EFFECTS OF THE METHANOL AND AQUEOUS EXTRACTS OF VITEX DONIANA LEAVES ON NA+/K+-ATPASE AND SOME MARKERS OF OXIDATIVE STRESS IN STREPTOZOTOCIN INDUCED DIABETIC ALBINO MALE RATS

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ABSTRACT

Diabetes mellitus is a chronic metabolic disorder which alters several cellular, tissue, organ and system functions, often leading to death. This research, however, was designed to determine the effects of the methanol and aqueous extracts of V. doniana leaves on diabetes mellitus. The antioxidant parameters, membrane stabilisation, Na+/K+-ATPase activity, glycated haemoglobin and electrolytes concentrations were measured using spectrophotometric methods. Other parameters such as the fasting blood glucose concentration, body weights and histopathology of the pancreas were also determined. Thirty-five albino male rats of 4-7 weeks old, weighing 70-140 g were used for this study. The rats were housed in steel cages and acclimatised for one week prior to the experiment. The rats were induced with diabetes using streptozotocin at 65 mg/kg body weight (bwt). The rats were grouped into seven. Group 1 was the normal control, given animal feed and distilled water; group 2, the drug control, received 5 mg/kgbwt of glibenclamide. Group 3 was the negative control, diabetic but not treated. Groups 4 and 5 were given 400 and 800 mg/kgbwt of the aqueous extract respectively whereas groups 6 and 7 received 400 and 800 mg/kgbwt of the methanol extract respectively. The administration lasted for 28 days. Phytochemical analysis of the methanol extract of the leaves indicated the presence of flavonoids, alkaloids, tannins, glycosides, phenols, reducing sugars, steroids, saponins, soluble sugars, terpenoids and hydrogen cyanide. Acute toxicity study showed the relative safety of the extracts at 5000 mg/kgbwt. Generally, there were significant (p<0.05) increases in the fasting blood glucose concentrations of all diabetic rats compared to that of the rats in the normal control. However, prior to sacrifice, all the treated rats showed normal concentrations of fasting blood glucose. There was no significant (p>0.05) difference in body weights of rats across all groups. There was no significant (p>0.05) difference in the glycated haemoglobin concentration of rats across all groups compared to that of the rats in the normal control. Also, there was a significant (p<0.05) increase in the activity of Na+/K+-ATPase of rats in group 6 while rats in  group 3 recorded a significant (p<0.05) low activity. The activities of SOD and CAT showed a significant (p<0.05) increase in rats of all treated groups while there was no significant (p>0.05) difference in GPactivities of rats in all treated groups compared to that of the rats in the normal control. Rats in group 6 showed a significant (p<0.05) reduction in MDA concentration. The methanol extract showed a higher membrane stabilising potential than the drug glibenclamide at 5 mg/kgbwt. Concerning electrolytes, there was generally a significant (p<0.05) reduction of Cl- in rats across all treated groups. A significant (p<0.05) reduction in HCO3- was recorded in group 7. Rats in groups 2 and 7 also showed significant (p<0.05) reductions in Na+ and Ca2+ across all treated groups compared to that of the normal control. Histopathology results revealed considerable regeneration of the pancreatic beta cells of the rats in groups treated with the methanol and aqueous extracts of V. doniana leaves. The results obtained from this research clearly indicate the effectiveness of the methanol and aqueous extracts of V. doniana leaves as antidiabetics.





TABLE OF CONTENTS

Title Page                                                                                                                    i

Declaration                                                                                                                  ii

Certification                                                                                                                iii

Dedication                                                                                                                  iv

Acknowledgements                                                                                                    v

Table of Contents                                                                                                       vi

List of Tables                                                                                                              xi

List of Figures                                                                                                             xii

List of Plates                                                                                                               xiii

Abstract                                                                                                                      xiv

 

 

CHAPTER 1: INTRODUCTION

1.1       Background of the Study                                                                               1

1.2       Statement of the Problem                                                                               3

1.3      Aim of the Study                                                                                             4

1.4      Objectives of the Study                                                                                   4

1.5       Justification of the Study                                                                               5

 

CHAPTER 2: REVIEW OF RELATED LITERATURE

2.1       Diabetes Mellitus                                                                                            7

2.1.1    Epidemiology and pathogenesis of type I diabetes mellitus (IDDM)                        7

2.1.2    Pathophysiology of type I diabetes mellitus                                                   8

2.1.3    Epidemiology and pathogenesis of type II diabetes mellitus                         10

2.1.4    Pathophysiology of type II diabetes mellitus (NIDDM)                                10

2.1.5    Clinical characteristics of patients with type I and II diabetes mellitus         11

2.1.6    Diabetes in pregnancy                                                                                     12

2.1.7    Management of diabetes mellitus                                                                   12

2.1.7.1 Current pharmacological therapies                                                                  13

2.1.7.2 Oral therapies                                                                                                  13

2.1.7.3 Lifestyle modification, literacy and self-management                                   14

2.1.8    Oxidative stress and DNA damage during diabetes mellitus                         15

2.2       Insulin Signalling Pathway                                                                             15

2.2.1    Glucose storage and uptake                                                                            15

2.2.2    Regulati7n of insulin signalling                                                                      17

2.2.3    Relationship between obesity and diabetes                                                    17

2.3       Vitex doniana                                                                                                  18

2.3.1    Scientific classification                                                                                   20

2.3.2    Botanic description                                                                                         20

2.3.3    Biology                                                                                                           20

2.4       Health and Medicinal Benefits of V. doniana                                                            21

2.5       Nutritional Components of V. doniana                                                          21

2.6       Phytochemical Components of V. doniana                                                    22

2.7       Glycated Haemoglobin (HbA1c)                                                                    23

2.7.1    Historical background of glycated haemoglobin                                            23

2.7.2    Non-enzymatic glycation compared with enzymatic deglycation                  24

2.7.3    Clinical use of HbA1c                                                                                    25

2.8       Antioxidant Enzymes                                                                                     26

2.8.1    Properties and biological implications of antioxidant enzymes                      30                               

2.8.1.1 Superoxide dismutase (SOD)                                                                         30

2.8.1.2 Catalase (CAT)                                                                                              32

2.8.1.2.1 Cellular role of catalase                                                                                33

2.8.1.3 Glutathione peroxidase (GPX)                                                                        34

2.9       Malondialdehyde (MDA)                                                                               35

2.10     Na+/K+-ATPase                                                                                               36

2.11     Lethal Dose (LD50)                                                                                         37

2.12     Electrolytes                                                                                                     37

2.12.1  Potassium                                                                                                        38

2.12.2  Sodium                                                                                                            38

2.12.3  Calcium                                                                                                           39

2.12.4  Chloride                                                                                                          40

2.12.5  Bicarbonate                                                                                                     40

2.13     Membrane Stabilisation                                                                                  41

 

CHAPTER 3: MATERIALS AND METHODS

3.1       Equipment                                                                                                       42

3.2       Reagents and Chemicals                                                                                 43

3.3       Collection and Identification of the Plant                                                      43

3.4       Methanol Extraction                                                                                       43

3.5       Aqueous Extraction                                                                                        44

3.6       Animal Experiment                                                                                         44

3.7       Animal Grouping                                                                                            44

3.8       Determination of the Lethal Dose (LD50) of the Extracts                              45

3.9       Induction of Diabetes Mellitus                                                                       45

3.10     Administration of the Extracts                                                                       45

3.11     Determination of the Fasting Blood Glucose Concentration                         46

3.12     Assessment of the Body Weights of the Rats                                                            46

3.13     Collection of Blood                                                                                        46

3.14     Determination of Glycated Haemoglobin                                                      47

3.15     Assay of Na+/K+-ATPase Activities                                                               48

3.16     Estimation of Malondialdehyde (MDA) Concentrations                               49

3.17     Measurement of Catalase (CAT)                                                                    49

3.18     Assay of Superoxide Dismutase (SOD) Activities                                         49

3.19     Assay of Glutathione Peroxidase (GPX) Activities                                        50

3.20     Determination of Membrane Stabilisation                                                      51

3.21     Estimation of Bicarbonate Ions (HCO3-) using Titration Method                  51

3.22     Determination of Sodium Ions (Na+) Concentrations                                                52

3.23     Determination of Potassium ions (K+) Concentrations                                   52

3.24     Determination of Chloride Ions (Cl-) Concentrations                                    53

3.25     Estimation of Calcium Ions (Ca2+) Concentrations                                        54

3.26     Histological Preparations                                                                                54

3.27     Statistical Analyses                                                                                         54

 

CHAPTER 4: RESULTS AND DISCUSSION

4.1       Results                                                                                                            55

4.1.1    Qualitative phytochemical composition of V. doniana leaves                        55

4.1.2    Acute toxicity study                                                                                       56

4.1.3    Effects of the methanol and aqueous extracts of V. doniana leaves on 

fasting blood glucose concentration                                                               57

 

4.1.4    Effects of the methanol and aqueous extracts of V. Doniana leaves on

body weights                                                                                                  59

 

4.1.5    Effects of the methanol and aqueous extracts of V. doniana leaves on

glycated haemoglobin concentrations                                                             61

 

4.1.6    Effects of the methanol and aqueous extracts of V. doniana leaves on

Na+/K+-ATPase activities                                                                               63

 

4.1.7    Effects of the methanol and aqueous extracts on malondialdehyde (MDA)

concentration                                                                                                  65

 

4.1.8    Effects of the methanol and aqueous extracts on antioxidant enzymes

activities                                                                                                          67

 

4.1.9    Effects of the methanol extract on membrane stabilisation                            69

4.1.10  Effects of the methanol and aqueous extracts on electrolytes

concentrations                                                                                                 71

 

4.1.11  Effect of the methanol and aqueous extracts of V. doniana leaves

extract on the histology of the pancreas                                                         75

 

4.2       Discussion                                                                                                       82

 

CHAPTER 5: CONCLUSION AND RECOMMENDATIONS

5.1       Conclusion                                                                                                      89

5.2       Recommendations                                                                                          90

References                                                                                                      91

Appendices                                                                                                    

 

 

 


 

LIST OF TABLES

2.1:      Clinical characteristics of patients with type I and II diabetes mellitus         11

4.1:      Qualitative phytochemical constituents V. doniana leaves                             55

4.2:      LD50 (oral) of the methanol and aqueous extracts of V. doniana leaves       56

 

 

 

 

 

 

 

 

 

 

LIST OF FIGURES

 

2.1:      Insulin signalling pathway                                                                              17

2.2:      V. doniana Leaves                                                                                          19

2.3:      Generation of reactive oxygen species and the defense mechanisms            

against damage by active oxygen                                                                   29                                                                                          

4.1:      Effects of the methanol and aqueous extracts of V. doniana leaves

on fasting blood glucose concentrations                                                         58

 

4.2:      Effects of the methanol and aqueous extracts of V. doniana leaves

on body weights                                                                                             60

 

4.3:      Effects of the methanol and aqueous extracts of V. doniana leaves

on glycated haemoglobin concentrations                                                        62

 

4.4:      Effects of the methanol and aqueous extracts of V. doniana leaves

on Na+/K+ ATPase activities                                                                           64

 

4.5:      Effects of the methanol and aqueous extracts of V. doniana leaves

on MDA concentrations                                                                                 66

 

4.6:      Effects of the methanol and aqueous extracts on antioxidant enzymes

activities                                                                                                          68

 

4.7:      In vitro membrane stabilising effects of the methanol and aqueous

extracts of V. doniana leaves                                                                          70

 

4.8       Effects of the methanol and aqueous extracts of V. doniana leaves

on concentrations of Cl-, K+ and HCO3-                                                                           72

4.9:      Effects of the methanol and aqueous extracts of V. doniana leaves on

Ca2+ and Na+ concentrations                                                                          74

 

 







LIST OF PLATES

 

1:         Photomicrograph showing the pancreas of a normal rat (H and E, X40)        75

2:         Photomicrograph showing the effects of STZ-induced diabetes on the

pancreas of untreated rats (H and E, X40)                                                     76

 

3:         Photomicrograph showing the effects of the drug, glibenclamide

(5 mg/kgbwt) on the Pancreas of Treated Diabetic Rats (H and E, X40)      77

 

4:         Photomicrograph showing the effects of the 400 mg/kgbwt of the

methanol extract on the pancreas of treated diabetic rats (H and E, X40)    78

 

5:         Photomicrograph showing the effects of the 800 mg/kgbwt of the

methanol extract on the pancreas of treated diabetic rats (H and E, X40)    79

 

6:         Photomicrograph showing the effects of the 400 mg/kgbwt of the

aqueous extract on the pancreas of treated diabetic rats (H and E, X40)      80

 

7:         Photomicrograph showing the effect of the 800 mg/kgbwt of the

aqueous extract on the pancreas of treated diabetic rats (H and E, X40)      81

 

 

 


 

CHAPTER 1

INTRODUCTION

 

1.1       BACKGROUND OF THE STUDY

Diabetes mellitus is a chronic metabolic disorder which partially or completely blocks the utilisation of glucose into useful form of energy often resulting in high blood sugar concentrations over a long period of time. It could be a result from the inability of the pancreas to produce enough insulin or the unresponsiveness of the body cells to produced insulin. Diabetes mellitus has been grouped into three main types. Type1 diabetes, also known as Insulin-Dependent Diabetes Mellitus (IDDM) results from the failure of the pancreas to produce enough insulin (WHO, 2013). It is regarded as an autoimmune disorder. Type 2 diabetes mellitus, previously known as non insulin dependent diabetes mellitus (NIDDM) begins with insulin resistance as cells fail to respond properly to the insulin produced. Type 2 diabetes mellitus is commonly caused by excessive body weight and low exercise (WHO, 2013). Gestational diabetes, the third main form, is temporary. It manifests as high blood sugar concentrations in pregnant women without a previous history of diabetes.

Diabtes mellitus is characterised by longterm hyperglycaemia. It is diagnosed when a patient demonstrates one of the following: fasting plasma glucose concentrations ≥ 7.0 mmol/l (126 mg/dl); plasma glucose concentrations  ≥ 11.1 mmol/l (200 mg/dl) two hours after a 75 g oral glucose load as in a glucose tolerance test; symptoms of high blood sugar and casual plasma glucose concentrations  ≥ 11.1 mmol/l (200 mg/dl) and glycated haemoglobin concentrations ≥ 48 mmol/mol (≥ 6.5 % Diabetes Control and Complications Trial) (Diabetes Care, 2010). However, glycated haemoglobin has been used as a better diagnostic tool for determining diabetic condition as well as its accompanying risks of cardiovascular diseases and death (Selvin et al, 2010).

Symptoms of diabetes mellitus include: frequent urination, increased thirst, and increased hunger. If untreated, diabetes can lead to severe complications which may include: diabetic ketoacidosis, hyperosmolar hyperglycemic state, or death (Kitabchi et al, 2009). There may also be serious complications such as cardiovascular diseases, stroke, chronic kidney diseases, foot ulcers and eye damage (WHO, 2013). Diabetes mellitus usually leads to processes that generate reactive oxygen species (ROS). This is usually accompanied with a decrease in both enzymatic and non enzymatic antioxidants, causing oxidative stress (Gumieniczek et al, 2002), compromise of membranes and leakage of important biological molecules from cells.

Type 2 diabetes can be prevented or delayed by maintaining normal weight, engaging in physical activity and eating a healthful diet. Dietary measures to help prevent diabetes mellitus include:  maintaining a diet rich in whole grains and fiber, choosing good fat such as polyunsaturated fats found in nuts, vegetable oils and fish. Also helpful are limiting sugary beverages and eating less red meat. Smoking cessation can also form an important preventive measure (Willi et al., 2007).

Furthermore, diabetes mellitus could be managed with the target of keeping blood sugar concentrations as close to normal, without causing hypoglycaemia. This is usually accomplished with a healthy diet, exercise, weight loss and use of appropriate medications such as metformins and sulfonylurease (Ripsin et al., 2009). In rare cases, a pancreas transplant and weight loss surgeries are often recommended (Picot et al., 2009). Insulin administration has also been useful in managing diabetes especially             type 1.

Recently, biological research has taken a turn into the exploitation of natural substances in plants for an improved management of diabetes, with its accompanying complications. Abdulrahman et al. (2015) demonstrated the antidiabetic effect of Moringa oleifera Lam. seeds in male rats. Salim et al, (2016) showed the hypoglycaemic effect of Vitex simplicifolia leaf extracts on rats. Numerous other plants and plant materials have been shown to exhibit ameliorative effects through different mechanisms that reverse diabetic complications (Zhou et al., 2013).

V. doniana is a perennial shrub highly distributed in high rainfall areas. It is variously called vitex or black plump (English), Dinya (Hausa), Oriri (Yoruba), Ejiji (Kogi) and Ucha okoro (Igbo) (Burkill, 2000). In north central and eastern part of Nigeria, the young leaves of V. doniana are employed as vegetables as well as sauces for meals especially for patients suffering from diabetes. In rural Abia State, for example, the hot aqueous extracts of these leaves have been used by diabetics.

Due to the ethical issues involving human experiments, rat models of the Wistar strain were used for this experiment. Thus, the pathophysiology of diabetes mellitus, as well as the effects of both aqueous and methanol extracts of V. doniana leaves administered to diabetic rats were carefully studied under controlled conditions.


1.2       STATEMENT OF THE PROBLEM

Diabetes is a macro degenerative disease in the world today, affecting over 150 million people and having complications which include: hypertension, atherosclerosis and microcirculatory disorders (Ogbonna et al., 2008).

Globally, the prevalence of diabetes mellitus is on the increase. In African communities, drastic lifestyle changes accompanying urbanisation and westernisation have been a major factor in higher rates (Sobngwi et al, 2010). Also, there has been an identification of genes that raise susceptibility to diabetes in communities of Ghana and Nigeria (Rotimi et al, 2010). Hence, it poses a great burden on health care coupled with difficult economic situations.

The impairment of energy metabolism by diabetes mellitus usually causes numerous complications often resulting in death (Kitabchi et al, 2009). Beta oxidation, an alternative means of generating energy results in overproduction of reactive oxygen species. This further leads to a compromise of natural antioxidants activities and reduced membrane integrity by lipid peroxidation (Rauscher et al, 2001). Other biochemical pathways for glucose metabolism are also affected.


1.3      AIM OF THE STUDY

The aim of the research work was to determine the effects of the methanol and aqueous extracts of V. doniana leaves on Na+/K+-ATPase and some markers of oxidative stress in streptozotocin-induced diabetic albino male rats.


1.4        OBJECTIVES OF THE STUDY

To fully achieve the aim of this research, the following objectives have been set out to form a clean guide:

  1. To determine the phytochemical content of the methanol and aqueous leaf extracts of V. doniana.
  2. To determine the lethal dose of the methanol and aqueous leaf extracts V. doniana.
  3. To determine if the methanol and aqueous leaf extracts of V. doniana could have some positive effects on some biochemical processes that are affected by diabetic conditions such as membrane stability and glucose metabolism.
  4. To investig.ate what happens to the activity of Na+/K+-ATPase under diabetic condition and consequent treatment with oral administration of the methanol and aqueous leaf extracts of V. doniana.
  5. To study the effects that the methanol and aqueous leaf extracts of V. doniana could have on Superoxide Dismutase (SOD), Catalase (CAT), Glutathione Peroxidase (GPX) and Malonyldialdehyde (MDA).
  6. To ascertain the effects of the methanol and aqueous leaf extracts of V. doniana on electrolyte such as sodium, potassium, chloride, calcium and bicarbonates.
  7. To investigate the effects of diabetic condition and treatment with the methanol and aqueous leaf extracts V. doniana on body weights of rats.
  8. To investigate if the methanol and aqueous leaf extracts of V. doniana could have any effects on the histology of the pancreas under diabetic condition.

 

1.5       JUSTIFICATION OF THE STUDY

A recent survey has concluded that 90-95% of all diagnosed cases of diabetes mellitus are of the type 2 (O’Brien, 2011). Type 2 diabetes mellitus is characterised by insulin resistance (Holt, 2010). Biochemical research however, has sought new therapeutic avenues in the treatment of diabetes and all its accompanying disorders. So far a wide array of pharmacological drugs is available for managing diabetes. Some of these drugs even have more life-threatening after effects. Prevalent economic hardship coupled with the high cost of prescription medicine, especially in the developing countries requires the need for natural herbal remedies that are cheaper.

Granted, V. doniana leaves as well as other parts of the plant have been used successfully in managing other health risks. However, little is known on the effects of V. doniana leaves in the management of disorders associated with diabetes mellitus, especially bordering on the activity of Na+/K+-ATPase and antioxidant enzymes.

The study will further underscore the application of V. doniana leaves extracts in particular, and plant extracts as a whole, in managing or even treating diabetic complications.

 


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