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.

Identification of potential inhibitors of SARS-CoV-2 main protease from Aloe vera compounds: A molecular docking study.

SARS-CoV-2 is the pathogen agent of the new corona virus disease that appeared at the end of 2019 in China. There is, currently, no effective treatment against COVID-19. We report in this study a molecular docking study of ten Aloe vera molecules with the main protease (3CLpro) responsible for the replication of coronaviruses. The outcome of their molecular simulation and ADMET properties reveal three potential inhibitors of the enzyme (ligands 6, 1 and 8) with a clear preference of ligand 6 that has the highest binding energy (-7.9 kcal/mol) and fully obeys the Lipinski's rule of five.

In vitro effects of anthocyanin extracts from Justicia secunda Vahl on the solubility of haemoglobin S and membrane stability of sickle erythrocytes.

BACKGROUND: Sickle cell disease or drepanocytosis is caused by the polymerisation of abnormal haemoglobin S when oxygen tension decreases. This lead to the changes in the shape of red blood cells and anaemia. It has also been postulated that the red cells of patients with sickle cell disease contain a higher than normal concentration of calcium ions. These ions are bound to membrane proteins resulting in dehydration and loss of red blood cell deformability and cell-to-cell adherence. Anthocyanins extracted from some Congolese plants used in traditional medicine against sickle cell disease have recently been shown to have anti-sickling activity in vitro. Justicia secunda is a plant used in Congo by Jehovah's Witnesses, well known for their refusal of blood transfusions, against anaemia. MATERIALS AND METHODS: Emmel, Itano and osmotic fragility tests were used to test the effect of anthocyanin extracts from Justicia secunda leaves on haemoglobin S solubility and sickle cell membrane stability. RESULTS: Anthocyanins from Justicia secunda were found to possess anti-sickling activity. Treated SS red blood cells recovered a normal, classical biconcave form with a radius of 3.3±0.3 µm, similar to that of normal erythrocytes. The solubility of deoxyhaemoglobin S increased and the osmotic fragility of drepanocytes decreased upon treatment with anthocyanin extracts. CONCLUSION: These findings suggest that anthocyanin extracts play a role in both stabilising the red blood cell membrane and inhibiting polymerisation of haemoglobin S. This provides a possible molecular basis for earlier reports on the anti-sickling properties of anthocyanins from some Congolese plants and their use in the management of sickle cell disease by Congolese traditional healers.