scholarly journals Anti-diabetic activity of Clerodendrum paniculatum leaves by In-vitro, In-vivo and Ex-vivo methods

2021 ◽  
Vol 16 (1) ◽  
pp. 211-118
Author(s):  
Venkatesh S ◽  
Aswani K ◽  
Asheena Asharaf V V ◽  
Anjitha P ◽  
Suresh A ◽  
...  

The present study has been undertaken to evaluate the in-vitro, in-vivo and ex-vivo anti-diabetic activity of leaves of chloroform extract Clerodendrum paniculatum (CECP). The extract was prepared by soxhlet extraction. Phytochemical screening indicates the presence of flavonoids, phenols, carbohydrates etc. The anti-diabetic activity of extract was studied by in-vitro (alpha amylase inhibition and alpha glucosidase inhibition assay), in-vivo (streptozotocin induced diabetes) and ex-vivo (glucose uptake by rat hemi - diaphragm method). For in-vitro studies, the inhibitory action of CECP was compared with standard drug Acarbose. The IC50 values of CECP for alpha amylase and alpha glucosidase was found to be 158.396 µg/ml and 113.122 µg/ml respectively and the extract shows significant anti-diabetic activity. For in-vivo and ex-vivo studies Glibenclamide was used as a standard drug to compare the blood glucose level and uptake of glucose was calculated. The results obtained from the study indicate that both 200 mg/kg and 400 mg/kg of CECP showed significant anti-diabetic activity. The 400 mg/kg of CECP showed better activity when compared to 200 mg/kg of the extract. The glucose uptake study was performed by isolated rat hemidiaphragm method. The hemi diaphragm obtained from the rats treated with both the doses of CECP showed significant glucose uptake.

Author(s):  
Jirawat Riyaphan ◽  
Chien-Hung Jhong ◽  
May-Jwan Tsai ◽  
Der-Nan Lee ◽  
Max K. Leong ◽  
...  

The inhibition of alpha-glucosidase and alpha-amylase is one of clinic strategies for remedy the type II diabetes. Herbal medicines are reported to alleviate hyperglycemia. However, the constituents from those sources whether are targeted to the alpha-glucosidase and alpha-amylase still unexplored. This study attempted to select the compounds for efficacy of hypoglycemia via cellular and mouse levels. The results illustrated that the cytotoxicity in all tested compounds at various concentrations except the concentration of 16-hydroxy-cleroda-3,13-dine-16,15-olide (HCD) at 30 µM were not significant difference (p > 0.05) when compared with the untreated control. Acarbose (reference drug), Antroquinonol, Catechin, Quercetin, Actinodaphnine, Curcumin, HCD, Docosanol, Tetracosanol, Berberine, and Rutin could effectively inhibit the alpha-glucosidase activity of Caco-2 cells when compared with the control (maltose). The compounds (Curcumin, HCD, Tetracosanol, Antroquinonol, Berberine, Catechin, Actinodaphnine, and Rutin) could reduce blood sugar level at 30 min in tested mice. The effects of tested compounds on area under curve (AUC) were significant (p < 0.05) among Acarbose, Tetracosanol, Antroquinonol, Catechin, Actinodaphnine, and Rutin along with Berberine and Quercetin. In in vitro (alpha-glucosidase) with in vivo (alpha-amylase) experiments suggest that bioactive compounds can be a potential inhibitor candidate of alpha-glucosidase and alpha-amylase for the alleviation of type II diabetes.


Molecules ◽  
2019 ◽  
Vol 24 (11) ◽  
pp. 2072 ◽  
Author(s):  
Mohammad Reza Youssefi ◽  
Elham Moghaddas ◽  
Mohaddeseh Abouhosseini Tabari ◽  
Ali Akbar Moghadamnia ◽  
Seyed Mohammad Hosseini ◽  
...  

Background: One of the most important causative agents of visceral leishmaniasis (VL) is Leishmania infantum, which is mainly spread by Phlebotomus and Lutzomyia sandflies in the Old and New World, respectively. Novel and effective drugs to manage this neglected vector-borne disease are urgently required. In this study, we evaluated the toxicity of carvacrol, thymol and linalool, three common essential oil constituents, on amastigotes and promastigotes of L. infantum. Methods: in vitro experiments were performed by 24 h MTT assay. Carvacrol, thymol and linalool at concentrations ranging from 1.3 to 10 μg/mL were tested on promastigotes of L. infantum. For in vivo test, two groups of hamsters (Mesocricetus auratus) received 100 mg/kg of body weight/day of carvacrol and thymol as intraperitoneal injection on day 7 post-infection, followed by a 48 h later injection. The third group was treated with the glucantime as standard drug (500 mg/kg) and the last group (control) just received normal saline. On the 16th day, the number of parasites and histopathological changes in liver and spleen were investigated. Results: 24 h MTT assay showed promising antileishmanial activity of thymol and carvacrol, with IC50 values of 7.2 (48 μM) and 9.8 μg/mL (65 μM), respectively. Linalool at all concentrations did not affect L. infantum promastigote viability. In vivo toxicity data of carvacrol and thymol showed that the former at 100 mg/kg was the safest and most effective treatment with little side effects on the liver. Conclusions: Overall, thymol and carvacrol are highly promising candidates for the development of effective and safe drugs in the fight against VL.


2020 ◽  
Vol 10 (3) ◽  
pp. 31-35
Author(s):  
R ARATHY ◽  
K MURUGAN ◽  
KV DINESH BABU ◽  
GS MANOJ

Diabetes is a notorious and growing clinical and public health issue. The International Diabetes Federation assumes that 592 million had diabetes by 2035 and that by 2040 the number will increase to 642 million. Cardiovascular corollary accounts for four million deaths annually attributable to diabetes. Evidence reveals that certain glucose-lowering phytochemicals can improve vascular outcomes with type 2 diabetes, which, together with better understanding of using multiple therapies concurrently, offers opportunities for beneficial personalization of medication regimens. Anthocyanins are coloured pigments and are natural antioxidants. Keeping this in focus, this study was undertaken to evaluate the in vitro antidiabetic activity in the petals of wild Impatiens balsamina L. The anthocyanin was extracted from floral petals of wild balsam species and purified to homogeneity using chromatographic techniques. Evaluation of in vitro antidiabetic properties of anthocyanin extract revealed a dose-dependent increase in the inhibitory effect on the alpha-glucosidase (200 μg/ml) and alpha-amylase enzymes (500 μg/ml) and was comparable with the standard acarbose drug (189 μg/ml and 50 μg/ml). These results indicated that anthocyanin could be used as a source of functional food and nutraceuticals. This information from wild species will be useful in finding more potent antidiabetic principle from the natural resources for the clinical development of antidiabetic therapeutics. Future studies are planned to substantiate the antidiabetic power of anthocyanin using in vivo animal models. Keywords: Alpha amylase, alpha glucosidase, diabetes, herbal remedies, Impatiens balsamina L.


Author(s):  
Jose Deepa ◽  
N. A. Aleykutty ◽  
Harindran Jyoti

Objective: To investigate the anti-diabetic activity of combined ethanolic extracts (1:1mixture) of dry leaves of Syzygium cumini and Psidium guajava belonging to the family Myrtaceae as well as to compare the anti-diabetic activity of these plants by in vitro methods.Methods: In vitro glucose uptake assay was performed on cultured L6 cell lines (rat myoblast cell line) and estimated the glucose uptake using high sensitivity glucose oxidase kit. In vitro alpha amylase inhibitory assay was performed on porcine alpha amylase and the absorbance was measured at 540 nm using a microplate reader. Acarbose was used as the standard in both the methods.Results: At a concentration of 100µg/ml the percentage glucose uptake by the combined ethanolic extract (1:1 mixture) of Syzygium cumini and Psidium guajava leaves was 43.95 while for acarbose the corresponding value was 51.71. At 100 μg/ml the percentage of glucose uptake by Syzygium cumini and Psidium guajava was 27.62 and 22.17 respectively. The percentage inhibition of alpha amylase by the combined ethanolic extract (1:1 mixture) of Syzygium cumini and Psidium guajava leaves at a concentration of 1000 µg/ml was 36.51 and it was 29.26 for Syzygium cumini and 23.43 for Psidium guajava. For acarbose the percentage inhibition of alpha amylase was 73.82 at the concentration of 1000 µg/ml.Conclusion: The combined extract of the leaves of the plants selected was found to be more effective than individual plant extracts against diabetes. The percentage glucose uptake of the combined extract was found to be closer to that of the standard drug acarbose. On comparison of two plants Syzygium cumini was found to be more active against diabetes than Psidium guajava. As the 1:1 mixture of the ethanolic extract is found to be more active, the combination of the two plants can be used to formulate drugs for treating diabetes.


2002 ◽  
Vol 30 (6) ◽  
pp. 581-595 ◽  
Author(s):  
Ingrid Langezaal ◽  
Sebastian Hoffmann ◽  
Thomas Hartung ◽  
Sandra Coecke

Immunotoxicology is a relatively new field in toxicology, and is one of emerging importance, because immunotoxicity appears to contribute to the development of cancer, autoimmune disorders, allergies and other diseases. At present, there is a lack of human cell-based immunotoxicity assays for predicting the toxicity of xenobiotics toward the immune system in a simple, fast, economical and reliable way. Existing immunotoxicity tests are mainly performed in animals, although species differences favour human-based testing. Whole-blood cytokine release models have attracted increasing interest, and are broadly used for pharmacological in vitro and ex vivo studies, as well as for pyrogenicity testing. We have adapted those methods for immunotoxicity testing, to permit the potency testing of immunostimulants and immunosuppressants. Following stimulation with a lipopolysaccharide or staphylococcal enterotoxin B, monocytes and lymphocytes release interleukin-1β and interleukin-4, respectively. Thirty-one pharmaceutical compounds, with known effects on the immune system, were used to optimise and standardise the method, by analysing their effects on cytokine release. The in vitro results were expressed as IC50 values for immunosuppression, and SC4 (fourfold increase) values for immunostimulation, and compared with therapeutic serum concentrations of the compounds in patients, and in vivo LD50 values from animal studies. The in vitro results correlated well with the in vivo data, so the test appears to reflect immunomodulation. Results were reproducible (CV = 20 ± 5%), and the method could be transferred to another laboratory (r2 = 0.99). We therefore propose this method for further validation and for use in immunotoxicity testing strategies.


Author(s):  
Folorunsho A. Ajayi ◽  
Olubukola. S. Olorunnisola ◽  
Adewale. Adetutu ◽  
Folashade G. Olorunfemi ◽  
Abiodun O. Owoade ◽  
...  

Thaumatococcus danielli (Benn.) Benth, a member of the Maranthaceae family has continued to be of immense benefit to the people in the tropics especially in Nigeria. The leaf is widely used among the “Yoruba’s” as a wrapping leaf and for the management of diabetes mellitus. Aim: This study, evaluated the anti-diabetic and possible mode of action(s) of ethanol leaves extract of Thaumatococcus danielli using in vivo and in vitro approach. Methods: Diabetes was induced in Albino rats by administration of Streptozotocin (65 mg/kg/b.wt, i.p). The ethanol leave extract of Thaumatococcus danielli (at a dose of 250 mg/kg and 500 mg/kg body weight was administered at single dose per day to diabetes induced rats for a period of 14 days. The possible mode of action of extract was assessed through in vitro inhibitory effect on alpha amylase, non-enzymatic glycosylation of haemoglobin and glucose uptake in yeast cell. Results: The results showed that the plant extracts demonstrated dose and time dependent reduction in blood glucose. The extract at 250 mg/kg /b.wt and 500 mg/kg/b.wt caused a significant percentage reduction (35.00%/42.04% and 42.16%/60.43%) in blood glucose when compared with the group treated with (25 mg/kg/b.wt) of the standard drug (30.51/40.88%) and the diabetic control (10.46%/-13.67%) on day 7 and day 14 respectively. Although, the extract demonstrated significant (p<0.05) dose dependent inhibitory effect on alpha amylase with an IC50 of 837.97 µg/ml, its activity was significantly (P<0.05) lower than the standard Acarbose. Conversely, the extract showed stronger inhibition of non-enzymatic glycosylation of haemoglobin (87.51%) and enhance glucose uptake in yeast cells by 85.56% when compared with the standard drug Trolax and Metronidazole respectively. Conclusion: The results of this study revealed that Thaumatococcus danielli (Benth) leaves contain anti-hyperglycaemic agent (s) and its possible mode of action is by promoting glucose uptake, inhibition of non-enzymatic glycosylation of haemoglobin and alpha amylase activity.


Peptides ◽  
2012 ◽  
Vol 37 (2) ◽  
pp. 320-326 ◽  
Author(s):  
Shiming Xu ◽  
Pei Han ◽  
Mei Huang ◽  
Joseph C. Wu ◽  
Chingpin Chang ◽  
...  

2019 ◽  
Vol 17 ◽  
pp. 205873921985742
Author(s):  
Jawad Zaheer ◽  
Qazi Najam-Us-Saqib ◽  
Misba Qamar ◽  
Muhammad Akram

Androsace foliosa syn. Androsace sarmentosa (botanical name of common rock jasmine) ( Primulaceae) is used in the treatment various disorders. The aim of this study is to evaluate in vitro anti-diabetic activity of crude methanolic extract of leaves and roots of A. foliosa by anti -alpha-glucosidase (α-Glc) and in vivo anti-diabetic activity of n-hexane fraction on alloxan-induced diabetic mice. Results of in vitro anti-diabetic (α-Glc) activity showed that n-hexane leaves fraction was most potent among all the fractions and showed IC50 (half maximal inhibitory concentration) value of 64.91 ± 0.16 µg and % inhibition of 89.35 ± 0.45, comparable to that of standard acarbose. In vivo n-hexane leaves fraction decreases blood glucose level and reduces body weight similar to that of standard drug glibenclamide. Based on the conclusion of both in vitro and in vivo activities, it can be accomplished that the plant A. foliosa acquires noteworthy anti-diabetic action and can be used to treat diabetes mellitus type II and to reduce body weight.


Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 293
Author(s):  
Hamza Mechchate ◽  
Imane Es-safi ◽  
Abdelhadi Louba ◽  
Ali S. Alqahtani ◽  
Fahd A. Nasr ◽  
...  

Withania frutescens L. is a wild perennial woody plant used by the local population for diverse therapeutic purposes. This work aims to study for the first time the potential inhibitory effect of this plant hydroethanolic extract on α-amylase and α-glucosidase activities using in vitro methods and its antidiabetic and antihyperglycemic activities using alloxan-induced diabetic mice as a model for experimental diabetes. Two doses were selected for the in vivo study (200 and 400 mg/kg) and glibenclamide, a well-known antidiabetic drug (positive control) in a subacute study (28 days) where the antihyperglycemic activity was also assessed over a period of 12 h on diabetic mice. The continuous treatment of diabetic mice with the extract of Withania frutescens for 4 weeks succeeded to slowly manage their high fasting blood glucose levels (after two weeks), while the antihyperglycemic test result revealed that the extract of this plant did not control hyperglycemia in the short term. No toxicity signs or death were noted for the groups treated with the plant extract, and it shows a protective effect on the liver and kidney. The in vitro assays demonstrated that the inhibition of alpha-amylase and alpha-glucosidase might be one of the mechanisms of action exhibited by the extract of this plant to control and prevent postprandial hyperglycemia. This work indicates that W. frutescens have an important long term antidiabetic effect that can be well established to treat diabetes.


2019 ◽  
Vol 9 (4) ◽  
pp. 289-294
Author(s):  
Babita Aggarwal ◽  
Pankaj Sharma ◽  
Hardarshan Singh Lamba

Background: Plants are rich and cheap source of active phytoconstituents. Present study was performed in order to authenticate the traditional use of Cocos nucifera in malaria treatment as well as to search an alternative for drug resistant parasites. Objective: In the present investigation, ethanolic (ACN) and hydroalcoholic (HACN) extracts of Cocos nucifera endocarp were evaluated for antimalarial potential as well as subjected to GC-MS analysis to characterize the bioactive components. Methods: In vitro antiplasmodial activity of ACN and HACN was assessed against P. falciparum strains MRC-02 (CQ sensitive) and RKL-09 (CQ resistant) and percentage schizont maturation inhibition was determined. To confirm the antimalarial potential, in vivo Peter’s 4-Day suppressive test using P. berghei strain was performed at a dose of 25 and 50 mg/kg/day for 4 consecutive days. Bioactive components were characterized by the application of Gas chromatography and Mass spectrometric technique to the extracts. Results: Promising in vitro antiplasmodial activity was exhibited by both alcoholic (ACN) and hydroalcoholic (HACN) extracts against P. falciparum strains MRC-02 (CQ sensitive) with IC50 values < 5 µg/mL. HACN (% Suppression = 75.43 ± 0.18; MST=19.21 days) and ACN (% Suppression = 34.65 ± 0.11; MST=10.11 days) showed moderate in vivo antimalarial activity (p < 0.05) at dose 50 mg/Kg while standard drug chloroquine (8mg/kg) suppressed 100% parasitaemia. Twenty compounds have been identified and characterized by GC-MS studies.


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