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Analgesic properties of aqueous bark extract of Adansonia digitata in Wistar rats
Abstract
The study investigated the analgesic effect of the aqueous extract of the bark of Adansonia digitata using Wistar rats. Thirty Wistar rats weighing between 150 and 170g of either sex were used for the study. Animal were picked randomly and grouped into six with each group made up of five animals (3 females and 2 males). Oral administration of 10ml/kg of normal saline were given to control group; 5mg/kg of indomethacin to reference group; and 25mg/kg, 50mg/kg, 100mg/kg or 200mg/kg of aqueous extracts of Adansonia digitata to each of the test groups respectively.Hotplate and formalin paw-licking tests were used for nociceptive assessment. Animals treated with aqueous bark extract of Adansonia digitata showed significantly (p<0.05) prolonged response time to thermal stimuli (4.42±0.11s) compared with control group (3.29±0.29s) in a dose dependent manner. Results formalin paw-licking test showed that at early phase, animals administered with aqueous bark extract of Adansonia digitata significantly (p<0.05) have reduced paw-licking time (47.88±3.48-40.80±3.85s) compared with the control group (91.51±7.32s). In the late phase, aqueous bark extract of Adansoni adigitata significantly (p<0.05) reduced the paw-licking time (43.57±2.6-25.49±3.46s) compared with the control group (66.31±5.04s). It is hereby concluded that aqueous bark extract of A. digitata possesses a strong analgesic effect.
... Because of their antioxidant properties, bioactive compounds change and reduce the risk of chronic pathologies associated with oxidative stress. These compounds are associated with some of the reported biological activities, such as anti-hyperglycemic [15,17,18], analgesic and antipyretic [15,19], antibacterial, antiviral [15,20], antioxidant [18], and antiinflammatory [4,10] properties. Moreover, polyphenols are well-known for reducing the worsening and/or development of oxidative stress. ...
... Therefore, this experimental work meant to analyze and report the proximate composition of baobab fruit pulp, as collected in several municipalities in the province of Luanda, Angola. Much of the recent research on baobab fruit has concentrated on regions in southern and eastern Africa, including Kenya and Sudan [8,19,[22][23][24], South Africa [25], Mali [18], and Nigeria [8,17]. Although the economic interest in baobab fruit continues to increase, there is still a lack of knowledge on Angolan fruits. ...
... Additionally, this research aims to assess the antioxidant activity in various baobab pulp extracts based on green solvents, and characterized by low toxicity, convenient accessibility, and great efficiency. Although prior research has been conducted on the antioxidant capacity of this fruit [5,9,15,17,19,22], we believe that this is a pioneering study on the evaluation of the in vitro scavenging effect of baobab extracts against physiologically important ROS and RNS. Furthermore, this study is noteworthy, considering that ROS and RNS are central in the cellular and biochemical process complexity of oxidative stress, which can be physiological (acting pro-hermetic) or pathogenic (producing destructive vicious circles) processes. ...
Background: Baobab fruit is valued for its nutritional and medicinal benefits. Although it is acknowledged that baobab pulp is beneficial for health, studies that link its nutraceutical properties to the ability to eliminate reactive species (ROS and RNS) are scarce. Methods: The nutritional profile and the antioxidant properties of baobab pulp extracts from Angola were evaluated. Thus, for the first time, the evaluation of in vitro scavenging capacity against the most physiologically relevant reactive oxygen species (ROS) and reactive nitrogen species (RNS) were the focus of investigation. Results: Angolan fruit pulp presented high contents of ash (8.0%) and total dietary fiber (52%). Vitamin E content was reported for the first time in fruit pulp. Green solvents were used to quantify bioactive compounds and antioxidant activity. Hydroalcoholic extracts exhibited the highest contents of phenolics (1573.0 mg/100 g) and flavonoids (768.7 mg/100 g). Thus, hydroalcoholic extracts showed higher antioxidant activity, and higher scavenging capacity for ROS (O2•−, H2O2, HOCl, ROO•) and RNS (•NO, ONOO⁻), being most active for •NO and ONOO⁻. Conclusion: For the first time, Angolan baobab fruit was described in respect to its nutritional contribution as well as its positive antioxidant effects, both as a functional food and as a nutraceutical ingredient.
... It is also being developed for its cosmeceutical potential (Rahul et al., 2015). Of significance is the medicinal value of A. digitata on various forms of pain (Fabiyi et al., 1993;Kamatou et al., 2011;Owoyele & Bakare, 2018;Ramadan, Harraz, & El-Mougy, 1994). Unlike most plants, all parts of A. digitata plant are shown to have helpful effects on pain perception. ...
... Interestingly, every part of the A. digitata plant appeared to be a potent pain killer. From its fruit pulp (Ramadan et al., 1994), seed and its oil (Kamatou et al., 2011), leaf (Fabiyi et al., 1993), bark (Owoyele & Bakare, 2018) to its root, A. digitata plant appears to be an excellent candidate for the development of a cheap and potent analgesic drug for various types of pain. The reported analgesic effects of A. digitata plant is limited neither by the diversity nor multifaceted nature of pain. ...
... The reported analgesic effects of A. digitata plant is limited neither by the diversity nor multifaceted nature of pain. Extracts from different parts of the plant were documented to favorably decrease pain perception associated with noxious thermal, chemical, and mechanical stimulus (Owoyele & Bakare, 2018). Also, specific types of pain such as neuropathic pain (Bakare, Oyewole, & Owoyele, 2019) and some symptomatic pain had all been shown to be mitigated by extracts from different parts of A. digitata plant. ...
Adansonia digitata (African baobab) is a long-living angiosperm classified as a member of Bombacoideae, a subfamily of Malvaceae. Today, the presence of African baobab tree is documented not only in Africa but also in South America, Asia, and Australia among others. Every part of baobab has been reported to be useful nutritionally or medicinally. The ethnopharmacological use of baobab includes: antimalarial, antidiabetic, analgesic effects, etc. Polyphenols, flavonoids (catechin, vitexin, quercetin, retin, etc.), mono- and poly-unsaturated fatty acids, and organic acids are some of the secondary metabolites identified in A. digitata. Also, potassium and calcium are the most abundant minerals present while the prominent trace elements are zinc and manganese. An increasing number of scientific studies have confirmed baobab analgesic properties. Neuropathic pain mitigation by A. digitata is linked to its flavonoids and mineral constituents. These substances alleviate neuropathic pain by a panoply of mechanisms including the inhibition of NF-κB to suppress inflammation, upregulation of Nrf2 to improve oxidative defense, inhibition of TRPV1 transcript to reduce pain, inhibition of NR2B subunit of NMDA receptor to suppress pain, and interaction of appropriate ion component like zinc with NR2A subunit of NMDA receptors to cause decrease transmission of pain signals, which together result to pain-relieving effects.
... The aqueous bark extracts considerably decreased the paw-licking time in the late phase (from 43.57 § 2.6 to 25.49 § 3.46 s) in comparison to the control group (66.31 § 5.04 s), with a significant difference (P < 0.05) (Owoyele and Bakare, 2018). Depending on the dosage, animals given the liquid extract from A. digitata bark showed a significantly longer response time (4.42 § 0.11 s) to heat stimuli than the control group (3.29 § 0.29 s) (Owoyele and Bakare, 2018). ...
... § 2.6 to 25.49 § 3.46 s) in comparison to the control group (66.31 § 5.04 s), with a significant difference (P < 0.05) (Owoyele and Bakare, 2018). Depending on the dosage, animals given the liquid extract from A. digitata bark showed a significantly longer response time (4.42 § 0.11 s) to heat stimuli than the control group (3.29 § 0.29 s) (Owoyele and Bakare, 2018). Traditional use of the A. digitata plant for inflammation management is supported by in vitro and in vivo animal models that show its potential as an anti-inflammatory agent source. ...
Purpose: Adansonia digitata L. is a highly esteemed and versatile tree native to Africa. It offers numerous benefits in terms of providing medication, food, clothing and serving as a vital source of natural remedies. The increasing demand for natural remedies as opposed to synthetic ones has prompted the exploration of several alternative natural products. The study reviewed research articles published from 2015 to January 2024 and indexed in the Scopus database to provide an up-to-date report on the species' scientific significance. and other pertinent terms. Results: It has been scientifically demonstrated that this plant's fruits, leaves, bark, roots, and seeds all have medicinal potential. This research highlighted the significant potential of the A. digitata tree as a valuable reservoir of phenolic and flavonoid compounds, which can be effectively harnessed for pharmacological purposes. Research undertaken in vitro and in vivo has provided evidence of this plant's helpful role in preventing and treating many ailments. The A. digitata tree exhibits significant potential as an antioxidant and antimicrobial agent as well as an antidiabetic and hepatoprotective agent. Conclusion: A comprehensive evaluation of the compounds identified in the A. digitata tree will yield extremely interesting results. The mechanism of action and clinical assessment should further be determined to ascertain the plant traditional, in vitro, and in vivo animal-documented results.
... The aqueous bark extracts considerably decreased the paw-licking time in the late phase (from 43.57 § 2.6 to 25.49 § 3.46 s) in comparison to the control group (66.31 § 5.04 s), with a significant difference (P < 0.05) (Owoyele and Bakare, 2018). Depending on the dosage, animals given the liquid extract from A. digitata bark showed a significantly longer response time (4.42 § 0.11 s) to heat stimuli than the control group (3.29 § 0.29 s) (Owoyele and Bakare, 2018). ...
... § 2.6 to 25.49 § 3.46 s) in comparison to the control group (66.31 § 5.04 s), with a significant difference (P < 0.05) (Owoyele and Bakare, 2018). Depending on the dosage, animals given the liquid extract from A. digitata bark showed a significantly longer response time (4.42 § 0.11 s) to heat stimuli than the control group (3.29 § 0.29 s) (Owoyele and Bakare, 2018). Traditional use of the A. digitata plant for inflammation management is supported by in vitro and in vivo animal models that show its potential as an anti-inflammatory agent source. ...
Purpose
Adansonia digitata L. is a highly esteemed and versatile tree native to Africa. It offers numerous benefits in terms of providing medication, food, clothing and serving as a vital source of natural remedies. The increasing demand for natural remedies as opposed to synthetic ones has prompted the exploration of several alternative natural products. The study reviewed research articles published from 2015 to January 2024 and indexed in the Scopus database to provide an up-to-date report on the species’ scientific significance.
Method
Searches for research papers have been conducted via Elsevier, Springer, Google Scholar, Taylor & Francis, PubMed, and Scopus using “A. digitata,” “chemical composition,” “antioxidant,” “antibacterial,” “antidiabetic,” “anticancer,” and other pertinent terms.
Results
It has been scientifically demonstrated that this plant's fruits, leaves, bark, roots, and seeds all have medicinal potential. This research highlighted the significant potential of the A. digitata tree as a valuable reservoir of phenolic and flavonoid compounds, which can be effectively harnessed for pharmacological purposes. Research undertaken in vitro and in vivo has provided evidence of this plant's helpful role in preventing and treating many ailments. The A. digitata tree exhibits significant potential as an antioxidant and antimicrobial agent as well as an antidiabetic and hepatoprotective agent.
Conclusion
A comprehensive evaluation of the compounds identified in the A. digitata tree will yield extremely interesting results. The mechanism of action and clinical assessment should further be determined to ascertain the plant traditional, in vitro, and in vivo animal-documented results.
... e test involved two distinct phases, early (neurogenic) and late (inflammatory) phases, and it was carried out to check the effects of the extract on inflammatory pain. Analgesic action of the extract to reduce paw licking time in both phases suggested the extract property as an opioid drugs to produce morphine-like effect for pain relief [68]. Moreover, several researchers had reported the contribution of glycosides, alkaloids, tannins, and flavonoids contained in plants for analgesic action [68]. ...
... Analgesic action of the extract to reduce paw licking time in both phases suggested the extract property as an opioid drugs to produce morphine-like effect for pain relief [68]. Moreover, several researchers had reported the contribution of glycosides, alkaloids, tannins, and flavonoids contained in plants for analgesic action [68]. ...
This review provides an updated and comprehensive overview on the ethnomedicinal use, phytochemistry, pharmacology, and toxicology of M. loriformis. Phytochemical analysis of M. loriformis revealed that it is composed of phenolics, flavonoids, condensed tannins, chlorophylls, alkaloids, and steroids. Numerous compounds including syringic acid, ß-O-D-glucopyranosyl-2-(2′-hydroxy-Z-6′-enecosamide) sphingosine, isovitexin, and 3β-O-D-glucopyranosyl-24ξ-ethylcholest-5-ene have been identified and isolated from this plant species. The present review attempts to bridge the gap between traditional use and pharmacological studies of M. loriformis while improving their existing therapeutic agents and product applications based on this plant.
... Analysis of the data obtained showed that the age of the respondents varied between 22 and 80 years, with a majority of the age group [41][42][43][44][45][46][47][48][49][50] at 34%. Then come the age groups [51][52][53][54][55][56][57][58][59][60], [31][32][33][34][35][36][37][38][39][40], [21][22][23][24][25][26][27][28][29][30] and finally those over 61, with a rate of 26%, 18.7%, 11.3% and 10% respectively. On the one hand, this could be explained by the ignorance of the traditional medicinal uses of plants by the younger generation. ...
... These results, which confirm the biological activity of these plants, explain the knowledge and practices in herbal medicine acquired by the inhabitants of the province. In fact, this research opens up new and interesting perspectives in the search for new therapeutic means, which can thus bring effective solutions by the manufacture of medicines sold in pharmacy for people suffering from hypertension International Journal of Pharmacology, Phytochemistry and Ethnomedicine Vol. 14 [27] Effective role in preventing weight gain, antiatherosclerotic and Cardioprotective [28,29] 2 Adansonia digitata Malvaceae Glutamic acid, aspartic acid, oleic acid, linoleic acid and palmitic acid [30] Analgesic, antioxidant, hepatoprotective [31][32][33] 3 ...
The use of plants to treat chronic diseases is part of an ancient Moroccan tradition. This study will present the first relevant documentation on medicinal plants used in the treatment of hypertension in Tarfaya province. This study aimed to collect and document information on medicinal plants traditionally used by the local population of Tarfaya province for the treatment of hypertension. Ethnobotanical surveys were conducted using 150 questionnaires in the study area. Documented data were evaluated using the quantitative ethno-botanical indices of frequency citation (FC) and Relative Frequency of Citation (RFC). The results obtained allowed to inventory 52 species of medicinal plants belonging to 29 families traditionally used against hypertension. The species were rich in diverse chemical constituents. The most cited families are Lamiaceae (9 species), Apiaceae (5 species), Compositae (3 species), Leguminosae (3 species) and Myrtaceae (3 species). Ten plants are reported for the first time as used in the treatment of hypertension. The most cited plant species are Allium sativum (RFC = 0.28), Allium cepa (RFC = 0.2), Olea europaea (RFC = 0.18), Searsia tripartita (RFC = 0.16), Ammodaucus leucotrichus (RFC = 0.15) and Myrtus communis (RFC = 0.15). Leaves were the most used organs. The decoction was the dominant method of preparation. This study showed that the inhabitants of Tarfaya use a wide variety of plants for the treatment of hypertension. This work is a source of information that can serve as a basis for phytochemists and pharmacologists interested in research on plants with antihypertensive effect.
... Allodynia and hyperalgesia are the main symptoms of peripheral neuropathy [45]. In this study, Wistar rats treated with the intraperitoneal injection of vincristine developed mechanical hyperalgesia and allodynia which are the major symptoms of neuropathic pain [46], and the use of analgesimeter (hyperalgesia) and Von Frey flaments (allodynia) for the evaluation of antinociceptive substances is widely adopted [47]. People (38%-100%) with cancer receiving chemotherapy treatment with anticancer drugs (paclitaxel, vincristine, and docetaxel) are subjected to peripheral neuropathy with allodynia and hyperalgesia as the main symptoms [48], which in most cases are resistant to efective analgesics on other pain models [49]. ...
Cissus quadrangularis Linn. (C. quadrangularis, Vitaceae) is a plant reported to treat injured tendons, broken bones, asthma, stomach ache, scurvy, and digestive disorders. The present study evaluated the antihyperalgesic effects of ethanolic extract of C. quadrangularis Linn. Vincristine sulfate (100 μg/kg, i.p.) was administered in rats for 10 days with 2 days break to induce painful peripheral neuropathy. Mechanical hyperalgesia and allodynia tests were performed to assess the threshold of painful neuropathy. Calcium levels in the sciatic nerve, oxidant stress markers, and levels of GABA and 5-HT were also determined in the brain and spinal cord after 15 days. Ethanolic extract of C. quadrangularis (180 and 360 mg/kg) and pregabalin (50 mg/kg) were administered for 15 consecutive days. The results revealed that the extract significantly (p<0.001) inhibited hyperalgesia and allodynia in animals after vincristine administration. The extract decreased total calcium levels in the sciatic nerve, MDA levels while increasing GSH activity, 5-HT level, as well as GABA levels in the brain and spinal cord. The results of this study suggest that the ethanolic extract of C. quadrangularis uses antioxidant capacity, calcium inhibitory action, and neuromodulation of GABA and 5-HT to prevent the development of painful neuropathy after vincristine administration. This demonstrates that C. quadrangularis is a promising molecule for the management of peripheral neuropathic pain induced by anticancer drugs.
... Consequently, the diuretic action is higher in mice that drank the plant-based beverage for 4 h. As far as it was possible to verify, although the "horchata" from Valencia is traditionally considered to have a diuretic effect, the literature describes a diuretic effect for both species that were used in this research to obtain this plant-based beverage, but this effect is not associated with the pulp of mukua or tubers of the tigernut, but with the leaves of both species (Bezerra et al., 2023;Owoyele and Bakare, 2018;Sánchez-Zapata et al., 2009). Thus, the diuretic action of plant-based beverage can be explained by its association with thermal water, as a solvent (Petraccia et al., 2006). ...
... This species is a multi-purpose tree which offers protection and provides clothing, food and medicine as well as raw material for many useful items [1][2][3][4][5][6][7][8][9] . The fruit pulp, seeds, leaves, flowers, roots and bark of baobab are edible and they have been studied by scientists for their pharmaceutical properties such as anti-asthma, antiviral, anti-anaemia, anti-oxidant, antimicrobial, anti-malarial, antidiarrhoea and anti-inflammatory activities [10][11][12][13][14][15][16][17][18] . The phytochemical analysis revealed presence of аlkaloids, saponins, flavonoids, tannins and terpenoids [6] . A. cruentus is an annual pseudo-cereal with broad leaves. ...
Adansonia digitata L. (Malvaceae) and Amaranthus cruentus L. (Amaranthaceae) leaves are consumed by people of northern of Côte d'Ivoire. Methanol extracts from these leaves have been investigated for their antibacterial activity and acute toxicity in rats. Antibacterial activity was evaluated by using agar diffusion and microdilution in 96 wells methods against Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa. The extracts acute toxicity were carried out based on OECD guidelines 423 with high limit dose of 2000 mg/kg body weight of test animal. All extracts had bacteriostatic activities against test bacteria with MICs values greater than 30 mg/ml. The highest dose administered did not produced mortality or changes in general behaviour of test animals. In conclusion consumption of leaves of Adansonia digitata and Amaranthus cruentus may prevent bacterial infections and is not toxic in experimental animals.
... These derangements were observed on the 3rd day post-CCI and lasted throughout the period of experiment. It has been shown that rats subjected to CCI elicited mechanical allodynia, cold allodynia and thermal hyperalgesia 15,16 . However, treatments with GS and CS resulted in a reduced response to pain behaviour by suppressing mechanical allodynia, cold allodynia and thermal hyperalgesia by increasing pain thresholds. ...
Neuropathic pain (NP) is an abnormality resulting from lesion or damage to parts of the somatosensory nervous system. It is linked to defective quality of life and often poorly managed. Due to the limited number of approved drugs, limited efficacy and side effects associated with the approved drugs, drugs or drug combinations with great efficacy and very minimal or no side effects will be of great advantage in managing NP. This study aimed at investigating the synergistic antinociceptive effects of the combination of glucosamine sulphate (GS) (240 mg/kg) and chondroitin sulphate (CS) (900 mg/kg) in chronic constriction injury (CCI)-induced neuropathy in rats. Forty-two Wistar rats were randomly distributed into seven groups (n = 6). Sciatic nerve was ligated with four loose ligatures to induce NP. Effects of drugs were examined on stimulus and non-stimulus evoked potentials, expression of dorsal root ganglia (DRG) pain modulators and structural architecture of DRG. Oral administration of GS and CS for 21 days reduced hyperalgesia, allodynia, sciatic nerve functional aberration and DRG pain modulators. Histopathology and immunohistochemistry revealed restoration of structural integrity of DRG. Our result showed that the combination of GS and CS produced antinociceptive effects by attenuating hyperalgesia, allodynia and downregulation of NP mediators. GS and CS additionally produced synergistic analgesic effect over its individual components.
... The presence of mechanical allodynia using von Frey filament following CCI as observed in this study have been variously reported. [41,42] Thermal stimulation has often been used to examine pain associated behavior in animals. [43] The benefits of thermal stimulation include the relative constant threshold across body sites, various psychophysical and physiological studies that has clearly established temperature range that result to heat nociception and its underlying mechanisms. ...
Objectives:
Damage to the peripheral and central nervous system lead to Neuropathic pain (NP) which is a widespread and devitalizing condition. chondroitin sulfate (CS), has been used in managing joint pain and osteoarthritis. In this study, the effectiveness of CS on NP induced by chronic constriction injury (CCI) is examined.
Methods:
Thirty Wistar rats were distributed at random into six groups (n = 5). Sciatic nerve ligation was carried out by encircling the nerve with four loose ligatures to induce NP. Allodynia (cold and mechanical) and heat hyperalgesia were assessed using Acetone, von Frey filament and Hot plate tests. CCI induction resulted to NP, prominent from the 3rd day after surgery. Structural architecture of sciatic nerves was evaluated via histological examination of the transverse section of the nerves.
Results:
Oral administration of CS (600 mg/kg and 900 mg/kg for 21 days) resulted in significant (P < 0.05) inhibition of allodynia (cold and mechanical) and thermal hyperalgesia. Lipid peroxidation, tumor necrosis factor-α (TNF-α), calcitonin gene related peptide (CGRP), C reactive protein (CRP), and oxidative stress were attenuated by CS. CS also improved interleukin (IL)-6, nitric oxide (NO), total antioxidant capacity (TAC).
Conclusion:
These findings suggest that CS attenuates allodynia, and thermal hyperalgesia induced by CCI by downregulating TNF-α, CRP, CGRP, oxidative enzymes, and upregulating IL-6, NO, and TAC. Nociceptive behavioral studies and histological findings showed significant improvement in the CS treated groups compared to CCI rats. These findings are responsible for the beneficial effect of CS in NP.
... Fruit pulp and leaf extracts of A. digitata improved the metabolism of carbohydrates and lipids [16,20,21]. Its aqueous extract demonstrated antimetabolic syndrome potential, remarked as weight loss, anti-inflammatory, hypolipidemic, hypoglycaemic, renal, hepatic, and cardio-protective activities [22,23] as well as analgesic effect [24]. Adeoye et al. [25] confirmed that apigenin and quercetin as secondary metabolites of ethylacetate partitioned fraction of A. digitata stem bark possess antimalarial activity, in silico. ...
Revalorization of Adansonia digitata L. “Baobab” pulp flour (BPF) to produce a notorious and functional cake in the current study was assessed. Wheat flour (WF 72%) was partially substituted by BPF at 5, 10, and 15% to prepare composite flour (WF + BPF) for potential cake manufacturing. Approximate chemical composition, macro- and microelements content, amino acids (AAs), total phenolic content (TPC), and antioxidant activity (AOA) of partially substituted composite flour (WF + BPF) were determined. The rheological properties of the composite flours were assessed using MIXOLAB. Moreover, an organoleptic evaluation of the baked cakes was performed with 20 trained panelists. The substitution with BPF significantly increased the total ash and crude fiber content in composite flour in a level-dependent manner, while moisture, crude fat, crude protein, available carbohydrates contents, and energy values were not significantly changed. Interestingly, macroelements such as Ca, K, and P were significantly increased, while Na was significantly decreased, whereas Mg content was not significantly changed. Similarly, microelements such as Zn, Fe, and Cu increased with the increase of BPF substitution. Significant increases in TPC and AOA were found by increasing the substitution with BPF. The biological value (BV), essential amino acid index (EAAI), protein efficiency ratio (PER), as well as essential amino acids (EAAs) requirement index (RI) were positively improved in WF + BPF. Adding BPF up to 10% not only improved the water absorption, α-amylase activity, and viscosity, but also caused a slight weakness in the gluten network, to produce a composite flour suitable for cake making. Conclusively, this study revealed that fortification with BPF up to 5–10% improved the nutritional quality without adverse effects on technological, and organoleptic characteristics and providing economic, commercial, and health benefits.
... Leaves, bark and fruits of this tree are traditionally employed in several African countries as food and for medicinal purposes, and for these reasons baobab is named as "the small pharmacy" or "chemist tree" [13]. It is well established for its antioxidant properties [14], anti-inflammatory [15,16], antipyretic activity [17], analgesic property [15]; Bamidele and Ahmed, [18], Hepatoprotective properties [19], antimicrobial activity [20]; antiviral activity [21], antitrypanosomal activity [22], antidiarrheal activity [23]. The pulp is therapeutically utilized as analgesic, antidiarrhoea/ antidysentery and for treatment of smallpox and measles [24]. ...
Objectives
The role of aqueous extract of Adansonia digitata was investigated against cadmium chloride-induced testicular damage in Wistar Rats.
Methods
Thirty (30) male Wistar Rats weighing (150–170) were divided into six groups (n=5). Group A served as control and received oral administration of phosphate buffer saline; group B received 800 mg/kg A. digitata only; group C were injected intraperitoneally with single dose 2 mg/kg b.w cadmium chloride; group D were injected intraperitoneally with single dose 2 mg/kg b.w cadmium chloride and treated with 800 mg/kg aqueous extract of A. digitata ; group E received 300 mg/kg vitamin E only; group F were injected intraperitoneally with single dose 2 mg/kg b.w cadmium chloride and treated with 300 mg/kg vitamin E. After 21 days, the animals were sacrificed by cervical dislocation, the testes were excised fixed in Bouins fluids for histological analysis and the other homogenized in 5% sucrose solution for determination of tissue malondialdehyde (MDA) and antioxidant enzyme activity, biochemical assay.
Results
The group treated with cadmium chloride plus A. digitata caused significant decrease in MDA levels with significant increase (p<0.05) in antioxidant activities and biochemical enzymes when compared to cadmium chloride only group.
Conclusions
Aqueous extract of A. digitata appears to have ameliorative effect against cadmium chloride-induced testicular damage. This could be attributed to the presence of polyphenolic compound.
... toms of neuropathic pain that can be modeled in animal studies [23]. The use of a hotplate for the screening of antinociceptive substances has been widely adopted and it has been linked to biochemical substances that act centrally at both the spinal and supra-spinal levels [24,25]. ...
Background:
The continuous search for a novel neuropathic pain drug with few or no side effects has been a main focus of researchers for decades. This study investigated the antinociceptive and neuroprotective effects of bromelain in sciatic nerve ligation-induced neuropathic pain in Wistar rats.
Methods:
Forty-eight Wistar rats randomly divided into eight groups comprised of six animals each were used for this study. Peripheral neuropathy was induced via chronic constriction of the common sciatic nerve. Thermal hyperalgesic and mechanical allodynia were assessed using a hotplate and von Frey filaments, respectively. The functional recovery and structural architecture of the ligated sciatic nerve were evaluated using the sciatic functional index test and a histological examination of the transverse section of the sciatic nerve. The neuroprotective effects of bromelain were investigated in the proximal sciatic nerve tissue after 21 days of treatment.
Results:
Bromelain significantly (P < 0.05) attenuated both the thermal hyperalgesia and mechanical allodynic indices of neuropathic pain. There were improvements in sciatic function and structural integrity in rats treated with bromelain. These rats showed significant (P < 0.05) increases in sciatic nerve nuclear transcription factors (nuclear factor erythroid-derived-2-related factors-1 [NrF-1] and NrF-2), antioxidant enzymes (superoxide dismutase and glutathione), and reduced membrane-lipid peroxidation compared with the ligated control group.
Conclusions:
This study suggest that bromelain mitigated neuropathic pain by enhancing the activities of nuclear transcription factors (NrF-1 and NrF-2) which increases the antioxidant defense system that abolish neuronal stress and structural disorganization.
... Since the inception of man, plants remain the cheapest natural sources of medicine, food supplement and poison. Recently, our lab reported anti-nociceptive property of Adansonia digitata bark in normal rats (Owoyele and Bakare 2018). The present study reinforced the earlier report and demonstrated Adansonia digitata plant as potential source of cheap oral antinociception effective in the treatment of neuropathic pain, a chronic pain that affects quality of life in millions of people around the world. ...
Diverse etiology of neuropathic pain conditions demands new understanding of its pathogenesis and development of effective therapy. Treatment of induced neuropathic pain using aqueous Adansonia digitata bark extract has not been investigated. We probed the systemic administration effects of A. digitata bark extract on sciatic nerve ligated induced neuropathic pain. Treatments with extract caused increased pain threshold on hot plate, hot- and cold-immersion test. Notably, an apparent decreased in systemic prostaglandin E2 occurred concurrently with strengthened oxidative defense system. By contrast, extract-hexamethonium, -propranolol, -atropine or -prazosin cotreatments in induced-neuropathic rats suggested no involvement of muscarinic, nicotinic, beta or alpha-1 receptors in the analgesic action of the extract. Though, a weaken oxidative defense system was observed based on oxidative markers measured. These results indicate the crude extract ability to induce pain relief in neuropathic pain and this coincides with degree of decreased PGE2 and increased antioxidants as well as decreased lipid peroxidation product. This is the first report demonstrating the usefulness of aqueous A. digitata bark extract in the management of neuropathic pain, an action that involves alteration of PGE2 and oxidative defense system.
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... Analgesics are class of drugs that act on central or peripheral nervous system to relieve pain selectively without altering consciousness [40]. The hot plate test excites supra-spinal neurons [41,42]. The results of hot plate and tail flick test reveal that PVFO possess significant analgesic activity with both doses. ...
The seeds of Phaseolus vulgaris are known as common beans or kidney beans. The dry seeds are eaten as pulse and are enriched with protein, fiber, starch, B vitamins (B1, B6, B9), iron, potassium and selenium. Beans also contain about 1-2 % of fixed oil. Phaseolus vulgaris is linked with anticancer, antihyperlipidemic, hypoglycemic and antioxidant actions. The fixed oil of Phaseolus vulgaris (PVFO) seeds is extracted with hexane and used in this study to assess acute oral toxicity, analgesic (by acetic acid induced writhing, hot plate and tail flick tests in mice) and anti-inflammatory (by carrageenan induced paw edema in rats) actions. Four groups were made (n=6): Group-I: Normal Saline Control (2ml/kg), Group-II: PVFO (2ml/kg), Group-III: PVFO (4ml/kg) and Group-IV: Standard Acetyl salicylic acid (ASA 300 mg/kg). PVFO in 2ml/kg and 4ml/kg dose demonstrated analgesic and anti-inflammatory activities but in hot plate results were unreliable as here significant activity started after 90 minutes. For toxicity test 5ml/kg dose was administered orally in mice and no toxicity symptoms were observed. It is therefore concluded that PVFO is safe for oral use up to 5ml/kg and may possess analgesic and anti-inflammatory actions.
Traditional Medicine in North East Africa: Research on Traditional Healer Preparations and Herbs explores the rich tapestry of traditional healing practices in North East Africa. This comprehensive work compiles the profound knowledge of indigenous herbalists and explores the intricate relationship between traditional healing and medicinal plants.
From combating diseases like cancer and diabetes to managing snakebites and obesity-related conditions, each chapter offers a detailed examination of plant-based remedies. Highlighting the contributions of plants like Moringa oleifera and Citrullus colocynthis, this book bridges the gap between ancient wisdom and modern research, making it essential for academics, researchers, and anyone interested in the healing powers of nature. Join us on this enlightening journey as we celebrate cultural diversity and uncover the enduring legacy of traditional medicine.
Key Features:
- In-depth studies on bioactive compounds and therapeutic properties of key African plants.
- Ethnobotanical insights into traditional healer practices.
- Comprehensive reviews linking traditional plant use to modern medical applications.
Ice cream’s appeal is unrivaled. Nonmilk and milk ingredients in ice cream formulas affect their nutritional value, structure, and organoleptical qualities. Seeking novel dietary ingredients instead of artificial flavoring compounds is vital for improving ice cream taste preference, adding antioxidants, and increasing nutritional value. The current study examines the feasibility of manufacturing a new flavored ice cream with excellent dietary value using Adansonia digitata L. (Baobab) fruit pulp (ADFP). The prepared ice cream’s physicochemical and microbiological quality, and rheological, microstructural, and organoleptic properties were investigated. Using ADFP instead of skim milk powder with a partial or complete replacement, five ice cream samples were produced and marked as IB-0, IB-25, IB-50, IB-75, and IB-100. Chemical characteristics were not noticeably impacted except protein and ash, which considerably decreased with increasing ADFP levels. Increasing ADFP in the samples increased titratable acidity and reduced pH. All ice cream samples were microbiologically acceptable with no pathogenic bacteria. By increasing ADFP in the samples, the daily values (%DV) of sodium, potassium, and magnesium were not considerably affected. Calcium reduced from 14.91% in IB-0 to 7.75% in IB-100. All microelements found in the study rose considerably as ADFP increased. Increasing ADFP levels significantly boosted antioxidant levels. The IB-100 sample had the highest total phenolic content (149.29 mg GAE 100 g⁻¹), antioxidant activity (98.12 µmol of TE 100 g⁻¹), total flavonoids (5.96 mg QE 100 g⁻¹), and total flavanols (4.01 mg QE 100 g⁻¹). The inclusion of ADFP had a beneficial effect on the color of the samples. It did not negatively affect the ice cream’s organoleptic acceptability as determined by organoleptic, rheological, and microstructural examinations. Interestingly, when skim milk powder was replaced with 50% and 75%, the hardness, viscosity, and aqueous phase separation were significantly improved. In conclusion, ADPF improves the nutritional value of ice cream and can be used as a natural coloring ingredient without affecting microstructural and rheological properties.
Background
Adansonia digitata has been used as a traditional medicine to treat various diseases including snakebite envenomation.
Objective
In this study, the protective and ameliorative potentials of crude methanol extract of Adansonia digitata fruit pulp against crude venom of Naja nigricollis in-vitro and in-vivo were investigated.
Method
The dose-dependent inhibitory studies, pharmacological, histopathological and in vivo studies were conducted using standard methods.
Result
The mean lethal dose of the crude methanolic extract of Adansonia digitata fruit pulp in Wistar rats was >5,000 mg/kg, while Naja nigricollis venom was 0.89 mg/kg. The anti-lethality effective concentration of the fruit pulp on Naja nigricollis venom was 92.52 mg/ml. Treatment significantly (p < 0.05) inhibited the activities of Naja nigricollis phospholipase A2 and dose-dependently reduced Naja nigricollis venom-induced paw oedema at 1-4 hours post-envenomation. In-vivo, treatment with 250 and 500 mg/kg of Adansonia digitata fruit pulp was protective against the clinical signs and mortality. Serum acetylcholinesterase activities were maintained in the group treated with normal saline and the ameliorative groups but decreased significantly (p < 0.05) in other groups. Brain acetylcholinesterase was high in all the groups by day 1 but was reduced with increasing dose by day 2 in the ameliorative groups only. Adansonia digitata fruit pulp also preserved the histoarchitecture of the brain, heart, liver and spleen from venom-induced pathologies.
Conclusion
Crude methanolic extract of Adansonia digitata fruit pulp possesses good protective and ameliorative neutralization effects on Naja nigricollis venom and could be promising in the management of snakebite envenomation.
Adansonia digitata L. (Malvaceae), commonly known as ‘baobab’, is a large, seasonal tree distributed in many parts of Africa. It is more prevalent in Botswana, Namibia, Zimbabwe, Malawi, Mozambique, South Africa, Mali, the Ivory Coast, Senegal, Cameroon, Uganda, Kenya and Tanzania. Baobab is a very important non-timber forest product (NTFP) and contributes to the livelihoods of the African people. Various parts of the tree are used in African traditional medicine in the treatment of numerous ailments such as tuberculosis, malaria, fever, diarrhoea, microbial infections, anaemia and toothache. In addition, various plant parts are used as sources of food. The seed oil is applied topically as medicine or cosmetic. Several in vitro and in vivo pharmacological activities, including antimicrobial, anti-oxidant, anti-inflammatory, antimalarial and antidiabetic have been noted. Much research has been done on the nutritive value of the fruit pulp, seed kernels and seed oil. Chromatography techniques, such as semi-automated high-performance thin-layer chromatography (HPTLC), ultra-performance liquid chromatography coupled to mass spectrometry (UPLC–MS), and gas chromatography coupled to mass spectrometry (GC–MS), were used to determine the chemical profiles of A. digitata fruit pulp and seed oil. Several compounds, including procyanidin dimer I, epicatechin, procyanidin dimer II, kaempferol glycoside I and kaempferol glycoside II, were identified in the fruit pulp using UPLC–MS, whilst palmitic acid, stearic acid, linoleic acid and oleic acid were the major fatty acids detected in the seed oil, following esterification and analysis using GC–MS. The presence of some of the compounds was confirmed using HPTLC under 366 nm radiation.
Cissus quadrangularis Linn. (Vitaceae) is a plant used to treat injured tendons, broken bones, asthma, stomach ache, scurvy and digestive disorders. The present study purposed to evaluate the antihyperalgesic effects ( in vivo ) and the immunomodulatory, antioxidant and anti-inflammatory properties ( in vitro ) of aqueous and ethanolic extracts of Cissus quadrangularis ( C. quadrangularis ). Immunomodulatory (chemiluminescence, cytokines and cell proliferation), anti-inflammatory (protein denaturation, 5-lipoxygenase, cyclooxygenase 1 and 2) and antioxidant (DPPH, ABTS and NO) tests were performed in vitro, while the anti- hyperalgesic (vincristine) investigations were conducted in vivo on Wistar rats. The results revealed that extracts developed immunomodulatory activity by inhibiting the production of ROS (intracellular/extracellular), of TNFα, IL-1β, IL-6 as well as inhibiting cell proliferation, and by stimulating the production of IL-10. The anti-inflammatory activity of the extracts was demonstrated by an inhibition of 5-LOX, protein denaturation and cyclooxygenases 1 and 2. In addition, extracts showed interesting scavenging effects, attesting their antioxidant potential. The extracts administered to the animals (180 and 360 mg/kg) inhibited (p < 0.001) hyperalgesia and allodynia in animals. These extracts also led to the reduction in serum and sciatic nerve levels of TNFα, IL-1β and IL-6, as well as to an increase in cell growth factors (NGF and IGF) production of treated animals. These results suggest that extracts of C. quadrangularis use immunomodulatory, anti-infammatory and antioxidant capacity to prevent and/cure painful neuropathy after vincristine administration. C. quadrangularis is therefore a promising natural substance for the management of neuropathic pain.
Adansonia digitata L. (Malvaceae), commonly known as ‘baobab’, is a large tree used in Africa for its medicinal and nutritional value. In many African countries, different plant parts are used to treat malaria, diarrhoea, fever, inflammation, kidney and bladder diseases. Baobab is a rich source of vitamin C, yielding levels of ascorbic acid rivalling many commercial fruits. Various in vitro and in vivo biological activities of various parts of the plant have been investigated, and results showed promising anti-oxidant, anti-inflammatory and antiviral properties. Here, we propose a quality control protocol for A. digitata based on chromatographic profiling of the non-volatile fraction from the fruit pulp and seed oil constituents. Using a semi-automated high-performance thin-layer chromatography (HPTLC) system, ultra-performance liquid chromatography coupled to mass spectrometry and photodiode array detection (UPLC-MS-PDA), and gas chromatography coupled to mass spectrometry and a flame ionisation detection (GC-MS-FID), the chemical profiles of six specimens of A. digitata were established. The fruit pulp was obtained commercially and extracted with methanol. The seed oils (commercial samples) were obtained by the cold pressing method and the fatty acid methyl esters (FAMEs) obtained by esterification. The non-volatile fractions were analysed using HPTLC and UPLC-MS-PDA, while the FAMEs were profiled using HPTLC and GC-MS-FID. Various compounds, including procyanidin dimer I, epicatechin, procyanidin dimer II, kaempferol glycoside I and kaempferol glycoside II, were identified in the fruit pulp using UPLC-MS-PDA, while HPTLC confirmed the presence of ascorbic acid, catechin and epicatechin in the fruit pulp. Analysis of the seed oil by GC-MS revealed the presence of four major FAMEs, namely palmitic acid, stearic acid, linoleic acid and oleic acid methyl esters.
Adansonia digitata L. (Malvaceae) is commonly known as baobab tree native to Africa. Baobab is a multi-purpose tree which offers protection and provides food, clothing and medicine as well as raw material for many useful items. The fruit pulp, seeds, leaves, flowers, roots, and bark of baobab are edible and they have been studied by scientists for their useful properties. The fruit pulp have very high vitamin C, calcium, phosphorus, carbohydrates, fibers, potassium, proteins and lipids content, which can be used in seasoning as an appetizer and also make juices. Seeds contain appreciable quantities of phosphorus, magnesium, zinc, sodium, iron, manganese, whereas they have high levels of lysine, thiamine, calcium and iron. Baobab has numerous biological properties including antimicrobial, anti-malarial, diarrhoea, anaemia, asthma, antiviral, anti-oxidant and anti-inflammatory activities amongst others. Phytochemical investigation revealed the presence of flavonoids, phytosterols, amino acids, fatty acids, vitamins and minerals. The review summarizes the information on various aspects of traditional information, taxonomic description, medicinal properties and importantly nutritional value.
Leonurus cardiaca, commonly known as motherwort, is a member of the Lamiaceae family. It has a number of interesting biological activities, for example, sedative and hypotensive, antioxidant, anti-inflammatory, and antimicrobial activities. The aim of the present study was to investigate the effect of alcoholic extract of aerial part of Leonurus cardiaca on nociceptive response using formalin, tail flick, and hot plate tests in mice. The acute treatment of mice with an ethanolic extract at doses of 500 and 250 mg/kg by intraperitoneal administration produced a significant antinociceptive in the first and second phases of formalin test, respectively. The hot plate and tail flick tests showed an increase in the antinociceptive effect at dose 500 mg/kg. These results suggest that Leonurus cardiaca possesses central and peripheral antinociceptive actions.
This study examined the total polyphenol content of eight wild edible plants from Ethiopia and their effect on NO production in Raw264.7 cells. Owing to its relatively high polyphenol concentration and inhibition of NO production, the methanol extract of Adansonia digitata L. leaf (MEAD) was subjected to detailed evaluation of its antioxidant and anti-inflammatory effects. Antioxidant effects were assessed by measuring free-radical-scavenging activity using 1,1-diphenyl-2-picrylhydrazyl (DPPH) and oxygen-radical-absorbance capacity (ORAC) assays, while anti-inflammatory effects were assessed by measuring inducible nitric oxide synthase (iNOS) expression in lipopolysaccharide (LPS)-stimulated RAW264.7 cells. In the ORAC assay, MEAD was 10.2 times more potent than vitamin C at eliminating peroxyl radicals. In DPPH assay, MEAD also showed a strong ROS scavenging effect. MEAD significantly inhibited iNOS activity (IC50=28.6 μg/ml) of LPS-stimulated Raw264.7 cells. We also investigated the relationship between iNOS expression and nuclear factor kappa B (NF-κB) activation. MEAD inhibited IκBα degradation and NF-κB translocation from the cytosol to the nucleus in LPS-induced RAW264.7 cells without significant cytotoxic effects, as confirmed by MTT assay. These results suggest that MEAD inhibits anti-inflammatory iNOS expression, which might be related to the elimination of peroxyl radicals and thus the inhibition of IκBα-mediated NF-κB signal transduction.
Cognitive dysfunction is a major health problem in the 21st century, and many neuropsychiatric disorders and neurodegenerative disorders, such as schizophrenia, depression, Alzheimer's Disease dementia, cerebrovascular impairment, seizure disorders, head injury and Parkinsonism, can be severly functionally debilitating in nature. In course of time, a number of neurotransmitters and signaling molecules have been identified which have been considered as therapeutic targets. Conventional as well newer molecules have been tried against these targets. Phytochemicals from medicinal plants play a vital role in maintaining the brain's chemical balance by influencing the function of receptors for the major inhibitory neurotransmitters. In traditional practice of medicine, several plants have been reported to treat cognitive disorders. In this review paper, we attempt to throw some light on the use of medicinal herbs to treat cognitive disorders. In this review, we briefly deal with some medicinal herbs focusing on their neuroprotective active phytochemical substances like fatty acids, phenols, alkaloids, flavonoids, saponins, terpenes etc. The resistance of neurons to various stressors by activating specific signal transduction pathways and transcription factors are also discussed. It was observed in the review that a number of herbal medicines used in Ayurvedic practices as well Chinese medicines contain multiple compounds and phytochemicals that may have a neuroprotective effect which may prove beneficial in different neuropsychiatric and neurodegenerative disorders. Though the presence of receptors or transporters for polyphenols or other phytochemicals of the herbal preparations, in brain tissues remains to be ascertained, compounds with multiple targets appear as a potential and promising class of therapeutics for the treatment of diseases with a multifactorial etiology.
Interesting analgesic activity has been previously identified in alkaloids isolated from the genus Psychotria (Rubiaceae). We here report the analgesic activity of umbellatine, a new glycoside indole monoterpene alkaloid isolated from Psychotria umbellata. Umbellatine produced a dose-dependent (100-300 mg/kg) analgesic effect, partially reversed by naloxone, in the tail-flick and hot-plate models. These results suggest an analgesic effect at least in part associated with the activation of opioid receptors. In the formalin- and capsaicininduced pain models, umbellatine (100-300 mg/kg) elicited significant and dose-related antinociception. Umbellatine acts synergistically when co-administered with the NMDA antagonist MK-801. These results indicate the involvement of NMDA receptors in the umbellatine mechanism of action. Such a combined mode of action can be of relevance for developing analgesics useful in neurophatic pain.
Evaluation of hypoglycemic activity of methanolic stem bark extract of Adansonnia digitata in Wistar rats has beeninvestigated. Antidiabetic potentials of the plant extract at the doses of 100,200 and 400 mg/kg intraperitoneally administered onStreptozocin diabetes Wistar rats. Treatment of streptozocin diabetic Wistar rats with the extract caused a significant (P<0.05)reduction in the blood glucose levels when compared with control. The dose of 100mg/kg shown a significant decreased (p<0.05)after 1, 3 5 and 7 hours of extract administration when compared to control normal saline. Also the dose of 200 mg/kg shown asignificant decreased (p<0.05) after 3, 5 and 7 hours of extract administration. The dose of 400 mg/kg also shown a significantdecreased( p<0.05) after 5 and 7 hours of extract administration when compared to control normal saline. The highest activity residesat the dose of 100 mg/kg with percentage glycemic change of 51 % after 7 hours of extract administration while the other two doses200 and 400 mg/kg have glycemic change of 39% and 31% respectively after 7 hours of extract administration. The phytochemicalscreening revealed the presences of tannins, carbohydrate, terpenes, saponins, flavonoids and alkaloids. The median lethal dose (LD50) in mice was calculated to be 1264.9 mg/kg bodyweight. This result suggests that the methanolic stem bark of Adansonniadigitata possess antidiabetic effect on streptozocin induced diabetic Wistar rats.Industrial relevance: The herbal medicines are getting more importance in the treatment
Treatment with proinflammatory prostaglandin E2 (PGE2) produced a transient sensitization of whole-cell currents elicited by the vanilloid capsaicin. The intracellular signaling pathways that mediate the initiation of this PGE2-induced sensitization of the capsaicin-elicited current in rat sensory neurons are not well established. Treatment with either forskolin (100 nM to 10 microM) or membrane-permeant analogs of cAMP, 8-bromo-cAMP (8-Br-cAMP) and chlorphenylthio-cAMP (10 microM to 1 mM), transiently sensitized neuronal responses elicited by capsaicin in a manner analogous to that produced by PGE2. The duration of sensitization was lengthened with increasing concentrations of forskolin; however, higher concentrations of 8-Br-cAMP or chlorphenylthio-cAMP led to a shortening of sensitization. The inactive analog of forskolin, dideoxy-forskolin, had no effect on capsaicin responses. Inclusion of the inhibitor of protein kinase A in the recording pipette completely suppressed the sensitization produced by PGE2 or forskolin. In recordings from membrane patches in the cell-attached configuration, the bath application of capsaicin evoked single-channel currents in which the level of channel activity was concentration-dependent and had an EC50 of 1.4 microM. These single-channel currents evoked by capsaicin exhibited an apparent reversal potential of +4 mV and were blocked by the capsaicin antagonist capsazepine. Exposure of the sensory neuron to either PGE2 or forskolin produced a large and transient increase in the mean channel activity (NPo) elicited by capsaicin, although the unitary conductance remained unaltered. Taken together, these observations suggest that modulation of the capsaicin-gated channel by the cAMP-protein kinase A signaling pathway enhanced the gating of these channels and consequently resulted in the sensitization of the whole-cell currents.
Despite the crucial role that prostaglandins (PGs) have in the sensitization of the central nervous system to pain, their cellular and molecular targets leading to increased pain perception have remained elusive. Here we investigated the effects of PGE(2) on fast synaptic transmission onto neurons in the rat spinal cord dorsal horn, the first site of synaptic integration in the pain pathway. We identified the inhibitory (strychnine-sensitive) glycine receptor as a specific target of PGE(2). PGE(2), but not PGF(2 alpha), PGD(2) or PGI(2), reduced inhibitory glycinergic synaptic transmission in low nanomolar concentrations, whereas GABAA, AMPA and NMDA receptor-mediated transmission remained unaffected. Inhibition of glycine receptors occurred via a postsynaptic mechanism involving the activation of EP2 receptors, cholera-toxin-sensitive G-proteins and cAMP-dependent protein kinase. Via this mechanism, PGE(2) may facilitate the transmission of nociceptive input through the spinal cord dorsal horn to higher brain areas where pain becomes conscious.
Prostaglandin E2 (PGE2) is a crucial mediator of inflammatory pain sensitization. Here, we demonstrate that inhibition of a specific glycine receptor subtype (GlyR alpha3) by PGE2-induced receptor phosphorylation underlies central inflammatory pain sensitization. We show that GlyR alpha3 is distinctly expressed in superficial layers of the spinal cord dorsal horn. Mice deficient in GlyR alpha3 not only lack the inhibition of glycinergic neurotransmission by PGE2 seen in wild-type mice but also show a reduction in pain sensitization induced by spinal PGE2 injection or peripheral inflammation. Thus, GlyR alpha3 may provide a previously unrecognized molecular target in pain therapy.
The aqueous extract of A. digitata fruit pulp showed a LD50 in mice by i.p. route of 8000 mg/kg and induced a marked and long lasting anti-inflammatory and antipyretic effects at 400 and 800 mg/kg per os in rats. The extract showed also a marked analgesic activity in mice at 2 h after administration. Phytochemical screening of the fruit pulp of the plant indicated the presence of sterols and/or triterpenes, saponins, tannins, carbohydrates and glycosides.
Context:
The roots of Alafia barteri Oliver (Apocynaceae), Combretum mucronatum Schumach (Combretaceae) and Capparis thonningii Schum (Capparaceae) are used in Traditional African Medicine to alleviate painful and inflammatory conditions.
Objective:
This study investigated the analgesic and anti-inflammatory effects of the methanol root extracts of Alafia barteri (MeAB), C. mucronatum (MeCM), and Capparis thonningii (MeCT).
Materials and methods:
Analgesic activity of the extracts (50, 100, and 200 mg/kg, p.o. 1 h) was evaluated using acetic acid-, formalin- and hot plate-induced pain while anti-inflammatory actions (100 or 200 mg/kg) were investigated using the carrageenan- and xylene-induced edema tests.
Results:
MeAB, MeCM, and MeCT (200 mg/kg) inhibited acetic acid-induced abdominal constriction by 55.07, 46.67, and 47.25%, respectively. In the formalin test, the index of pain inhibition of early and late phases was, respectively, 47.83 and 81.98% for MeAB, 56.10 and 63.81% for MeCM, and 42.84 and 63.29% for MeCT (200 mg/kg). MeAB and MeCT pretreatments significantly increased the reaction time by 46.67 and 25.53%, respectively, 120 min post-treatment in the hot-plate test. Naloxone (5 mg/kg, s.c.) pretreatment 15 min before extract administration, significantly (p < 0.05) reversed the analgesic effect of MeAB and MeCT in the formalin test. MeAB, MeCM, and MeCT showed significant anti-inflammatory activity with 60.44 and 30.39%, 63.74 and 58.08%, and 50.55 and 77.84% (200 mg/kg, 4 h), respectively, inhibition of paw and ear edema.
Discussion and conclusion:
The analgesic and anti-inflammatory effects of MeAB and MeCT involve an interaction with opioid pathway and/or inhibition of chemical mediators of pain and inflammation.
In the last decade the number of bioscience journals has increased enormously, with many filling specialised niches reflecting new disciplines and technologies. The emergence of open-access journals has revolutionised the publication process, maximising the availability of research data. Nevertheless, a wealth of evidence shows that across many areas, the reporting of biomedical research is often inadequate, leading to the view that even if the science is sound, in many cases the publications themselves are not "fit for purpose", meaning that incomplete reporting of relevant information effectively renders many publications of limited value as instruments to inform policy or clinical and scientific practice [1-21]. A recent review of clinical research showed that there is considerable cumulative waste of financial resources at all stages of the research process, including as a result of publications that are unusable due to poor reporting [22]. It is unlikely that this issue is confined to clinical research [2-14,16-20].
Peroxynitrite (PN; ONOO⁻) and its reactive oxygen precursor superoxide (SO; O₂•⁻) are critically important in the development of pain of several etiologies including pain associated with chronic use of opiates such as morphine (also known as opiate-induced hyperalgesia and antinociceptive tolerance). This is now an emerging field in which considerable progress has been made in terms of understanding the relative contributions of SO, PN, and nitroxidative stress in pain signaling at the molecular and biochemical levels. Aggressive research in this area is poised to provide the pharmacological basis for development of novel nonnarcotic analgesics that are based upon the unique ability to selectively eliminate SO and/or PN. As we have a better understanding of the roles of SO and PN in pathophysiological settings, targeting PN may be a better therapeutic strategy than targeting SO. This is because, unlike PN, which has no currently known beneficial role, SO may play a significant role in learning and memory. Thus, the best approach may be to spare SO while directly targeting its downstream product, PN. Over the past 15 years, our team has spearheaded research concerning the roles of SO and PN in pain and these results are currently leading to the development of solid therapeutic strategies in this important area.
Pain is ubiquitous. At some point in time it affects everyone. For many millions pain becomes chronic, a scourge that impacts every facet of life—work, hobbies, family relations, social fabric, finances, happiness, mood, and even the very essence of identity. According to the National Institutes of Health (NIH), pain is one of our most important national public health problems, a silent epidemic. In 1998, NIH reported that the annual amount spent on health care, compensation, and litigation related to pain had reached one hundred billion dollars ($100,000,000,000). Considering that health care costs have doubled since then, it is not unreasonable to assume that the costs related to pain care have doubled as well.
In Brazilian folk medicine, the leaves of Garcinia brasiliensis are used to treat tumors, inflammation of the urinary tract and arthritis as well as to relieve pain. Nevertheless, scientific information regarding Garcinia brasiliensis is limited; there are no reports related to its possible anti-inflammatory and antinociceptive effects. This study employed in vivo inflammatory and nociceptive models to evaluate the scientific basis for the traditional use of Garcinia brasiliensis.
Carrageenan-induced paw edema, peritonitis and fibrovascular tissue growth induced by s.c. cotton pellet implantation were used to investigate the anti-inflammatory activity of Garcinia brasiliensis ethanolic extract (GbEE) in rats. Formalin and acetic acid-induced writhing tests were used to investigate the antinociceptive activity in mice.
GbEE at test doses of 30-300 mg/kg p.o. clearly demonstrated anti-inflammatory effects by reduced paw edema induced by carrageenan, inhibited leukocyte recruitment into the peritoneal cavity, and in the model of chronic inflammation using the cotton pellet-induced fibrovascular tissue growth in rats, the GbEE significantly inhibited the formation of granulomatous tissue. The extracts at test doses of 30-300 mg/kg, p.o., clearly demonstrated antinociceptive activity, except for the first phase of the formalin test.
GbEE markedly demonstrated anti-inflammatory action in rats and antinociceptive activity in mice, which supports previous claims of the traditional use of species of the Garcinia genus for inflammation and pain.
The formalin test in mice is a valid and reliable model of nociception and is sensitive for various classes of analgesic drugs. The noxious stimulus is an injection of dilute formalin (1% in saline) under the skin of the dorsal surface of the right hindpaw. The response is the amount of time the animals spend licking the injected paw. Two distinct periods of high licking activity can be identified, an early phase lasting the first 5 min and a late phase lasting from 20 to 30 min after the injection of formalin. In order to elucidate the involvement of inflammatory processes in the two phases, we tested different classes of drugs in the two phases independently. Morphine, codeine, nefopam, and orphenadrine, as examples of centrally acting analgesics, were antinociceptive in both phases. In contrast, the non-steroid anti-inflammatory drugs indomethacin and naproxen and the steroids dexamethasone and hydrocortisone inhibited only the late phase, while acetylsalicylic acid (ASA) and paracetamol were antinociceptive in both phases. The results demonstrate that the two phases in the formalin test may have different nociceptive mechanisms. It is suggested that the early phase is due to a direct effect on nociceptors and that prostaglandins do not play an important role during this phase. The late phase seems to be an inflammatory response with inflammatory pain that can be inhibited by anti-inflammatory drugs. ASA and paracetamol seem to have actions independent of their inhibition of prostaglandin synthesis and they also have effects on non-inflammatory pain.
Previous in vitro and in vivo studies have determined that the d isomer of methadone has N-methyl-D-aspartate (NMDA) receptor antagonist activity. The present studies examined the ability of d-methadone to attenuate the development of morphine tolerance in mice and rats and to modify NMDA-induced hyperalgesia in rats. A decrease in the percentage of mice analgesic (tail-flick response) after 5 days of once-daily morphine (7 mg/kg s.c.) was completely blocked by coadministration of d-methadone given s.c. at 10 mg/kg. Morphine given s.c. to mice on an escalating three times per day dosing schedule resulted in a nearly 3-fold increase in the tail-flick ED50 dose of morphine which was prevented by s.c. coadministered d-methadone at 15 mg/kg. In rats, intrathecal (i.t.) morphine produced a 38-fold increase in the ED50, which was completely prevented by the coadministration of i.t. d-methadone at 160 micrograms/rat. A decrease in thermal paw withdrawal latency induced by the i.t. administration of 1.64 micrograms/rat NMDA was completely blocked by pretreatment with 160 micrograms/rat d-methadone. Thus, systemically coadministered d-methadone prevents systemically induced morphine tolerance in mice, i.t. d-methadone attenuates tolerance produced by i.t. morphine in rats, and i.t. d-methadone, at the same dose which modulates morphine tolerance, blocks NMDA-induced hyperalgesia. These results support the conclusion that d-methadone affects the development of morphine tolerance and NMDA-induced hyperalgesia by virtue of its NMDA receptor antagonist activity.
To ascertain whether chronic exposure to nerve growth factor (NGF) alters the responsiveness of sensory neurons to prostaglandin E(2) (PGE(2)), sensory neurons taken from adult rats were grown in culture in the presence or absence of NGF for 7 days. Neurons then were exposed to PGE(2) and release of immunoreactive calcitonin gene-related peptide (iCGRP) and production of immunoreactive cAMP (icAMP) were examined. Growing neurons in the presence of 250 ng/ml NGF increased the content and the release of iCGRP from sensory neurons. Independent of NGF treatment, exposure to 100 nM PGE(2) augmented capsaicin- or potassium-stimulated release of iCGRP by 1. 5-fold compared with cells not exposed to PGE(2). In a similar manner, NGF treatment did not alter the ability of PGE(2) to increase the content of icAMP. These data suggest that prostaglandin-induced sensitization of sensory neurons is not influenced by NGF.
This article has no abstract; the first 100 words appear below.
Chronic neuropathic pain is a serious problem resulting from injury to the central or peripheral nervous system; it affects more than 2 million Americans. Despite advances in our understanding of the pathophysiology and molecular biology of neuropathic pain, its clinical management remains disappointing and controversial. Antidepressants and anticonvulsants have been demonstrated to provide analgesia but are effective in less than half of patients half the time.¹ Opioid treatment of neuropathic pain is often discouraged, because of concern about ineffectiveness, the potential for the development of tolerance, the risk of addiction, and limiting side effects.² In this issue of the Journal, . . .
Source Information
From the Memorial Sloan-Kettering Cancer Center, New York.
The transient outward potassium currents (also known as A-type currents or IA) are important determinants of neuronal excitability. In the brain, IA is modulated by protein kinase C (PKC), protein kinase A (PKA), and extracellular signal-related kinase (ERK), three kinases that have been shown to be critical modulators of nociception. We wanted to determine the effects of these kinases on IA in superficial dorsal horn neurons. Using whole cell recordings from cultured mouse spinal cord superficial dorsal horn neurons, we found that PKC and PKA both inhibit IA in these cells, and that PKC has a tonic inhibitory action on IA. Further, we provide evidence supporting the hypothesis that PKC and PKA do not modulate IA directly, but rather act as upstream activators of ERKs, which modulate IA. These results suggest that ERKs serve as signal integrators in modulation of IA in dorsal horn neurons and that modulation of A-type potassium currents may underlie aspects of central sensitization mediated by PKC, PKA, and ERKs.
The root of Ilex pubescens (Mao-Dong-Qing in Chinese, MDQ) has been commonly used for treatment of cardiovascular and inflammatory diseases in the Chinese medical system. The current studies aimed to investigate the anti-inflammatory and analgesic effects as well as the underlying mechanisms of a purified saponin fraction (PSF) derived from MDQ. PSF was found to significantly suppress the paw edema of rats induced by histamine given intraperitoneally at dosages ranging from 12.5-100 mg/kg. Meanwhile, PSF given orally at dosages of 200 and 100 mg/kg significantly inhibited acetic acid-induced abdominal writhing response of mice and prolonged the time required for mouse tail flick after exposure to a source of radiant heat. The mechanistic studies showed that cyclooxygenase-2 (COX-2) protein expression in carrageenan-injected paw tissues of rats was markedly attenuated by intraperitoneal injection of PSF at dosages of 12.5 to 100 mg/kg. PSF could also markedly inhibit production of proinflammatory cytokines, especially IL-1 beta, IL-6 and TNF-alpha, but enhance production of anti-inflammatory cytokines of IL-4 and IL-10 in the carrageenan-injected paw tissues in rats. These effects resulted in an overall attenuation of the ratio of proinflammatory/anti-inflammatory cytokines and, ultimately suppression of the paw edema. In conclusion, the current study has demonstrated the in vivo anti-inflammatory and analgesic effects of PSF, and suggested that the molecular mechanisms might be associated with inhibition of the elevated expression of COX-2 protein and the overproduction of the proinflammatory cytokines, as well as augmentation of the anti-inflammatory cytokines IL-4 and IL-10 in the carrageenan-injected paw tissues of rats.
- N Dafny
N. Dafny, Chapter 8: Pain Modulation and Mechanisms, (2017) (Accessed 21 August
2017), http://neuroscience.uth.tmc.edu/s2/chapter08.html 2017.
A review on Adansonia digitata Linn
- M Sundarambal
- P Muthusamy
- R Radha
- S A Jerad
M. Sundarambal, P. Muthusamy, R. Radha, S.A. Jerad, A review on Adansonia digitata Linn, J. Pharmacogn. Phytochem. 4 (2015) 12-16.
Preliminary phytochemical evaluation of in vivo and in vitro plant parts of Adansonia digitata L.: an endangered medicinal tree
- S Sugandha
- C Ranjeetha
- R Shasi
- P Varsha
S. Sugandha, C. Ranjeetha, R. Shasi, P. Varsha, Preliminary phytochemical evaluation of in vivo and in vitro plant parts of Adansonia digitata L.: an endangered
medicinal tree, Univ. J. Pharm. 3 (2014) 34-40.
The Characterization and Bioactivity Determination of Adansonia digitata L. Fruit Pulp, for Commercial Product Development Thesis of Bachelor of Science in Nutraceuticals for
- O Brady
O. Brady, The Characterization and Bioactivity Determination of Adansonia digitata
L. Fruit Pulp, for Commercial Product Development Thesis of Bachelor of Science in
Nutraceuticals for Health and Nutrition Dublin vol. 3, (2011), p. 117.
A review on Adansonia digitata Linn
- Sundarambal
Preliminary phytochemical evaluation of in vivo and in vitro plant parts of Adansonia digitata L.: an endangered medicinal tree
- Sugandha