An Outline on Vasicine, its Ethnomedical and Nanoformulation Approach

Adhatoda vasica (also called Vasaka) is a traditional medicinal herb used traditionally for the relief of cough, asthma, nasal congestion, bronchial inflammation, upper respiratory infections, bleeding disorders, skin diseases, leprosy, tuberculosis, diabetes, allergic conditions, rheumatism, tumor, and many more diseases. The present study aims to investigate the biological activities of vasicine, a potent alkaloid from A. vasica with different biological/ pharmacological assays and in silico techniques. Vasicine showed antimicrobial activity as evidenced fromthe colony-forming unit assay. It showed antioxidant activity in ABTS scavenging assay (IC50 = 11.5 μg/ml), ferric reducing power assay (IC50 = 15 μg/ml), DPPH radical scavenging assay (IC50 = 18.2 μg/ml), hydroxyl radical scavenging assay (IC50 = 22 μg/ml), and hydrogen peroxide assay (IC50 = 27.8 μg/ml). It also showed anti-inflammatory activity in proteinase inhibitory assay (IC50 = 76 μg/ml), BSA method (IC50 = 51.7 μg/ml), egg albumin method (IC50 = 53.2 μg/ml), and lipooxygenase inhibition assay (IC50 = 76 μg/ml). Vasicine showed antidiabetic activity in α-amylase inhibition assay (IC50 = 47.6 μg/ml), α-glucosidase inhibition assay (IC50 = 49.68 μg/ml), and non-enzymatic glycosylation of hemoglobin assay. It showed antiviral activity against HIV-protease (IC50 = 38.5 μg/ml). Vasicine also showed anticancer activity against lung cancer cells (IC50 = 46.5 μg/ml) and human fibroblast cells (IC50 = 82.5 μg/ml). In silico studies revealed that similar to the native ligands, vasicine also showed a low binding energy, i.e., good binding affinity for the active binding sites and interacted with α-amylase (-6.7 kcal/mol), α-glucosidase (-7.6 kcal/mol), cyclooxygenase (-7.4 kcal/mol), epidermal growth factor receptor (-6.4 kcal/mol), lipooxygenase (-6.9 kcal/mol), and HIV-protease (-6.4 kcal/mol). The present study ascertains the potential of vasicine as a bioactive compound isolated from A. vasica having therapeutic usefulness in many human diseases.

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“…Vasicine ( Figure 2 ) is also called peganine ( 8 ). The bronchodilatory activity of vasicine is well reported.…”

Section: Introductionmentioning

confidence: 99%

Valorization of Adhatoda vasica leaves: Extraction, in vitro analyses and in silico approaches

et al. 2023

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“…The primary alkaloid of A. vasica (vasicine and vasicinone) are well-known therapeutic respiratory agents. Vasicine has also been known for its diverse biological attributes including anti-inflammatory, anti-cancer, anti-hypertensive, abortifacient, anti-allergic, and anti-tubercular activities ( Singh and Sharma, 2013 ; Ghanta et al, 2020 ; Kumari et al, 2021 ). The well-established chemical and pharmacological potential of A. vasica for the treatment of various ailments prompts us to investigate and identify potent HbF inducers from this ethnomedicinal plant and repurpose its use as HbF inducers for β-thalassemia treatment.…”

Section: Introductionmentioning

confidence: 99%

In Vitro and In Vivo Studies for the Investigation of γ-Globin Gene Induction by Adhatoda vasica: A Pre-Clinical Study of HbF Inducers for β-Thalassemia

Iftikhar¹,

Rahman

Khan³

et al. 2022

Front. Pharmacol.

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Fetal hemoglobin (HbF) is a potent genetic modifier, and the γ-globin gene induction has proven to be a sustainable therapeutic approach for the management of β-thalassemia. In this study, we have evaluated the HbF induction ability of A. vasica in vitro and in vivo, and the identification of potential therapeutic compounds through a bioassay-guided approach. In vitro benzidine-Hb assay demonstrated strong erythroid differentiation of K562 cells by A. vasica extracts. Subsequently, an in vivo study with an aqueous extract of A. vasica (100 mg/kg) showed significant induction of the γ-globin gene and HbF production. While in the acute study, the hematological and biochemical indices were found to be unaltered at the lower dose of A. vasica. Following the bioassay-guided approach, two isolated compounds, vasicinol (1) and vasicine (2) strongly enhanced HbF levels and showed prominent cellular growth kinetics with ample accumulation of total hemoglobin in K562 cultures. High HbF levels were examined by immunofluorescence and flow cytometry analysis, concomitant with the overexpression in the γ-globin gene level. Compound 1 (0.1 µM) and compound 2 (1 µM) resulted in a greater increase in F-cells (90 and 83%) with marked up (8-fold and 5.1-fold) expression of the γ-globin gene, respectively. Molecular docking studies indicated strong binding affinities of (1) and (2) with HDAC2 and KDM1 protein that predict the possible mechanism of compounds in inhibition of these epigenetic regulators in the γ-globin gene reactivation. Altogether, these observations demonstrated the therapeutic usefulness of A. vasica for fostering HbF production in clinical implications for blood disorders.

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“…The herb contains bioactive alkaloids such as vasicinone, vasicine, deoxyvasicine, maiontone, vasicinolone, and vasicinol that produce an anti-inflammatory effect and soothe the irritation in the tissues of the throat (Hossain & Hoq, 2016). Vasicinone is the primary metabolite of vasicine, and it regulates the receptors to inhibit various throat infections and possess bronchodilatation activity (Claeson et al, 2000;Kumari et al, 2021). The leaves, flowers, fruit, and roots are extensively employed in treating cough, whooping cough, cold, and clinging phlegm in the mouth, throat, and chest (Gohel et al, 2021).…”

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Formulation and evaluation of medicated lozenges using traditional herbs to treat sore throat infection

Kadirvel¹,

Mithulesh²,

Narayana³

et al. 2022

Food Processing Preservation

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tween 5 to 16 years are caused by viruses (Worrall, 2011). Recently, the sore, prickly, itchy, and swollen throat has become the most prevalent symptom of COVID-19 infection (WHO, 2020). The treatment of various medical conditions, including sore throat, is done via oral drug delivery as they accurately monitor the dosage, enable self-medication, better patient conformity, and avert pain. However, the solid dosage forms cannot be consumed by the patients having dysphagia, which causes difficulty in swallowing. Lozenges are designed with drugs incorporated for dysphagia patients and require the slow release of drugs in the mouth. The consumption of medicated lozenges is considered the universal remedy for a sore throat. Medicated lozenges are flavored hard candies containing one or more active ingredients intended to be sucked and held in the mouth to reduce the pain and soothe the tissues of the throat

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An Outline on Vasicine, its Ethnomedical and Nanoformulation Approach

Cited by 5 publications

References 44 publications

Valorization of Adhatoda vasica leaves: Extraction, in vitro analyses and in silico approaches

Valorization of Adhatoda vasica leaves: Extraction, in vitro analyses and in silico approaches

In Vitro and In Vivo Studies for the Investigation of γ-Globin Gene Induction by Adhatoda vasica: A Pre-Clinical Study of HbF Inducers for β-Thalassemia

Formulation and evaluation of medicated lozenges using traditional herbs to treat sore throat infection

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