Flavanol Polymerization Is a Superior Predictor of α-Glucosidase Inhibitory Activity Compared to Flavanol or Total Polyphenol Concentrations in Cocoas Prepared by Variations in Controlled Fermentation and Roasting of the Same Raw Cocoa Beans

Raw cocoa beans were processed to produce cocoa powders with different combinations of fermentation (unfermented, cool, or hot) and roasting (not roasted, cool, or hot). Cocoa powder extracts were characterized and assessed for α-glucosidase inhibitory activity in vitro. Cocoa processing (fermentation/roasting) contributed to significant losses of native flavanols. All of the treatments dose-dependently inhibited α-glucosidase activity, with cool fermented/cool roasted powder exhibiting the greatest potency (IC50: 68.09 µg/mL), when compared to acarbose (IC50: 133.22 µg/mL). A strong negative correlation was observed between flavanol mDP and IC50, suggesting flavanol polymerization as a marker of enhanced α-glucosidase inhibition in cocoa. Our data demonstrate that cocoa powders are potent inhibitors of α-glucosidase. Significant reductions in the total polyphenol and flavanol concentrations induced by processing do not necessarily dictate a reduced capacity for α-glucosidase inhibition, but rather these steps can enhance cocoa bioactivity. Non-traditional compositional markers may be better predictors of enzyme inhibitory activity than cocoa native flavanols.

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EVALUASI AKTIVITAS INHIBISI XANTIN OKSIDASE DAN KANDUNGAN SENYAWA POLIFENOL DARI EKSTRAK SAPPAN

Jurnal Bioteknologi & Biosains Indonesia (JBBI) ◽

10.29122/jbbi.v5i2.2880 ◽

2018 ◽

Vol 5 (2) ◽

pp. 157

Author(s):

Sri Ningsih ◽

. Churiyah

Keyword(s):

Uric Acid ◽

Xanthine Oxidase ◽

Inhibitory Activity ◽

Ethanolic Extract ◽

Polyphenol Content ◽

Total Polyphenol ◽

Caesalpinia Sappan ◽

Total Polyphenol Content

Evaluation of xanthine oxidase inhibitory activity and polyphenolic content of sappan extractABSTRACTHyperuricemia is a disease that is characterized by a high uric acid level, in which the number of patients tends to increase every year. This research was intended to evaluate the xanthine oxidase (XO) inhibitory activity and determinate the total polyphenol content of heartwood sappan (Caesalpinia sappan L.) extract. The extract was prepared by macerating the dry powder wood using 70% ethanol at room temperature. The quality of ethanolic extract obtained was evaluated based on BPOM guideline. XO inhibitory power was determined by measuring uric acid produced in the xanthine/XO system in vitro. The polyphenol content of the extract was measured using Folin-Ciocalteu reagent spectrophotometrically. The results showed that the quality of sappan semisolid extract fulfilled the required standard. Sappan extract inhibited XO activity by 98% relative to the positive control, allopurinol, at the final extract concentration of 100 µg/mL. The total polyphenol content was 26% of the crude extract. It could be concluded that sappan ethanolic extract has the potential to be developed as an ingredient for hyperuricemia treatment.Keywords: hyperuricemia, sappan, total polyphenol, xanthine, xanthine oxidase ABSTRAKHiperurisemia adalah penyakit yang dicirikan dengan kadar asam urat tinggi dimana prevalensi penderita cenderung meningkat. Penelitian ini bertujuan untuk mempelajari aktivitas esktrak kayu sappan (Caesalpinia sappan L.) dalam menginhibisi enzim XO (xantin oksidase) secara in vitro dan penentuan kadar senyawa polifenol total yang terkandung di dalamnya. Ekstrak dibuat dengan cara maserasi serbuk kayu menggunakan pelarut etanol 70% pada suhu kamar. Kualitas ekstrak dievaluasi mengacu pada parameter karakterisasi ekstrak yang ditetapkan oleh BPOM. Aktivitas inhibisi XO ditetapkan dengan mengukur kadar asam urat yang terbentuk pada sistem xantin/XO in vitro. Kadar polifenol ekstrak diukur menggunakan pereaksi Folin-Ciocalteu secara spektrofotometri. Hasil analisis menyatakan bahwa kualitas ekstrak kental sappan memenuhi persyaratan yang ada. Pengujian inhibisi XO dengan pembanding positif allopurinol pada konsentrasi akhir ekstrak sebesar 100 µg/mL menunjukkan bahwa ekstrak mempunyai kekuatan menginhibisi XO sebesar 98% relatif terhadap pembanding positif allopurinol. Kadar senyawa polifenol total dalam ekstrak sappan sebesar 26% dari ekstrak kasar. Dari penelitian ini dapat disimpulkan bahwa ekstrak sappan mempunyai potensi untuk dikembangkan sebagai bahan untuk mengatasi hiperurisemia.Kata Kunci: hiperurisemia, polifenol total, sappan, xantin, xantin oksidase

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Thrombin Activity by Intrinsic Activation of Plasma In-Vitro Accelerates with Increasing Age of the Donor

Thrombosis and Haemostasis ◽

10.1055/s-0038-1648450 ◽

1992 ◽

Vol 67 (03) ◽

pp. 377-380 ◽

Cited By ~ 16

Author(s):

S H Ibbotson ◽

G M Tate ◽

J A Davies

Keyword(s):

Negative Correlation ◽

Maximal Activity ◽

Significant Negative Correlation ◽

Older Individuals ◽

Contact Activation ◽

Strong Negative Correlation ◽

Thrombin Activity ◽

Plasma Donor ◽

Thrombotic Diseases

SummaryThrombotic diseases increase in incidence with advancing years and this might be partly due to an increased propensity for fibrin formation in older individuals. Accordingly we decided to investigate whether the time taken to generate 50% thrombin activity in vitro varied with the age of the plasma donor. Coagulation was initiated in defibrinated, diluted plasma by contact activation and thrombin activity measured using the chromogenic substrate, S2238. The rate of thrombin generation was assessed by measuring the time taken to reach 50% maximal activity (T50/s). There was a highly significant negative correlation between T50 and age, T50 declining from 93 s at 19 years to 71 s at 65 years (r = −0.637, p <0.0001). A strong negative correlation was demonstrated between T50 and FVII level (r = -0.415, p = 0.0007) and FVIII: C level (r = -0.465, p = 0.0001). Although FVII concentration correlated with age (r = 0.307, p = 0.014) no relationship was seen between age and FVIII :C. These data suggest that coagulation rates in plasma accelerate with age.

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Utilization of a Model Cocoa Fermentation System and Roasting to Assess Differences Among Bioactive Compounds and Bioactivity of Cocoa Through Variable Processing Conditions (FS07-04-19)

Current Developments in Nutrition ◽

10.1093/cdn/nzz040.fs07-04-19 ◽

2019 ◽

Vol 3 (Supplement_1) ◽

Author(s):

Kathryn Racine ◽

Brian Wiersema ◽

Andrew Lee ◽

Laura Griffin ◽

Lauren Essenmacher ◽

...

Keyword(s):

Degree Of Polymerization ◽

Control Treatment ◽

Cocoa Bean ◽

Cocoa Beans ◽

Cocoa Powder ◽

Funding Sources ◽

Food Research ◽

The Impact

Abstract Objectives Cocoa beans (Theobroma cacao) are a highly concentrated source of dietary flavanols that undergo processing steps, to enhance sensory characteristics. Although it is widely accepted that preservation of native cocoa flavanols is critical for retaining bioactivity, it is possible that reactions occurring throughout cocoa processing may generate compounds with novel activities, potentially preserving or enhancing bioactivity. Our objective was to evaluate the impact of fermentation and roasting on levels of flavanols and bioactivity of cocoa. Methods Combinations of fermentation and roasting parameters were employed via a controlled laboratory fermentation model system and roasting operation. Cocoa powders were produced from unfermented cocoa beans using different treatments representing extremes of fermentation and roasting. Cocoa beans were fermented in a simulated pulp media for 168 h. Fermentation and roasting temperatures varied depending on treatment group. Further processing (winnowing, grinding, pressing) produced cocoa powders for each treatment. Extracts were made from the final beans and powders. Total polyphenols were quantified by the Folin-Ciocalteu assay. HILIC UPLC-MS/MS was employed to analyze flavanols based on their degree of polymerization (DP). Results Fermentation and roasting contributed to losses of native flavanols. Total polyphenol levels and individual flavanols (DP 1–10) were approximately 27–90% lower in hot fermented/hot roasted cocoa powder and approximately 11–54% lower in cool fermented/cool roasted cocoa powder when compared to the unfermented/unroasted (control) treatment. Hot roasting had the most significant impact on flavanol degradation. There was also a direct relationship between increasing flavanol concentration in cocoa powder and DP. Conclusions Compared to fermentation, roasting demonstrated a more significant impact on flavanol degradation and composition among cocoa bean treatments. Further research in vitro and in vivo is being performed currently to determine whether these process-induced flavanol losses correlate with reduced anti-obesity and anti-inflammatory activities. Funding Sources This work was supported by the Agriculture and Food Research Initiative (AFRI) of the US Department of Agriculture.

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Impact of roasting on the flavan-3-ol composition, sensory-related chemistry, and in vitro pancreatic lipase inhibitory activity of cocoa beans

Food Chemistry ◽

10.1016/j.foodchem.2018.02.036 ◽

2018 ◽

Vol 255 ◽

pp. 414-420 ◽

Cited By ~ 9

Author(s):

Todd H. Stanley ◽

Charlene B. Van Buiten ◽

Scott A. Baker ◽

Ryan J. Elias ◽

Ramaswamy C. Anantheswaran ◽

...

Keyword(s):

Pancreatic Lipase ◽

Inhibitory Activity ◽

Cocoa Beans

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Change in stability of procyanidins, antioxidant capacity and in-vitro bioaccessibility during processing of cocoa powder from cocoa beans

LWT ◽

10.1016/j.lwt.2016.04.065 ◽

2016 ◽

Vol 72 ◽

pp. 559-565 ◽

Cited By ~ 20

Author(s):

Mine Gültekin-Özgüven ◽

Ijlal Berktaş ◽

Beraat Özçelik

Keyword(s):

Antioxidant Capacity ◽

Cocoa Beans ◽

Cocoa Powder ◽

In Vitro Bioaccessibility

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IN VITRO SCREENING OF ACTINIOPTERIS DICHOTOMA FOR ENZYME INHIBITORY ACTIVITY RELATED TO TYPE 2 DIABETES

INDIAN DRUGS ◽

10.53879/id.53.06.10505 ◽

2016 ◽

Vol 53 (06) ◽

pp. 70-73

Author(s):

M Telagari ◽

◽

K. K. Hullatti

Keyword(s):

Type 2 Diabetes ◽

Inhibitory Activity ◽

Skin Diseases ◽

In Vitro Screening ◽

Glucosidase Activity ◽

Ic50 Values ◽

Calculated Fraction

Actiniopteris dichotoma Mett. (Pteridaceae) is documented in Ayurveda for treatment of Prameha (Diabetes), Atisara and skin diseases. However, the antidiabetic properties of this plant have not been fully validated using scientific tools. The present study screens the A. dichotoma extract and fractions for enzyme inhibitory (α–amylase and α–glucosidase) activity related to type 2 diabetes. The extract was prepared using cold maceration followed by Soxhlation and finally fractionated the combined extracts. Different concentrations (0.1–0.5 mg/mL) of extract and four fractions were subjected to enzyme inhibitory assays. The absorbance was measured at 540 and 405 nm and IC50 values were calculated. Fraction 2 has shown highest α–amylase and α–glucosidase inhibitory activity, (IC50 values are 0.131 and 0.114 mg/mL) which was comparable with acarbose (0.125 and 0.093 mg/mL). Hence, further studies may throw light on the antidiabetic potential of A. dichotoma especially in the management of T2D.

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Simulated Gastrointestinal Digestion of Cocoa: Detection of Resistant Peptides and In Silico/In Vitro Prediction of Their Ace Inhibitory Activity

Nutrients ◽

10.3390/nu11050985 ◽

2019 ◽

Vol 11 (5) ◽

pp. 985 ◽

Cited By ~ 7

Author(s):

Angela Marseglia ◽

Luca Dellafiora ◽

Barbara Prandi ◽

Veronica Lolli ◽

Stefano Sforza ◽

...

Keyword(s):

Inhibitory Activity ◽

In Silico ◽

Internal Standard ◽

Gastrointestinal Digestion ◽

Ace Inhibitory Activity ◽

Cocoa Beans ◽

Vitro Assay ◽

Simulated Gastrointestinal Digestion ◽

Ace Inhibitory

In this study we investigated the oligopeptide pattern in fermented cocoa beans and derived products after simulated gastrointestinal digestion. Peptides in digested cocoa samples were identified based on the mass fragmentation and on the software analysis of vicilin and 21 KDa cocoa seed protein sequences, the most abundant cocoa proteins. Quantification was carried out by liquid chromatography/electrospray ionisation mass spectrometry (LC/ESI-MS) using an internal standard. Sixty five peptides were identified in the digested samples, including three pyroglutamyl derivatives. The in vitro angiotensin-converting enzyme (ACE)-inhibitory activity of cocoa digests were tested, demonstrating a high inhibition activity, especially for digestates of cocoa beans. The peptides identified were screened for their potential ACE inhibitory activity through an in silico approach, and about 20 di-, three- and tetra-peptides actually present in our samples were predicted as active. Two of the potentially active peptides were chemically synthesized and then assessed for their inhibitory activity by using the ACE in vitro assay. These peptides demonstrated an ACE inhibitory activity, however, that was too weak to explain alone the high activity of cocoa digestates, suggesting a synergic effect of all cocoa peptides. As a whole, results showed that an average chocolate portion (30 g) ensures an amount of peptides after digestion that, assuming complete absorption, could reach almost a complete inhibition of ACE.

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Inhibitory effects of bioaccessible anthocyanins and procyanidins from apple, red grape, cinnamon on α-amylase, α-glucosidase and lipase

International Journal for Vitamin and Nutrition Research ◽

10.1024/0300-9831/a000652 ◽

2020 ◽

pp. 1-9

Author(s):

Pınar Ercan ◽

Sedef Nehir El

Keyword(s):

Inhibitory Activity ◽

Digestive Enzymes ◽

Positive Control ◽

Anthocyanin Content ◽

Inhibitory Effects ◽

Total Anthocyanin ◽

Total Anthocyanin Content ◽

Before And After ◽

Red Grape

Abstract. The goals of this study were to determine and evaluate the bioaccessibility of total anthocyanin and procyanidin in apple (Amasya, Malus communis), red grape (Papazkarası, Vitis vinifera) and cinnamon (Cassia, Cinnamomum) using an in vitro static digestion system based on human gastrointestinal physiologically relevant conditions. Also, in vitro inhibitory effects of these foods on lipid (lipase) and carbohydrate digestive enzymes (α-amylase and α-glucosidase) were performed with before and after digested samples using acarbose and methylumbelliferyl oleate (4MUO) as the positive control. While the highest total anthocyanin content was found in red grape (164 ± 2.51 mg/100 g), the highest procyanidin content was found in cinnamon (6432 ± 177.31 mg/100 g) (p < 0.05). The anthocyanin bioaccessibilities were found as 10.2 ± 1%, 8.23 ± 0.64%, and 8.73 ± 0.70% in apple, red grape, and cinnamon, respectively. The procyanidin bioaccessibilities of apple, red grape, and cinnamon were found as 17.57 ± 0.71%, 14.08 ± 0.74% and 18.75 ± 1.49%, respectively. The analyzed apple, red grape and cinnamon showed the inhibitory activity against α-glucosidase (IC50 544 ± 21.94, 445 ± 15.67, 1592 ± 17.58 μg/mL, respectively), α-amylase (IC50 38.4 ± 7.26, 56.1 ± 3.60, 3.54 ± 0.86 μg/mL, respectively), and lipase (IC50 52.7 ± 2.05, 581 ± 54.14, 49.6 ± 2.72 μg/mL), respectively. According to our results apple, red grape and cinnamon have potential to inhibit of lipase, α-amylase and α-glucosidase digestive enzymes.

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