Analgesic and Anti-Inflammatory Potential of Indole Derivatives

Rudrapal, Mithun; Çeli̇k, İsmail; Chinnam, Sampath; Çevik, Ulviye Acar; Tallei, Trina Ekawati; Nizam, Aatika; Joy, Francis; Abdellattif, Magda H.; Walode, Sanjay G.

doi:10.1080/10406638.2022.2139733

Cited by 9 publications

(1 citation statement)

References 49 publications

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“…Ten distinct poses of the ligand molecules were acquired after docking with target proteins (x, y, z = 34.55, 56.37, 23.86) by employing AutoDock Vina's standard settings (34)(35)(36)(37)(38)(39). The Biovia Discovery Studio was chosen to illustrate ligand-protein interactions (40)(41)(42)(43)(44)(45)(46)(47).…”

Section: Molecular Dockingmentioning

confidence: 99%

Utilizing Andrographis paniculata leaves and roots by effective usage of the bioactive andrographolide and its nanodelivery: investigation of antikindling and antioxidant activities through in silico and in vivo studies

Baru Venkata,

Prasanth,

Pasala

et al. 2023

Front. Nutr.

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To valorise the bioactive constituents abundant in leaves and other parts of medicinal plants with the objective to minimize the plant-based wastes, this study was undertaken. The main bioactive constituent of Andrographis paniculata, an Asian medicinal plant, is andrographolide (AG, a diterpenoid), which has shown promising results in the treatment of neurodegenerative illnesses. Continuous electrical activity in the brain is a hallmark of the abnormal neurological conditions such as epilepsy (EY). This can lead to neurological sequelae. In this study, we used GSE28674 as a microarray expression profiling dataset to identify DEGs associated with andrographolide and those with fold changes >1 and p-value <0.05 GEO2R. We obtained eight DEG datasets (two up and six down). There was marked enrichment under various Kyoto Encyclopaedia of Genes and Genomes (KEGG) and Gene Ontology (GO) terms for these DEGs (DUSP10, FN1, AR, PRKCE, CA12, RBP4, GABRG2, and GABRA2). Synaptic vesicles and plasma membranes were the predominant sites of DEG expression. AG acts as an antiepileptic agent by upregulating GABA levels. The low bioavailability of AG is a significant limitation of its application. To control these limitations, andrographolide nanoparticles (AGNPs) were prepared and their neuroprotective effect against pentylenetetrazol (PTZ)-induced kindling epilepsy was investigated using network pharmacology (NP) and docking studies to evaluate the antiepileptic multi-target mechanisms of AG. Andrographolide is associated with eight targets in the treatment of epilepsy. Nicotine addiction, GABAergic synapse, and morphine addiction were mainly related to epilepsy, according to KEGG pathway enrichment analysis (p < 0.05). A docking study showed that andrographolide interacted with the key targets. AG regulates epilepsy and exerts its therapeutic effects by stimulating GABA production. Rats received 80 mg/kg body weight of AG and AGNP, phenytoin and PTZ (30 mg/kg i.p. injection on alternate days), brain MDA, SOD, GSH, GABAand histological changes of hippocampus and cortex were observed. PTZ injected rats showed significantly (***p < 0.001) increased kindling behavior, increased MDA, decreased GSH, SOD, GABA activities, compared with normal rats, while treatment AGNPs significantly reduced kindling score and reversed oxidative damage. Finally, we conclude that the leaves and roots of A. Paniculata can be effectively utilized for its major bioactive constituent, andrographolide as a potent anti-epileptic agent. Furthermore, the findings of novel nanotherapeutic approach claim that nano-andrographolide can be successfully in the management of kindling seizures and neurodegenerative disorders.

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Section: Molecular Dockingmentioning

confidence: 99%

Utilizing Andrographis paniculata leaves and roots by effective usage of the bioactive andrographolide and its nanodelivery: investigation of antikindling and antioxidant activities through in silico and in vivo studies

Baru Venkata,

Prasanth,

Pasala

et al. 2023

Front. Nutr.

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A Novel Cortex Phellodendri Chinensis–Based Carbon Dots Platform for Remarkable Analgesia for Clinical Pain Management

Peng,

Zeng,

et al. 2024

Veterinary Medicine & Sci

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In this study, we explored the eco‐friendly synthesis of photoluminescent CCDs employing a direct one‐step pyrolysis process, utilizing natural Cortex Phellodendri Chinensis as the precursor material and studied their analgesic effect in mice. The synthesized carbon dots underwent comprehensive characterization through a range of spectroscopic and microscopic techniques. These included UV‐Vis, FTIR, fluorescence spectroscopy and HR‐TEM, DLS instruments. HR‐TEM results exhibited the presence of homogenous spherical‐shaped C‐dots of about 3.3 nm without aggregates. Furthermore, the prepared CCDs were studied for their in vivo analgesic effect in mice by performing tail‐immersion, hot plate and acetic acid writhing tests. Also, an MTT assay was performed to assess the in vitro cytotoxicity of CCDs against L929 cells. In vitro cytotoxicity studies revealed that L929 cells exhibited higher cell viability when treated with prepared CCDs. The cellular uptake studies revealed the phase contrast images of MG‐63 cells at wavelength 488 nm clearly depicted the aggregation of green, fluorescent CCDs within the cells while leaving nuclei unobscured. In addition, to the best of our understanding, the results presented in this paper showed that CCDs exhibited an important analgesic effect and enhanced anti‐nociceptive activity, which may be due to stimulation of the opioidergic system. Consequently, CCDs appear to be a viable analgesic alternative for traditional analgesic candidates in pain management.

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Sustainable one-pot synthesis of novel soluble cellulose-based nonionic biopolymers for natural antimicrobial materials

Dang

Wang

et al. 2023

Chemical Engineering Journal

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Analgesic and Anti-Inflammatory Potential of Indole Derivatives

Cited by 9 publications

References 49 publications

Utilizing Andrographis paniculata leaves and roots by effective usage of the bioactive andrographolide and its nanodelivery: investigation of antikindling and antioxidant activities through in silico and in vivo studies

Utilizing Andrographis paniculata leaves and roots by effective usage of the bioactive andrographolide and its nanodelivery: investigation of antikindling and antioxidant activities through in silico and in vivo studies

A Novel Cortex Phellodendri Chinensis–Based Carbon Dots Platform for Remarkable Analgesia for Clinical Pain Management

Sustainable one-pot synthesis of novel soluble cellulose-based nonionic biopolymers for natural antimicrobial materials

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