Preclinical Development of Nononcogenic Drugs (Small and Large Molecules)

Colerangle, John B.

doi:10.1016/b978-0-12-803620-4.00025-6

Cited by 27 publications

(23 citation statements)

References 18 publications

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“…34 In addition, results from acute toxicity test serves as a guide in dosage selection for long term toxicity studies as well as other studies that involve the use of animals. 35 Based on the estimated intraperitoneal LD50, the methanol leaf extract of Ficus asperifolia is considered as slightly toxic in mice. 36 Injection of carrageenan into the hind paws of the negative control rats caused oedema development that peaked at the 4 th hour post injection.…”

Section: Resultsmentioning

confidence: 99%

Preliminary Studies on the Anti-Inflammatory and Analgesic Effects of Methanol Leaf Extract of Ficus asperifolia Miq

Abdullahi¹,

Yaro²,

Nazifi³

2020

TJNPR

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is used in the treatment of diabetes mellitus, hypertension, dysentery, diseases of the kidneys, urinary and respiratory tract infections. 7, 9 Previous studies conducted on Ficus asperifolia showed that it possesses gastroprotective, 10 uterotonic, 11 hypoglycaemic 12 and hypolipidaemic properties. 13 The leaves of the plant have been found to possess antioxidant activities 14 as well as ameliorative effects against testicular problems. 8 Essential oils obtained from Ficus asperifolia were found to possess antimicrobial properties 15 and according to Watcho et al., 16 the fruit extracts possess androgenic-like activities. However, there are relatively scarce reports on the antiinflammatory or analgesic properties of the plant despite its wide usage in ethno-medicine against inflammatory diseases and pain management. This study, therefore, was aimed at evaluating the antiinflammatory and analgesic activities of methanol leaf extract of Ficus asperifolia on mice and rats. Materials and Methods Drugs and chemicals The drugs and chemicals used for the studies include: Morphine sulphate

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Section: Resultsmentioning

confidence: 99%

Preliminary Studies on the Anti-Inflammatory and Analgesic Effects of Methanol Leaf Extract of Ficus asperifolia Miq

Abdullahi¹,

Yaro²,

Nazifi³

2020

TJNPR

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“…Prioritizing compounds with a lower chance of causing toxicity, early in the drug discovery process, would help in the drug development process. 30 With this consideration we conducted acute (single-dose) toxicity study 31 to determine the short-term adverse pathological effects on major mice organs of HU-MCA-13 when administered in mice in a single dose, for a period of 24 h. One group of 5 mice received HU-MCA-13 orally at a dose of 2000 mg/kg, dissolved in a nano-emulsifying drug delivery system 32 in a bolus of 0.4 mL/mouse. After 24 h exposure, the animals were sacrificed, and organs were harvest for pathology analyses.…”

Section: Resultsmentioning

confidence: 99%

Neurotropic activity and safety of methylene-cycloalkylacetate (MCA) derivative 3-(3-allyl-2-methylenecyclohexyl) propanoic acid

Lahiani

Haham-Geula

Lankri

et al. 2020

ACS Chem. Neurosci.

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Polyneuropathy is a disease involving multiple peripheral nerves injuries. Axon regrowth remains the major prerequisite for plasticity, regeneration, circuit formation, and eventually functional recovery and therefore, regulation of neurite outgrowth might be a candidate for treating polyneuropathies. In a recent study, we synthesized and established the methylene-cycloalkylacetate (MCAs) pharmacophore as a lead for the development of a neurotropic drug (inducing neurite/axonal outgrowth) using the PC12 neuronal model. In the present study we extended the characterizations of the in vitro neurotropic effect of the derivative 3-(3-allyl-2-methylenecyclohexyl) propanoic acid (MCA-13) on dorsal root ganglia and spinal cord neuronal cultures and analyzed its safety properties using blood biochemistry and cell counting, acute toxicity evaluation in mice and different in vitro “off-target” pharmacological evaluations. This MCA derivative deserves further preclinical mechanistic pharmacological characterizations including therapeutic efficacy in in vivo animal models of polyneuropathies, toward development of a clinically relevant neurotropic drug.

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“…Acute toxicity studies are conducted to test the shortterm adverse effects of a substance in single or multiple of dose (Gad, 2014). Findings from this studies is important, as it can provide the information for the possible acute toxicity in human, to estimate the safe dose before the efficacy study, to determine the appropriate dosage for multiple-dose toxicity, to estimate the time course for the drug-induced clinical observation and to determine the target organ toxicity produced by the drugs (Colerangle, 2017).…”

Section: Discussionmentioning

confidence: 99%

“…eISSN: 2550-2166 © 2020 The Authors. Published by Rynnye Lyan Resources used in acute toxicity study and the doses that can produce pain, distress and lethality should be avoided (Colerangle, 2017). From the weight, relative organ weight (ROW) and serum biochemistry results, it can be concluded that single-dose administration of PRM at 2000 mg/kg body weight in Wistar rats is safe.…”

Section: Discussionmentioning

confidence: 99%

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Nutritional composition, phytochemicals and acute toxicity of herbal mixture (lemon, apple cider, garlic, ginger and honey) in zebrafish embryo and Wistar rat

Sajak¹,

Azlan²,

Abas³

et al. 2020

Food Res.

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This study was aimed to provide the reference frame for the safe dose design of polyphenol-rich herbal mixture, which consist of lemon, apple cider, garlic, ginger and honey (PRM) for the future efficacy study. Prior to this, the nutritional composition was first conducted and the identification of metabolites that present in PRM was determined using proton nuclear magnetic resonance (1H-NMR) spectroscopy. The acute toxicity of the PRM was then evaluated in zebrafish embryo and Wistar rats following The Organisation for Economic Co-operation and Development (OECD) guidelines. The PRM nutritional composition and sugar profile showed it was high in carbohydrate, ash and protein and the main sugar is fructose. It also contains metabolites such as fructosefuranose, lactic acid, ascorbic acid, acetic acid, cycloalliin, pyruvate, 5- hydroxymethylfurane, α- and β-glucose. From the zebrafish embryo acute toxicity result, the lethal concentration, LC50 of PRM was at 487.50 μg/mL. Meanwhile, in Wistar rats’ model, no lethality was observed in the group treated with PRM at the end of the study (14 days). No changes were also observed from the behavioural and appetite as well as the biochemical parameters (AST, ALT, total cholesterol, triglyceride, LDL, HDL, total protein and creatinine) of the treated group. Therefore, the safe dose for PRM can be up to 2000 mg/kg b.w. in Wistar rats and below 487.50 μg/mL in zebrafish embryo model.

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Preclinical Development of Nononcogenic Drugs (Small and Large Molecules)

Cited by 27 publications

References 18 publications

Preliminary Studies on the Anti-Inflammatory and Analgesic Effects of Methanol Leaf Extract of Ficus asperifolia Miq

Preliminary Studies on the Anti-Inflammatory and Analgesic Effects of Methanol Leaf Extract of Ficus asperifolia Miq

Neurotropic activity and safety of methylene-cycloalkylacetate (MCA) derivative 3-(3-allyl-2-methylenecyclohexyl) propanoic acid

Nutritional composition, phytochemicals and acute toxicity of herbal mixture (lemon, apple cider, garlic, ginger and honey) in zebrafish embryo and Wistar rat

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