PHYTOCHEMICAL COMPOSITION, ANALGESIC, ANTIINFLAMMATORY AND TONIC PROPERTIES OF VISCUM ALBUM (MISTLETOE)

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Abstract

Viscum album (Mistletoe) is a semi-parasitic plant which grows on the stems of other tree species. This present study was carried out to investigate the phytochemical composition, acute toxicity, analgesic, antiinflammatory and tonic properties of Viscum album, which was soxhlet-extracted using ethanol as solvent.Qualitative phytochemical analysis of ethanol extract of Viscum album showed the presence of saponins, alkaloids, flavonoids, phenolics, tannins, terpenes, glycosides and steroids. Quantitative screening yielded high result for flavonoids (6.93mg/100g), followed by alkaloids, saponins, tannins, steroids phenols, terpenes and glycosides yielding (6.39, 5.81, 4.38, 3.12, 2.76, 1.95 and 0.94)mg/100g respectively. Acetic acid-induced writhing model was employed for analgesic activity assay and aspirin was used as standard control. Oral administration of (400 and 800mg/kg b.w) significantly reduced the nociceptive responses induced by acetic acid by (80.34±0.67 and 58.95±2.25) % respectively. The antiinflammatory activity was screened using a phlogistic agent, egg albumin-induced rat paw edema, using aspirin (100mg/kg) as reference control. It was observed that administration of (200 and 400mg/kg) of extract significantly inhibited inflammatory response by (58.22±8.24 and 58.73±4.40) % respectively at the end of 120min of the assay. The tonic profile of the extract was screened on laboratory water bath, using an isolated rabbit jejunum. First, the effects of different concentrations of ethanol extract of Viscum album(300, 600 and 1200) µg/ml were assayed and it was found to reduce the basal contractions (15.00±0.41, 14.00±0.41 and 16.00±0.58)mm to (2.75±0.48, 2.00±0.41 and 1.75±0.25)mm respectively, which represent (81.74, 85.68 and 88.93)% respectively. Then the effects of same concentration of extract 300µg/ml was examined on different concentrations of acetylcholine (3.33, 6.66 and 13.32)µg/ml and was shown to inhibit the excitatory activity of acetylcholine from (17.00±0.41, 21.75±0.48 and 21.75±0.48)mm to (2.25±0.25, 6.50±0.29 and 6.50±0.29)mm, which represent (86.75, 79.29 and 70.05)% respectively. Furthermore, results of the effects of same concentration of atropine on acetylcholine induced contraction had no significant effect, but began inhibiting acetylcholine activity upon increased concentrations of atropine. The reduction in the contractile response to acetylcholine, following supposed blockade of cholinergic receptors by plant extract was far more considerable than atropine in rabbit jejunum. These results indicate that the ethanol extract of Viscum album is a potent analgesic, antiinflammatory and tonic compound. These findings further suggest that the analgesic, antiinflammatoryeffects and the relaxing effects of theethanol extract of Viscum album on jejunal contractions may in fact be due to the presence of the phytoconstituents present. However, further research on the isolation and characterization of the responsible phytochemicals is pertinent.






TAB LE OF CONTENTS

Title Page                                                                                                                                i

Declaration                                                                                                                              ii

Certification                                                                                                                            iii

Dedication                                                                                                                              iv

Acknowledgements                                                                                                                v

Table of Contents                                                                                                                   vi

List of Tables                                                                                                                          xi

Abstract                                                                                                                                  xii

CHAPTER 1: INTRODUCTION

1.1       Background of the Study                                                                                           1

1.2       Aim of the Study                                                                                                        3

1.3       Objectives of the Study                                                                                              3

1.4       Statement of the Problem                                                                                           4

1.5       Justification                                                                                                                 5

CHAPTER 2:            LITERATURE REVIEW

2.1       Pain                                                                                                                             6

2.1.1    Acute pain                                                                                                                   7

2.1.2    Chronic Pain                                                                                                               8

2.1.3    Special Types Of pain                                                                                                 10

2.1.3.1 Neuropathic pain                                                                                                         10

2.1.3.2 Phantom pain                                                                                                              11

2.1.3.3 Central pain                                                                                                                 12

2.1.3.4 Allodynia                                                                                                                    13

2.1.3.5 Nociceptive pain                                                                                                         13

2.1.3.6 Breakthrough pain                                                                                                      14

2.1.3.7 Psychogenic pain                                                                                                        14

2.1.4    Pathways of pain                                                                                                        15

2.1.5    Regulators of pain                                                                                                       16

2.1.6    Pain management and treatment                                                                                 17

2.1.6.1 Assessment of pain                                                                                                     18

2.1.6.11 Physiological assessment                                                                                          18

2.1.6.12 Pain scales                                                                                                                 18

2.1.7    Treatment of pain                                                                                                        19

2.1.7.1 Non-pharmacological approach                                                                                  20

2.1.7.11Acupuncture:                                                                                                             20

2.1.7.12Heat and cold                                                                                                            20

2.1.7.12.1    Transcutaneous electrical nerves stimulation (TENS)                                           20

2.1.7.2 Pharmacological approach                                                                                          21

2.1.7.21 Analgesics and anesthesia                                                                                         21

2.1.7.211 Paracetamol (acetaminophen)                                                                                 21

2.1.7.212 NSAIDs                                                                                                                  22

2.1.7.213 Opioids                                                                                                                   23

2.1.7.214Gabanoids, gabapentin, and gregabalin                                                                   24

2.2                Overview of inflammation                                                                                         25

2.2.1    Types of inflammation                                                                                                27

2.2.1.1 Acute inflammation                                                                                                    27

2.2.1.2 Chronic inflammation                                                                                                 28

2.2.2    Etiology of inflammation                                                                                            29

2.2.3    Pathophysiology                                                                                                         30

2.2.4    Inflammatory mediators                                                                                             30

2.2.5    Treatment of inflammation                                                                                         32

2.2.6        Inflammatory diseases                                                                                                34

2.3       Smooth Muscles: introduction                                                                                    35

2.3.1    Core function of smooth muscles                                                                               36

2.3.2    Organs involved in smooth muscles functionality                                                      36

2.3.3    Smooth muscle                                                                                                            37

2.3.4    Mechanism of smooth muscle functionality                                                               38

2.3.5    Pathophysiology of smooth muscle                                                                            39

2.3.6    Important modulators of smooth muscle tone                                                            41

2.3.6.1 Structural modulators                                                                                                 41

2.3.6.2 Organic chemical modulators                                                                                     41

2.3.6.21 Neurotransmitters as organic modulators                                                                 42

2.3.6.211 Acetylcholine                                                                                                                      43

2.3.6.22Classification of neurotransmitters                                                                            44

2.3.6.23 Drugs that influence neurotransmitters                                                                     45

CHAPTER 3:  MATERIALS AND METHODS

3.1       Materials                                                                                                                    47

3.1.1    Plant material                                                                                      47

3.1.2    Animals                                                                                                                       47

3.1.3    List of instruments/equipment                                                                                    47

3.1.4    Preparation of reagents for phytochemical assay                                                        49

3.2       Methods                                                                                                                      51

3.2.1    Extractionof plant material                                                                                         51

3.2.2    Qualitative phytochemical analysis of ethanol extract of Viscum album                   51

3.2.2.1 Test for saponins                                                                                                         52

3.2.2.2 Test for flavonoids                                                                                                      52

3.2.2.3 Test for alkaloids                                                                                                        53

3.2.2.4 Test for terpenes                                                                                                         53

3.2.2.5 Test for tannins           `                                                                                               53

3.2.2.6 Test for phenols                                                                                                          54

3.2.2.7 Test for steroids                                                                                                          54

3.2.2.8 Test for glycosides                                                                                                      54

3.2.3    Quantitative phytochemical analysis of ethanol extract of Viscum album                 54

3.2.3.1 Determination of saponins                                                                                          54

3.2.3.2 Determination of alkaloids                                                                                         55

3.2.3.3 Determination of tannins                                                                                            56

3.2.3.4 Determination of flavonoids                                                                                       56

3.2.3.5 Determination of phenolic content                                                                             57

3.2.3.6 Determination of cardiac glycosides                                                                                    57

3.2.3.7 Determination of steroids                                                                                           58

3.2.3.8 Determination of terpenes                                                                                          58

3.2.4    Acute toxicity and lethal dose test (LD50)                                                                  59

3.2.5    Evaluation of analgesic activity                                                                                  59

3.2.5.1 Experimental animals                                                                                                  60

3.2.5.2 Experimental procedure                                                                                              60

3.2.6    Evaluation of antiinflammatory activity                                                                     61

3.2.6.1 Induction of a hind paw edema                                                                                  61

3.2.6.2 Experimental animals                                                                                                  61

3.2.6.3 Procedure                                                                                                                    62

3.2.7    Evaluation of tonic effect                                                                                           62

3.2.7.1 Reagents for tyrode solution                                                                                      63

3.2.7.2 Calculation of drug volumes and concentrations for tonic activity                            63

3.2.7.3 Experimental protocol                                                                                                 64

3.2.8    Statistical analysis                                                                                                       65

CHAPTER 4 :           RESULTS AND DISCUSSION

4.1       Results                                                                                                                        66

4.1.1    Phytochemical assay                                                                                                   66

4.1.1.1 Qualitative phytochemical report                                                                               66

4.1.1.2 Quantitative phytochemical Report                                                                           67

4.1.2    Acute toxicity profile                                                                                                  69

4.1.3    Analgesic effect                                                                                                          70

4.1.4    Antiinflammatory effect                                                                                             71

4.1.5    Tonic effect                                                                                                                 73

4.2       Discussion                                                                                                                   76

CHAPTER 5:  CONCLUSION AND RECOMMENDATION

References                                                                                                                              84

Appendix                                                                                                                                92

 

 

 

 

 

 

 

LIST OF TABLES

4.1:      Phytochemical components of ethanol extract of Viscum album (Mistletoe)            65

4.2:      Quantitative phytochemicals content of extract of Viscum album (Mistletoe)          66

4.3:      Acute toxicity results of ethanol extract of Viscum album                                        68

4.4:      Analgesic effect of Viscum album on acetic acid induced writhing  in        experimental albino rats.                                                                                                69

4.5:      Results for antiinflammation                                                                                      70

4.6:      Change in paw diameter and % change in paw diameter of antiinflammation          70

4.7a:    Effect of the extract Viscum album on isolated rabbit jejunum                                 72

4.7b:    Effects of Ach (Acetylcholine) on isolated rabbit jejunum                                        72

4.7c:    Effects of atropine on acetylcholine induced contraction                                          73

4.7d:    Effects of extract on acetylcholine administration on isolated rabbit jejunum          74

 


 


CHAPTER 1

INTRODUCTION


            1.1              BACKGROUND OF THE STUDY

The benefits of medicinal plants cannot be overemphasized. A plethora of health challenges have been remedied by recent advancements in their research and applications. Plant derived substances have constantly remained significant in drug development, especially in the discovery of novel analgesic and antiinflammatory drugs. They not only help as aforementioned, but also greatly contribute to understanding the complex pathway of pain transmission, receptor types and endogenous ligands which play critical role in its transmission. The search for new naturally occurring analgesic, antiinflammatory and compounds is taking aggressive dimensions due to their efficacy, reduced contraindications, creating significant leads in the development of highly efficacious synthetic molecules (Qurqn, 2009).

Viscum album belongs to the family Loranthaceae. It is a small greenish plant, known as mistletoe in English. Mistletoe (Viscum album) is a semi-parasitic plant which thrives on varieties of host trees which includes pine, oak, birch and apple. The plant is preponderantly found in Northern areas of Pakistan on the hills in Chitral and Dir Upper. The plant has a record length growth of up to 100 cm with leathery leaves alternate on the stems. Fruit of Viscum album is a waxy white gelatinous berry. The term semi-parasitic implies that the mistletoe plant undergoes photosynthetic process independently, while feeding off the host’s water and minerals endowment. There are several varieties of mistletoe, which are defined by the host that they parasitize. European mistletoe is dioecious, that is each plant is unique with either male or female flowers. They are pollinated by insects and bear small white berries on evergreen foliage, other varieties bear red berries. Alkaloids, glycosides, phenylpropanoids, tannins, lignins sugars and viscotoxinsare some of the several chemical components found in Viscum album. Several subcomponents of flavonoids like quercetin, kaempferol and rarely naringenin have also been found to be present. Methyl derivatives of quercetin and kaempferol have also been reported from this plant (Ame et al., 2010)

MISTLETOE preparations have been widely used in Europe and other parts of the world including Africa for centuries to treat epilepsy, infertility, hypertension, cardiovascular disorders and arthritis. Medicinal use of Viscum albumh as also been recorded in ancient Greek practice. The treatment of diseases associated with spleen disorders and menstruation using preparations of Viscum album have been documented by Hippocrates (460–377 BC). In folklore medicine, mistletoe has been used as a panacea for a wide range of diseases such as sciatica, neuralgia, rheumatic deafness and asthma, diabetes mellitus, chronic cramps, stroke, epilepsy, stomach upsets, as antihypertensive and discomforts associated with menopause. Medicinally, Viscum album is recorded to be highly useful in diuretics, as antispasmodic and relieving cardiac problems (Ohiri et al., 2003)

Chemical constituents isolated from Viscum album (mistletoe) have been tentatively recorded to possess the potential for the treatment of several cancer types, including bladder, breast, pancreas and many more, based on the observation that the plant, like cancer, is parasitic and lethal to its host. Albeit, there is lack of quality clinical trials and no significant evidence of an effect (Ernst, 2006; Hong et al., 2014; Von Schoen-Angerer et al., 2015).

However, not so much findings are there to show that extract and compounds isolated from Viscum album reduce the activity of smooth muscle. Further studies however are needed. In folk medicine, it has been utilized for its cardiovascular properties; clinical efficacy has not been established. Injectable mistletoe extract is widely used in Europe but have not yet been ratified for use in the United States. Several experimental studies have shown to imply that administration of extracts from mistletoe could prove beneficial in alleviating critical medical conditions or cases of degenerative joint diseases/osteoarthritis, diarrhea, arteriosclerosis, epilepsy, gastrointestinal disorders, heart conditions, high blood pressure, infertility, indigestion, tachycardia and bachycardia.


1.2       AIM OF THE STUDY

The aim of this study was to assay the phytochemical composition, analgesic, antiinflammatory and tonic properties of extract of Viscum album (Mistletoe).


1.3       OBJECTIVES OF THE STUDY

a)      To evaluate the qualitative and quantitative phytochemical compositions such as tannins, flavonoids, saponins, phenolic compounds, alkaloids and terpenes of the extract of Viscum album.

b)      To determine the acute toxicity (LD50) of the extract of Viscum album in experimental Wistar rats.

c)      To evaluate the analgesic effect of the extract of Viscum album on experimental albino rats.

d)     To evaluate the anti-inflammatory effect of the extract of Viscum album on selected experimental wistar rats.

e)      To determine in vivo, the tonic potential of the extract of Viscum album on isolated rabbit jejunum.

f)       To determine the mechanism of the tonicity potential of the extract of Viscum album on isolated rabbit jejunum.


1.4       STATEMENT OF THE PROBLEM

Mistletoe (Viscum album) is widely utilized in traditional practice for remedy in cases of infertility, hypertension, and arthritis, mostly in the southern part of Nigeria. The plant grows in diverse parts of the African rainforests and has long been employed in villages and urban metropolis, to alleviate certain physiological diseases and dysfunction. Though numerous therapies for pain, inflammatory and tonic disorders.

The World Health Organization (WHO) also encourages research studies pertaining to the treatment and/or prevention of the above mentioned maladies using traditional medical practices as there is the worldwide belief, that herbal remedies are safer and less harmful to the human and animal systems, than the widely used synthetic drugs (Meite et al., 2009)

 A tenable solution is to find and develop new traditional remedies for the cure, treatment and possible prevention of the maladies both in children and in adults.


1.5       JUSTIFICATION FOR THE STUDY

The use of herbal remedies, according to WHO, to treat diseases and disorders would provide best sources from which new varieties of medications could be developed (Akuodor et al., 2011). The traditional application of this specific plant for the cure of a plethora of pain, inflammatory and tonicity-related dysfunctions and maladies underpins this research study, designed to assay the composition, analgesic, anti-inflammatory and tonic tendencies of the ethanol extract of the leaves of Viscum album (mistletoe) on selected experimental albino rats.


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