Macrophages.

Plant polyphenols are widely used to treat various inflammatory diseases, owing to their ability to suppress reactive oxygen species production and the expression of inflammatory cytokines. Herein, we investigated phenolic compounds from Calystegia soldanella using UPLC Q-TOF MS/MS and their antioxidative and anti-inflammatory activities were analyzed. The C. soldanella ethyl acetate fraction (CsEF) had the strongest antioxidative activity, given its high polyphenol compound content. It also exhibited anti-inflammatory effects, inhibiting the production of inflammatory cytokines such as NO, PGE2, IL-1β, IL-6, and TNF-α in LPS-stimulated mouse macrophages. CsEF activated the nuclear transcription factor Nrf-2, thereby upregulating antioxidant enzymes such as HO-1 and NQO-1 and inhibiting NF-κB expression, which in turn, suppressed the expression of COX-2, iNOS, and inflammatory cytokines, ultimately exerting anti-inflammatory effects. Further, UPLC-Q-TOF-MS/MS was used to analyze the polyphenol compound contents in CsEF. The quercetin glycosides isoquercitrin and quercitrin were the primary flavonoid compounds, while the caffeic acid derivatives, chlorogenic acid and dicaffeoylquinic acid, were the primary phenolic acids. Thus, C. soldanella, which had only a limited use thus far as a medicinal plant, may serve as a natural medicinal resource for treating inflammatory diseases.

Both Acidic pH Value and Binding Interactions of Tartaric Acid With α-Glucosidase Cause the Enzyme Inhibition: The Mechanism in α-Glucosidase Inhibition of Four Caffeic and Tartaric Acid Derivates.

The inhibition mechanism of four caffeic and tartaric acid derivates, including caffeic acid (CA), tartaric acid (TA), caftaric acid (CFA) and chicoric acid (CHA) against α-glucosidase was characterized by substrate depletion, fluorescence quenching, isothermal titration calorimetry (ITC) and molecular docking. TA and CA were found with the highest and no inhibition effect respectively, and caffeoyl substitution at 2 and/or 3-OH of TA significantly decreased its inhibition. The enzyme inhibition effects of organic acids were not in an inhibitor concentration-dependent mode, and there was a rush increase in inhibition at a respective acidic pH value, especially for CFA and CHA, suggesting the important role of acidic pH in the enzyme inhibition for both compounds. Besides, CA, CFA and CHA were shown with strong quenching effects on α-glucosidase fluorescence because of π-conjugations between aromatic ring of caffeoyl moiety and that of enzyme fluorescent residues. However, no fluorescence quenching effect was observed for TA due to lack of aromatic ring. Additionally, a direct binding interaction behavior was observed for TA with α-glucosidase according to the fitted independent binding model in ITC, but not for CFA and CHA. Therefore, both acidic pH and binding interactions of TA with α-glucosidase resulted in the enzyme inhibition.

Elicitor-induced phenolic acids accumulation in Salvia virgata Jacq. hairy root cultures

Phenolic acids, as the predominant secondary metabolites of Salvia plants, are largely used in pharmaceutical industries. The main aim of the study was to establish hairy root cultures of Salvia virgata Jacq. Also, the effects of methyl jasmonate (22.4 and 11.2 ppm), Ag+ ions (5 and 2.5 ppm) and yeast extract (100 and 50 ppm) were assessed on total phenol, total flavonoid, rosmarinic acid and salvianolic acid A contents in the hairy roots after 1, 3 and 5 days of exposure. Results showed that Agrobacterium rhizogenes strains (A4, ATCC15834, R1000, GM1534 and C58C1) had different potential to induce hairy roots on leaf explants. The transformed roots were molecularly confirmed using rolC gene, and the highest transformation frequency (56%) was obtained by ATCC15834 strain. Among the established hairy root lines, the highest amount of rosmarinic acid (0.45 ± 0.01 mg/g DW) and dry root biomass (2.29 ± 0.04 g) was obtained in AT3, the line which was induced by ATCC15834 strain. The maximum accumulation of total phenol (123.6 ± 0.93 mg GAE/g DW), total flavonoid (5.09 ± 0.07 mg QUE/g DW), rosmarinic acid (18.45 ± 0.8 mg/g DW) and salvianolic acid A (2.11 ± 0.04 mg/g DW) was observed in the hairy roots elicited with 22.4 ppm methyl jasmonate on day three after treatment. The results support that elicitation could be an effective procedure for the improvement of caffeic acid derivatives production in S. virgata hairy root cultures. The results of this study approved that the application of elicitors is an effective procedure for the stimulation of phenolic acids production in the hairy root cultures of Salvia virgata Jacq.

Hyphenated LC-ABTS·+ and LC-DAD-HRMS for simultaneous analysis and identification of antioxidant compounds in Astragalus emarginatus Labill. extracts

The compounds in leaf and stem extracts of Astragalus emarginatus Labill. (AEL), a plant species used in traditional Lebanese medicine, were investigated for antioxidant properties. First, the activity of various extracts was assessed using the Trolox equivalent antioxidant capacity, oxygen radical absorption capacity, and 2,2-diphenyl-1-picryl-hydrazyl-hydrate assays. The extract obtained using 30% ethanol showed the greatest activity. The antioxidant compounds in this extract were screened using a hyphenated high-performance liquid chromatography-2,2-azinobis-(3-ethylbenzothiazoline-6-sulfonate) radical (ABTS·+) system before being separated by ultra-high-performance liquid chromatography and identified using high-resolution mass spectrometry and ultra-violet-visible diode array detection. Approximately 40 compounds were identified. Hydroxycinnamates (caffeic, ferulic, and p-coumaric acid derivatives) and flavonoids (quercetin, luteolin, apigenin, and isorhamnetin derivatives) were the two main categories of the identified compounds. The active compounds were identified as caffeic acid derivatives and quercetin glycosides. In addition, the catechol moiety was shown to be key to antioxidant activity. This study showed that AEL is a source of natural antioxidants, which may explain its medicinal use.

The contribution of phenolics to the anti-inflammatory potential of the extract from Bolivian coriander (Porophyllum ruderale subsp. ruderale)

Porophyllum ruderale subsp. ruderale is a food product used for seasoning in Central and Southern America. The present research aimed to investigate the chemical composition of an extract prepared from aerial parts of P. ruderale using UHPLC-DAD-MS/MS, to isolate and identify major natural products present in the extract, and to furtherly investigate their anti-inflammatory activity in vitro. Twenty-five compounds were detected and characterized using UV–Vis and MS data. All characterized compounds were quantified. Ten major phenolics were isolated and identified by NMR. One previously undescribed natural product was isolated and established as 1-O-(4-hydroxy-3,5-dimethoxy)benzoyl-6-O-galloyl-β-d-glucose (12). Anti-inflammatory activity was evaluated based on the influence of the extract and isolated compounds on the TLR4-dependent secretion of IL-8 and TNF-α by human primary neutrophils in vitro. Phenolic acids, and caffeic acid derivatives in particular, contributed to the extract's bioactivity.

In Vitro Tests for a Rapid Evaluation of Antidiabetic Potential of Plant Species Containing Caffeic Acid Derivatives: A Validation by Two Well-Known Antidiabetic Plants, Ocimum gratissimum L. Leaf and Musanga cecropioides R. Br. ex Tedlie (Mu) Stem Bark.

Plant bioactive extracts represent a major resource for identifying drugs and adjuvant therapy for type 2 diabetes. To promote early screening of plants’ antidiabetic potential, we designed a four in vitro tests strategy to anticipate in vivo bioactivity. Two antidiabetic plants were studied: Ocimum gratissimum L. (Oc) leaf extract and Musanga cecropoides R. Br. ex Tedlie (Mu) stem bark extract. Chemical compositions were analyzed by LCMS and HPLC. Antidiabetic properties were measured based on (1) INS-1 cells for insulin secretion, (2) L6 myoblast cells for insulin sensitization (Glut-4 translocation), (3) L6 myoblast cells for protection against hydrogen peroxide (H2O2) oxidative stress (cell mortality), and (4) liver microsomial fraction for glucose-6-phosphastase activity (G6P). Oc extract increased insulin secretion and insulin sensitivity, whereas it decreased oxidative stress-induced cell mortality and G6P activity. Mu extract decreased insulin secretion and had no effect on insulin sensitivity or G6P activity, but it increased oxidative stress-induced cell mortality. Results were compared with NCRAE, an antidiabetic plant extract used as reference, previously characterized and reported with increased insulin secretion and insulin sensitivity, protection against oxidative stress, and decreased G6P activity. The proposed set of four in vitro tests combined with chemical analysis provided insight into the interest in rapid early screening of plant extract antidiabetic potential to anticipate pharmaco-toxicological in vivo effects.