Vol 23, No 1 (2024)
- Year: 2024
- Articles: 6
- URL: https://archivog.com/1871-5230/issue/view/10040
Medicine
Exploration of Antileishmanial Compounds Derived from Natural Sources
Abstract
Aims::Leishmaniasis is a deadly tropical disease that is neglected in many countries. World Health Organization, along with a few other countries, has been working together to protect against these parasites. Many novel drugs from the past few years have been discovered and subjected against leishmaniasis, which have been effective but they are quite expensive for lower-class people. Some drugs showed no effect on the patients, and the longer use of these medicines has made resistance against these deadly parasites. Researchers have been working for better medication by using natural products from medicinal plants (oils, secondary metabo-lites, plant extracts) and other alternatives to find active compounds as an alternative to the current synthetic drugs.
Materials and Methods:To find more potential natural products to treat Leishmania spp, a study has been conducted and reported many plant metabolites and other natural alternatives from plants and their extracts. Selected research papers with few term words such as natural products, plant metabolites, Leishmaniasis, in vivo, in vitro, and treatment against leishmania-sis; in the Google Scholar, PubMed, and Science Direct databases with selected research papers published between 2015 and 2021 have been chosen for further analysis has been included in this report which has examined either in vivo or in vitro analysis.
Results:This paper reported more than 20 novel natural compounds in 20 research papers that have been identified which report a leishmanicidal activity and shows an action against pro-mastigote, axenic, and intracellular amastigote forms.
Conclusion:Medicinal plants, along with a few plant parts and extracts, have been reported as a possible novel anti-leishmanial medication. These medicinal plants are considered nontoxic to Host cells. Leishmaniasis treatments will draw on the isolated compounds as a source further and these compounds compete with those already offered in clinics.
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In-vitro and In Silico Assessment of Anti-inflammation Properties of Saponarin Extracted from Hordeum Vulgare
Abstract
Background:Hordeum vulgare, commonly known as Barley grass, is a historically significant cultivated plant with profound implications for societies, agricultural sciences, and human nutrition. It has been valued for both sustenance and its potential medicinal properties
Objective:This study aims to comprehensively investigate the medicinal properties of Hordeum vulgare, focusing on its potential therapeutic benefits and anti-inflammatory properties. Addition-ally, we seek to quantify and compare the phytochemical content of two distinct extracts: Barley Grass Hexane Extract (BGHE) and Barley grass aqueous extract (BGAQ).
Methods:We quantified the phytochemical contents of BGHE and BGAQ and evaluated their anti-inflammatory effects using UV spectroscopy at 560 nm, coupled with the RBC membrane stabilization technique. Subsequently, we conducted in silico studies to assess the in vitro anti-inflammatory potential of Barley grass leaf extracts.
Results:Both BGHE and BGAQ demonstrated significant inhibitory effects on inflammation com-pared to the control group. However, BGHE exhibited superior anti-inflammatory efficacy when compared to BGAQ, suggesting its role as a potential anti-inflammatory agent. In silico studies further supported the anti-inflammatory potential of Barley grass leaf extracts.
Conclusion:Hordeum vulgare, or Barley grass, offers a wealth of health benefits, including anti-inflammatory, anti-diabetic, anti-cancer, antioxidant, anti-acne, and anti-depressant properties. These properties contribute to improved immunity, reduced cardiovascular disorders, and alleviation of fatigue. The distinct extracts, BGHE and BGAQ, both exhibit promising anti-inflammatory capabilities, but BGHE shows better anti-inflammatory activity. This research sheds light on the therapeutic potential of Barley grass, making it a valuable candidate for further exploration in the field of natural medicine.
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Cinnamic Acid Ameliorates Acetic Acid-induced Inflammatory Response through Inhibition of TLR-4 in Colitis Rat Model
Abstract
Background:Cinnamic acid, an active compound in cinnamon spp., has anti-inflammatory and antioxidant characteristics and is favorable in managing inflammatory bowel diseases.
background:Background: Cinnamic acid is a chemical with anti-inflammatory and antioxidant characteristics, thus might help to manage inflammatory bowel disease.
Objective:Evaluate cinnamic acid's effects on colitis in rats.
Methods:To induce colitis in experimental rats, excluding the sham group, a 4% intrarectal solu-tion of acetic acid was administered. The rats were then given oral doses of cinnamic acid at 30, 45, and 90 mg/kg for two days. The animals were assessed for macroscopic and microscopic changes, and the levels of inflammatory mediators such as tumor necrosis factor-alpha (TNF-α), interleukin-6 (IL-6), and myeloperoxidase (MPO) were measured using Eliza kits. Additionally, real-time PCR was performed to examine the gene level of toll-like receptor 4 (TLR-4) in the colon.
Results:Effective reduction of inflammation in acetic acid-induced colitis was achieved through Cinnamic acid administration at doses of 45 and 90 mg/kg. The decrease was achieved by inhibiting the activities of TNF-α, IL-6, and MPO while downregulating the expression of TLR-4. It is important to note that macroscopic and microscopic evaluations were significant in determining the effectiveness of cinnamic acid in reducing inflammation.
Conclusion:Downregulation of inflammatory cytokines and TLR-4 expression may contribute to cinnamic acid's anti-inflammatory effect.
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Standardization and Pharmacological Evaluation of Ziziphus mauritiana Extract for Sedative and Anticonvulsant Activity in Mice and Rat
Abstract
Introduction:Ziziphus mauritiana, sometimes called Indian jujube or Ber, belongs to the Rhamnaceae group of plants. The aqueous and ethanolic Ziziphus mauritiana formulations were shown to have analgesic, antipyretic, potent analgesic, anti-inflammatory, and anti-emetic properties.
Aim & Objectives:The aim of this study is to investigate the sedative and anticonvulsant activities of Ziziphus mauritiana extract by governing 200 and 400 mg/kg body weight orally
Material and Methods:The leaves are extracted with ethanol and lukewarm water with a soxhlet apparatus for 72 hours. After that acute extract toxicity study was performed and then locomotor activity, pentobarbital induced sleeping time and anticonvulsant activity were per-formed with the extract.
Results:Oral administration of extract at dosages of 200 & 400 mg/kg was employed after an immediate toxicity test. At a dosage of 400 mg/kg, the number of locomotions was reduced significantly lengthened the period of time spent sleeping and there was showed a dosage-de-pendent reduction in all phases of an epileptic episode.
Conclusion:In this study, the extract reduced locomotor activity, however, it had a superior profile for an antiepileptic action than phenytoin since it decreased locomotor activity to a lesser level. The considerable increase in pentobarbitone sleep hours with the extracts at a higher dose supported the sedative action of Z. mauritiana.
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Pyrazoles as Anti-inflammatory and Analgesic Agents: In-vivo and In-silico Studies
Abstract
Background::Pyrazole is a well-known nucleus in the pharmacy field with a wide range of other activities in addition to anti-inflammatory and analgesic, i.e., anticonvulsant, antiviral, and anticancer activities. There are well-known marketed drugs having pyrazole moi-ety as celecoxib, and lonazolac as COX-II inhibitors.
Aims::We aim to synthesize better anti-inflammatory than existing ones. Thiophene is also known for its analgesic and anti-inflammatory action. Thus, the fusion of both gives better anti-inflammatory agents. In the present studies, derivatives from two series of pyrazole were prepared by reacting substituted chalcone (3a-3f) derivatives prepared from 2-acetyl thiophene. They substituted aromatic aldehydes with phenyl hydrazine to form (5a-5f) and with 2, 4-dinitro phenyl hydrazine giving compounds (6a-6f) separately.
Methods::Purified and characterized pyrazoles have been analyzed for in-vivo analgesic and anti-inflammatory activities by using standard methods. Compounds 5e, 5f, and 6d were proved to be potent analgesics and series (5a-5f) was found to have anti-inflammatory action, which was further validated using docking and ADME studies.
Results::The ADME profile of synthesized compounds was found to be satisfactory.
Conclusion::The synthesized compounds can serve as lead for further drug designing.
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Analysis of Tolfenamic Acid using a Simple, Rapid, and Stability-indicating Validated HPLC Method
Abstract
Background:Tolfenamic acid (TA) belongs to the fenamates class of non-steroidal anti-inflammatory drugs. Insufficient information is available regarding the availability of a reliable and validated stability-indicating method for the assay of TA.
Objective:A relatively simple, rapid, accurate, precise, economical, robust, and stability-indicating RP-HPLC method has been developed to determine TA in pure and tablet dosage forms.
Methods:The method was validated according to the ICH guideline, and parameters like linearity, range, selectivity, accuracy, precision, robustness, specificity, and solution stability were determined. TLC and FTIR spectrometry were used to ascertain the purity of TA. The specificity was determined with known impurities and after performing forced degradation, while the robustness was established by Plackett-Burman's experimental design. The mobile phase used for the analysis was acetonitrile and water (90:10, v/v) at pH 2.5. The detection of the active drug was made at 280 nm using a C18 column (tR = 4.3 min.). The method's ap-plicability was also checked for the yellow polymorphic form of TA.
Results:The results indicated that the method is highly accurate (99.39-100.80%), precise (<1.5% RSD), robust (<2% RSD), and statistically comparable to the British Pharmacopoeia method with better sensitivity and specificity.
Conclusion:It was observed that the stress degradation studies do not affect the method's accuracy and specificity. Hence the proposed method can be used to assay TA and its tablet dosage form.
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