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International Journal of Molecular... Nov 2016The contribution of natural products to the drug-discovery pipeline has been remarkable since they have served as a rich source for drug development and discovery.... (Review)
Review
The contribution of natural products to the drug-discovery pipeline has been remarkable since they have served as a rich source for drug development and discovery. Natural products have adapted, during the course of evolution, optimum chemical scaffolds against a wide variety of diseases, including cancer and diabetes. Advances in high-throughput screening assays, assisted by the continuous development on the instrumentation's capabilities and omics, have resulted in charting a large chemical and biological space of drug-like compounds, originating from natural sources. Herein, we attempt to integrate the information on the chemical composition and the associated biological impact of carob fruit in regards to human health. The beneficial and health-promoting effects of carob along with the clinical trials and the drug formulations derived from carob's natural components are presented in this review.
Topics: Diabetes Mellitus; Diarrhea; Fabaceae; Fruit; Galactans; Humans; Hyperlipidemias; Mannans; Neoplasms; Plant Gums
PubMed: 27834921
DOI: 10.3390/ijms17111875 -
Neurogastroenterology and Motility Aug 2016Faecal incontinence (FI) is common and its pathophysiology and treatments continue to evolve. However, a standard measure(s) for assessing its clinical outcome has been... (Review)
Review
Faecal incontinence (FI) is common and its pathophysiology and treatments continue to evolve. However, a standard measure(s) for assessing its clinical outcome has been elusive. Consequently, over 100 measures and scoring systems, each with intrinsic biases have been reported. These include adequate relief or global satisfaction, ≥50% reduction in episodes or days without FI, quality of life (QOL), FI severity scales and composite indices. Earlier scales relied on the frequency and type of solid, liquid or flatus incontinence and effects on life style whereas newer scales have incorporated urgency, use of pads, antidiarrhoeals and amount of leakage, using prospective daily stool diaries or retrospective weekly or single point assessments. Such a plethora of measures have negatively impacted the assessment and outcome of clinical trials, and have made comparisons difficult. So, how does one sort out the grain from the chaff? In a provocative, post-hoc analysis published in this issue, the minimal clinically important difference, i.e. the smallest change detected by an instrument that is associated with a clinically meaningful change was used to assess FI endpoint. Based on this a ≥50% reduction in FI episodes is recommended as a clinically meaningful outcome measure when assessed by prospective stool diary, and it correlates with symptoms and severity. However, this requires further validation in multi-centre, longer duration and therapeutically effective clinical trial(s). Simultaneous assessment of coping strategies, QOL and psychosocial domains can provide further insights regarding the overall impact of treatments. This mini-review discusses the advances and controversies in defining meaningful FI endpoints.
Topics: Fecal Incontinence; Humans; Outcome Assessment, Health Care; Quality of Life
PubMed: 27440495
DOI: 10.1111/nmo.12905 -
La Clinica Terapeutica 2023The legume tree known as carob (Ceratonia siliqua L.) is indigenous to the Mediterranean area and over the centuries its pods had been traditionally used mostly as... (Meta-Analysis)
Meta-Analysis Review
The legume tree known as carob (Ceratonia siliqua L.) is indigenous to the Mediterranean area and over the centuries its pods had been traditionally used mostly as animal feed. However, it has gained great attention in human nutrition due to the molecular compounds it contains, which could offer many potential health benefits: for example, carob is renowned for its high content of fiber, vitamins, and minerals. Moreover, in traditional medicine it is credited with the ability to control glucose metabolism and gut microbiome. Modern science has also extensively acknowledged the numerous health advantages deriving from its consumption, including its anti-diabetic, anti-inflammatory, and antioxidant properties. Due to its abundant contents of pectin, gums, and polyphenols (such as pinitol), carob has garnered significant attention as a well-researched plant with remarkable therapeutic properties. Notably, carob is extensively used in the production of semi-finished pastry products, particularly in ice cream and other creams (especially as a substitute for cocoa/chocolate): these applications indeed facilitate the exploration of its positive effects on glucose metabolism. Our study aimed at examining the effects of carob extract on intestinal microbiota and glucose metabolism. In this review, we conducted a thorough examination, comprising in vitro, in vivo, and clinical trials to appraise the consequences on human health of polyphenols and pectin from different carob species, including recently discovered ones with high polyphenol contents. Our goal was to learn more about the mechanisms through which carob extract can support a balanced gut flora and improve one's glucose metabolism. These results could influence the creation of novel functional foods and dietary supplements, to help with the management and prevention of chronic illnesses like diabetes and obesity.
Topics: Animals; Humans; Gastrointestinal Microbiome; Polyphenols; Glucose; Fabaceae; Pectins
PubMed: 37994761
DOI: 10.7417/CT.2023.2484 -
Frontiers in Pharmacology 2021(TFG) is used as an antidiarrheal traditional medicine in Western Kenya. This study aimed to investigate the antidiarrheal activity of its aqueous extracts and the...
Aqueous Tuber Extracts of (Kotschy ex Schweinf.) Torre and Hillc. (Fabaceae). Possess Significant Antidiarrheal Activity and Spasmolytic Effect Possibly Mediated by Modulation of Nitrous Oxide System, Voltage-Gated Calcium Channels, and Muscarinic Receptors.
(TFG) is used as an antidiarrheal traditional medicine in Western Kenya. This study aimed to investigate the antidiarrheal activity of its aqueous extracts and the putative mechanism (s) of action using Sprague-Dawley rats and New Zealand white rabbits respectively. The antidiarrheal effects of the extract were evaluated in castor oil-induced diarrhea, the castor oil-induced enteropooling, and phenol red gastric motility tests. On the other hand, isolated rabbit's jejunal segments were used to evaluate the spasmolytic effect of TFG on spontaneous contraction, in acetylcholine-induced contraction, in presence of 80mMK, calcium chloride-induced contraction as well as in presence of the following antagonists: naloxone, methylene blue, L-NAME, prazosin, and propranolol in the studies. The data were express as Mean ± S.E.M and analyzed by one-way ANOVA and Tukey's post hoc test in cases of significance which was set at < 0.05. The extract was phytochemically characterized using Liquid chromatography Mass spectroscopy (LC-MS).The extract possessed significant inhibitory effect in the experiments. The extract exhibited significant spasmolytic effect on both spontaneous contraction and in jejunal segment pre-contracted acetylcholine as well as in presence of 80mMK solution. It also attenuated the spasmogenic effect of various concentration of calcium chloride. The extract's spasmolytic effect was, however, significantly attenuated in presence of several antagonists (methylene blue and L-NAME) but the adrenergic blockers (prazosin and propranolol) had no significant effect in the LC-MS identified thirty compounds where Proathocyanidin (11.54%), Syringic acid (7.30%), and 4-Hydroxybenzoic acid (6.19%) had the highest percentage abundance. In conclusion, the results obtained in this study partially validate the traditional uses of the tubers of this plant species as an antidiarrheal. These antidiarrheal effects are probably mediated via modulation of nitrous oxide pathway, voltage gated calcium channels, and muscarinic receptors.
PubMed: 33796023
DOI: 10.3389/fphar.2021.636879 -
Health Science Reports Oct 2023The study aimed to evaluate the pharmacological properties of methanolic extracts of leaves and barks of (L.) Kurz (family: Lythraceae) focusing on antioxidant,...
Exploring therapeutic potential of (L.) Kurz leaf and bark focusing on antioxidant, antithrombotic, antimicrobial, anti-inflammatory, analgesic, and antidiarrheal properties.
BACKGROUND AND AIMS
The study aimed to evaluate the pharmacological properties of methanolic extracts of leaves and barks of (L.) Kurz (family: Lythraceae) focusing on antioxidant, thrombolytic, anti-inflammatory, antibacterial, analgesic, and antidiarrheal effects.
METHODS
1,1-Diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging assay, clot lysis, disc diffusion, and membrane stabilizing methods were employed to assess in vitro antioxidant, thrombolytic, antibacterial, and anti-inflammatory properties of the leaf and bark methanolic extracts (ME) of and different organic solvents, that is, petroleum ether (PE), dichloromethane (DCM), chloroform (CL), and aqueous (AQ) fractions. In addition, central and peripheral analgesic and antidiarrheal activities of both crude extracts were evaluated at two doses (200 and 400 mg/kg of body weight [bw]).
RESULTS
All the extracts and fractions showed promising antioxidant properties by scavenging DDPH free radicals with IC of 6.11-20.79 μg/mL. AQ fraction (41.24%) of leaves and ME (44.90%) of bark exerted notable in vitro thrombolytic activity. The CL fraction of leaves and AQ fraction of the bark showed 43.16% and 45.37% inhibition of RBC hemolysis, respectively, compared to the inhibition of RBC hemolysis by aspirin in a hypotonic-induced membrane stabilizing assay. Besides, both extracts were observed to provide significant ( < 0.001) central and peripheral analgesic responses at both doses of 200 and 400 mg/kg bw. Furthermore, both doses of bark extract ( < 0.001) and the 400 mg/kg bw of leaf extract ( < 0.05) were observed to possess statistically significant antidiarrheal activity. Additionally, in an acute toxicity investigation, both extracts had a median lethal dose (LD) greater than 5000 mg/kg bw, indicating their safety level.
CONCLUSION
The current study proves the ethnomedicinal uses of ; however, further studies are required for phytochemical screening to isolate the responsible bioactive compounds and discover the lead molecules from the plant species.
PubMed: 37885464
DOI: 10.1002/hsr2.1654 -
ACS Omega Aug 2023is a natural medicinal plant that is widely used for its various pharmacological effects including antiviral, antitumor, anti-inflammatory, and antibacterial...
is a natural medicinal plant that is widely used for its various pharmacological effects including antiviral, antitumor, anti-inflammatory, and antibacterial activities. However, there is no scientific evidence to support its antidiarrheal effect. In this study, the antidiarrheal activity of was evaluated using several validated models. By using HPLC-ESI-MS in conjunction with a network pharmacology approach, the possible antidiarrheal mechanisms of active fragments were studied, and they were subsequently verified in a mouse model of diarrhea. Finally, utilizing molecular docking, active compounds that might have antidiarrheal properties were hypothesized. The results show that the main antidiarrheal part of has 10 chemical components in the -butanol fraction (PSNB). The key targets of PSNB and diarrhea, EGFR, AKT1, and PIK3CA, were screened by network pharmacology analysis. And the mechanism of PSNB in the treatment of diarrhea may be highly related to the EGFR tyrosine kinase inhibitor resistance and PI3K/AKT signaling pathway. Besides, through the qRT-PCR and western-blot experiments, it was found that PSNB could inhibit the gene expression of proinflammatory factors by reducing the protein expression of AKT1 and PI3K and regulating the NF-κB signaling pathway in mice. In addition, asperuloside, paederosidic acid, paederoside, paederosidic acid methyl ester, and 6'-O-E-feruloylmonotropein have better docking energies than other chemical components in PSNB with EGFR, AKT1, and PIK3CA. In conclusion, the main antidiarrheal active site of is the -butanol site. PSNB may exert an antidiarrheal effect by regulating the PI3K/Akt/NF-κB signaling pathway. Among them, asperuloside, paederosidic acid, paederoside, paederosidic acid methyl ester, and 6'-O-E-feruloylmonotropein may be the active ingredients that exert an antidiarrheal effect.
PubMed: 37576641
DOI: 10.1021/acsomega.3c03887 -
BMC Complementary and Alternative... Nov 2017The current study was conducted to evaluate the antioxidant, analgesic, antihyperglycemic, neuropharmacological and antidiarrheal activities of ethanolic extract of...
BACKGROUND
The current study was conducted to evaluate the antioxidant, analgesic, antihyperglycemic, neuropharmacological and antidiarrheal activities of ethanolic extract of Lepisanthes rubiginosa L. leaves in different experimental models.
METHODS
Quantitative and qualitative analysis were done by TLC (thin layer chromatography) and DPPH (1,1-diphenyl-2-picrylhydrazyl) free radical scavenging assay. Analgesic, antihyperglycemic and antidiarrheal activities were evaluated using acetic acid induced writhing in mice, oral glucose tolerance test and castor oil induced diarrhea, respectively. Neuropharmacological activity was investigated in mice using both Open Field and Hole Board methods.
RESULTS
TLC analysis indicated the presence of antioxidant compounds in the extract we used. The extract showed IC value was 31.62 μg/mL whereas the standard ascorbic acid showed 12.02 μg/mL. In acetic acid induced writhing assay, the extract showed 46.07% and 58.43% writhing inhibition at the doses of 250 mg/kg and 500 mg/kg body weight, respectively whereas standard diclofenac-Na (25 mg/kg) showed 86.52% writhing inhibition. The plant extract showed significant (p < 0.05) antihyperglycemic activity on mice as compared to control groups. In neuropharmacological activity assay the experimental animal showed a noticeable decrease in locomotion by showing a decrease in number of square crossed and head dipping at both doses (250 mg/kg & 500 mg/kg). In antidiarrheal activity test, the plant extract at the doses of 250 mg/kg and 500 mg/kg showed percent inhibition of defecation 57.89 and 77.19 respectively, whereas standard loperamide (3 mg/kg) showed percent inhibition of defecation 88.59.
CONCLUSION
The results demonstrated that the extract has potential antioxidant, analgesic, antihyperglycemic, neuropharmacological and antidiarrheal activity.
Topics: Analgesics; Animals; Antidiarrheals; Antioxidants; Behavior, Animal; Blood Glucose; Ethanol; Female; Hypoglycemic Agents; Male; Mice; Plant Extracts; Plant Leaves; Sapindaceae; Tannins
PubMed: 29166935
DOI: 10.1186/s12906-017-2010-y -
Toxicology Reports 2021(dodder) belonging to the family Convolvulaceae has many ethno-medicinal uses such as antidiarrheal and antiemetic. This plant has been employed to treat diarrhea,...
BACKGROUND
(dodder) belonging to the family Convolvulaceae has many ethno-medicinal uses such as antidiarrheal and antiemetic. This plant has been employed to treat diarrhea, where the antidiarrheal use of this plant is well established in different communities around the world without scientific bases. In addition, the antibacterial, anthelmintic, anticholinergic, and antihistaminic effects of this parasitic vine are partly responsible for the folkloric antidiarrheal use of this plant. In the present study, the antidiarrheal activity was evaluated in pigeons () using the juice (JCR), aqueous (CRAE), and methanol (CRME) extracts.
METHODS
The antidiarrheal effect of was evaluated using different reported research models, with few modifications. In pigeons, diarrhea was induced by administration of castor oil (6 mL/kg, PO), ampicillin (250 mg/kg, IP), magnesium sulfate (2 gm/kg, PO), and cisplatin (6 mg/kg, IV). In these experiments, loperamide (2 mg/kg, IM) was used as a positive control, whereas JCR (1 mL/kg (1%) and 1 mL/kg (2%), CRAE (50, 100 and 200 mg/kg) and CRME (50, 100 and 200 mg/kg) were administered intramuscularly at different doses into each pigeon in the test groups.
RESULTS
In addition to cisplatin-induced diarrhea, all paradigms tested gave significant results ( < 0.01). The JCR, at different doses, exhibited a significant ( < 0.01) a dose-dependent antidiarrheal effect on both the frequency and the onset of diarrhea. Similarly, CRAE and CRME, at doses of 100 and 200 mg/kg, showed considerable ( < 0.001) inhibition against the onset and frequency of diarrhea. On the other hand, JCR, CRAE, and CRME exerted significant effects ( < 0.001) on the percentage inhibition (PI) of diarrhea and gastrointestinal charcoal transit in a dose-dependent manner. In this respect, the maximum PI ( < 0.01) of JCR, CRAE, and CRME in different experimental paradigms was 43.13, 49.14, and 55.99 %, respectively.
CONCLUSIONS
Taken all together, results from this study reveal that the juice, aqueous, and methanol extract of exhibit significant anti-motility and anti-secretory potential. These findings may explain the medicinal use of folk medicine as an antidiarrheal medicinal plant.
PubMed: 33717992
DOI: 10.1016/j.toxrep.2021.02.013 -
Evidence-based Complementary and... 2020has been used in traditional medicine as a remedy to alleviate several gastrointestinal disorders that provoke stomachaches, abdominal cramps, and diarrhea. However,...
has been used in traditional medicine as a remedy to alleviate several gastrointestinal disorders that provoke stomachaches, abdominal cramps, and diarrhea. However, there is not enough scientific evidence that supports these effects. Therefore, the purpose of this study was to evaluate antispasmodic and antidiarrheal activities of aqueous extract of (AqExt-TL) as well as its mechanism of action in experimental models. Antispasmodic activity and the mechanism of action of AqExt-TL were assessed on segments of the guinea pig ileum precontracted with KCl, acetylcholine (ACh), or electrical field stimulation (EFS). Furthermore, the antispasmodic effect of two coumarins (umbelliferone and herniarin) previously identified in this species was evaluated. Antidiarrheal activity of AqExt-TL was determined using the charcoal meal test in mice. AqExt-TL showed antispasmodic activity in segments of the guinea pig ileum precontracted with KCl (83.7 ± 1.9%) and ACh (77.2 ± 5.3%) at the maximal concentration; however, practically, it did not alter the contractions induced by EFS (10.1 ± 2.2%). Antispasmodic activity of AqExt-TL was not significantly altered by hexamethonium (a ganglionic blocker) or L-NAME (an inhibitor of nitric oxide synthase). However, this extract decreased the maximal contractile response to calcium (82.7 ± 8.5%), serotonin (68.1 ± 8.5%), and histamine (63.9 ± 5.9%) in their concentration-response curves. Umbelliferone and herniarin also induced an antispasmodic effect on tissues precontracted with KCl. In addition, low doses of AqExt-TL reduced to 50% the distance traveled by charcoal meal in the gastrointestinal transit model in mice as loperamide, an antidiarrheal agent, did. These results provided evidence of the antispasmodic and antidiarrheal activity of , which supports its use in the folk medicine in relieving symptoms in some gastrointestinal disorders. In the antispasmodic effect, the blockade of histaminergic and serotoninergic pathway as well as the calcium channels seems to be involved. Finally, umbelliferone and herniarin could be partially responsible for the antispasmodic activity induced by .
PubMed: 33193797
DOI: 10.1155/2020/7140642 -
Biomedicine & Pharmacotherapy =... Feb 2019Diarrhea is one of the leading causes of infant death in the world accounting for high child mortality rate. It is also present in different pathophysiologies related to...
Diarrhea is one of the leading causes of infant death in the world accounting for high child mortality rate. It is also present in different pathophysiologies related to several etiological agents. The aim of this study is to investigate the antidiarrheal effect of α -Terpineol (α-TPN) in different diarrhea models in rodents. The antidiarrheal effect of α-TPN in the treatment of acute diarrhea and enteropooling induced by castor oil or PGE in Swiss mice pretreated orally with saline (NaCl 0.9%), Loperamide (5 mg/kg) and α-TPN (6.25, 12.5, 25 and 50 mg/kg) was analyzed. Additionally, parameters of severity, total weight of faeces and post-treatment for 4 h were evaluated. Modulation of the opioid and cholinergic pathways was performed and intestinal transit model using activated charcoal as marker was also used. The effect of α-TPN on secretory diarrhea was investigated using the model of fluid secretion in intestinal loops isolated from cholera toxin-treated mice. α-TPN showed antidiarrheal effect (*p < 0.05), reducing the total stool amount (*55%, *48%, *44%, *24%) and diarrheal (*47%, *66%; *56%, 10%) respectively for the doses tested. All doses investigated in the enteropooling test presented significant changes (*46%, *78%, *66%, *41% respectively) in relation to the control. α-TPN through the muscarinic pathway reduced the gastrointestinal transit (*31%), besides inhibiting PGE-induced diarrhea (*39%). α-TPN also reduced fluid formation and loss of Cl ions, by interacting directly with GM1 receptors and cholera toxin, thus increasing the uptake of intestinal fluids. The results suggest an anti-diarrheal activity of α-TPN due to its anticholinergic action, ability to block PGE and GM1 receptors and interaction with cholera toxin in secretory diarrhea, making it a promising candidate drug for the treatment of diarrheal diseases.
Topics: Animals; Antidiarrheals; Castor Oil; Cyclohexane Monoterpenes; Cyclohexenes; Diarrhea; Dose-Response Relationship, Drug; Female; Gastrointestinal Motility; Male; Mice; Monoterpenes
PubMed: 30540974
DOI: 10.1016/j.biopha.2018.11.131