In Vivo, Proteomic, and In Silico Investigation of Sapodilla for Therapeutic Potential in Gastrointestinal Disorders

Ansari, Sameen Fatima; Khan, Arif‐ullah; Qazi, Neelum Gul; Shah, Fawad Ali; Naeem, Komal

doi:10.1155/2019/4921086

Cited by 15 publications

(22 citation statements)

References 24 publications

(33 reference statements)

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“…The anti-enteropooling efficacy of T. leucostaphylum (crude and fractionated) extracts was explored to further investigate mechanistic aspects of activity. The presence of castor oil in the intestine stimulates the release of various pro-inflammatory mediators, such as prostaglandins, nitric oxide and histamine, which induce gastrointestinal motility [24]. In our experiments, compared to other fractions, the DTL extract clearly and dose-dependently repressed castor oil induced enteropooling into the small intestine.…”

Section: Discussionmentioning

confidence: 44%

Evaluation of Various Solvent Extracts of Tetrastigma leucostaphylum (Dennst.) Alston Leaves, a Bangladeshi Traditional Medicine Used for the Treatment of Diarrhea

et al. 2020

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Tetrastigma leucostaphylum (TL) is an important ethnic medicine of Bangladesh used to treat diarrhea and dysentery. Hence, current study has been designed to characterize the antidiarrheal (in vivo) and cytotoxic (in vitro) effects of T. leucostaphylum. A crude extract was prepared with methanol (MTL) and further partitioned into n-hexane (NTL), dichloromethane (DTL), and n-butanol (BTL) fractions. Antidiarrheal activity was investigated using castor oil induced diarrhea, enteropooling, and gastrointestinal transit models, while cytotoxicity was evaluated using the brine shrimp lethality bioassay. In antidiarrheal experiments, all doses (100, 200, and 400 mg/kg) of the DTL extract significantly reduced diarrheal stool frequency, volume and weight of intestinal contents, and gastrointestinal motility in mice. Similarly, in the cytotoxicity assay, all extracts exhibited activity, with the DTL extract the most potent (LC50 67.23 μg/mL). GC-MS analysis of the DTL extract identified 10 compounds, which showed good binding affinity toward M3 muscarinic acetylcholine, 5-HT3, Gut inhibitory phosphodiesterase, DNA polymerase III subunit alpha, and UDP-N-acetylglucosamine-1 carboxyvinyltransferase enzyme targets upon molecular docking analysis. Although ADME/T analyses predicted the drug-likeness and likely safety upon consumption of these bioactive compounds, significant toxicity concerns are evident due to the presence of the known phytotoxin, 2,4-di-tert-butylphenol. In summary, T. leucostaphylum showed promising activity, helping to rationalize the ethnomedicinal use and importance of this plant, its safety profile following both acute and chronic exposure warrants further investigation.

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Section: Discussionmentioning

confidence: 44%

Evaluation of Various Solvent Extracts of Tetrastigma leucostaphylum (Dennst.) Alston Leaves, a Bangladeshi Traditional Medicine Used for the Treatment of Diarrhea

et al. 2020

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“…Hematoxylin and eosin staining was performed according to our previous protocols ( Ali et al, 2019 ; Ansari et al, 2019 ; Ullah et al, 2020 ). Briefly, the non-coated slides initially underwent a deparaffinization step with xylene, followed by hydration (graded ethanolic series), and finally with water.…”

Section: Methodsmentioning

confidence: 99%

Carveol a Naturally-Derived Potent and Emerging Nrf2 Activator Protects Against Acetaminophen-Induced Hepatotoxicity

et al. 2021

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Acetaminophen (N-acetyl p-aminophenol or APAP) is used worldwide for its antipyretic and anti-inflammatory potential. However, APAP overdose sometimes causes severe liver damage. In this study, we elucidated the protective effects of carveol in liver injury, using molecular and in silico approaches. Male BALB/c mice were divided into two experimental cohorts, to identify the best dose and to further assess the role of carveol in the nuclear factor E2-related factor; nuclear factor erythroid 2; p45-related factor 2 (Nrf2) pathway. The results demonstrated that carveol significantly modulated the detrimental effects of APAP by boosting endogenous antioxidant mechanisms, such as nuclear translocation of Nrf2 gene, a master regulator of the downstream antioxidant machinery. Furthermore, an inhibitor of Nrf2, called all-trans retinoic acid (ATRA), was used, which exaggerated APAP toxicity, in addition to abrogating the protective effects of carveol; this effect was accompanied by overexpression of inflammatory mediators and liver = 2ltoxicity biomarkers. To further support our notion, we performed virtual docking of carveol with Nrf2-keap1 target, and the resultant drug-protein interactions validated the in vivo findings. Together, our findings suggest that carveol could activate the endogenous master antioxidant Nrf2, which further regulates the expression of downstream antioxidants, eventually ameliorating the APAP-induced inflammation and oxidative stress.

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“…Filtration of the whole extract was carried out by employing standard protocols via filter paper (Whatman No.1) followed by evaporation through a rotary evaporator, Tokyo Rikakikai Type A 1000S, at a lowered pressure and a temperature up to 50°C for generating dry extract in a yield of 20 g. After complete elimination of chloroform, sequential extraction of the leftover residue was carried out by suspending in a mixture of methanol and water (4 L, 20 : 80) via the above-mentioned technique. A 90 g yield of the extract was obtained by evaporating the solvent under a reduced pressure [ 9 ].…”

Section: Methodsmentioning

confidence: 99%

“…Charcoal meal transit time was determined by the method described previously [ 9 ]. Rats were fasted for about 24 hours with free availability to water.…”

Section: Methodsmentioning

confidence: 99%

“…The current research aims to evaluate the possible effect of Ficus palmata in gastrointestinal activities including antidiarrheal, antimotility, enteropooling, antispasmodic, and antiulcer. Furthermore, in order to explore the underlying molecular mechanisms, molecular techniques including ELISA and IHC were employed to analyze the levels of inflammatory markers [ 9 ].…”

Section: Introductionmentioning

confidence: 99%

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Proteomic Analysis and In Vivo Studies Reveal the Potential Gastroprotective Effects of CHCl3 and Aqueous Extracts of Ficus palmata

Ansari

Khan

Qazi

et al. 2021

Evidence-Based Complementary and Alternative Medicine

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Ficus palmata is rich in several phytochemicals such as chromone, isoflavones, terpenes, lignans, coumarins, glycosides, and furanocoumarins and have been traditionally used for the management of different gastrointestinal disorders. This research reveals the effects of Ficus palmata fruit extracts—Ficus palmata chloroform (Fp.CHCl3) and Ficus palmata aqueous (Fp.Aq)—on gut activity through in vivo and in vitro analyses. Antidiarrheal and enteropooling assays were analyzed with castor oil-induced diarrhea and intestinal fluid accumulation. Jejunum tissues of rabbits were isolated (antispasmodic) for in vitro experiments. Antimotility was carried out by charcoal meal for determining transient time, and ethanol-induced ulcer assay was used to measure the ulceration of stomach; molecular pathways were assessed through proteomic approach. Fp.CHCl3 and Fp.Aq extracts attributed dose-dependently protection against diarrhea, and intestinal fluid secretions were inhibited dose dependently. Extracts of Fp.CHCl3 and Fp.Aq produced reduction in spontaneous and K+ (at 80 Mm)-induced contractions in isolated jejunum tissues, along with the decreased length covered by charcoal in charcoal meal transient time activity. The extract exhibited gastroprotective outcome in rats and reduced tumor necrotic factor (TNF-α) levels and IL-18, measured by proteomic approach. Morphological studies’ results showed that ethanol induced significant gastritis, apoptosis, swelling of mucosa, and hydropic degeneration leading to cellular degeneration and necrosis, observed through staining techniques. Furthermore, ethanol activated the inflammation pathway in all gastric zones by elevating the levels of cyclooxygenase-2, TNF-α, and nuclear factor kappa light-chain enhancer of activated B-cells. Overall results expressed the antidiarrheal, antispasmodic, enteropooling, antimotility, and antiulcer activities of Ficus palmata fruit extract.

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In Vivo, Proteomic, and In Silico Investigation of Sapodilla for Therapeutic Potential in Gastrointestinal Disorders

Cited by 15 publications

References 24 publications

Evaluation of Various Solvent Extracts of Tetrastigma leucostaphylum (Dennst.) Alston Leaves, a Bangladeshi Traditional Medicine Used for the Treatment of Diarrhea

Evaluation of Various Solvent Extracts of Tetrastigma leucostaphylum (Dennst.) Alston Leaves, a Bangladeshi Traditional Medicine Used for the Treatment of Diarrhea

Carveol a Naturally-Derived Potent and Emerging Nrf2 Activator Protects Against Acetaminophen-Induced Hepatotoxicity

Proteomic Analysis and In Vivo Studies Reveal the Potential Gastroprotective Effects of CHCl3 and Aqueous Extracts of Ficus palmata

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