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Trifolium repens is a well-known herbaceous, perennial herb and has been extensively used in the traditional medicine system over the years. Various parts of the plant are traditionally used as a curative agent against several health ailments such as skin problems, wound healing, stomach disorders, sedative, fever, antiseptic, analgesic, expectorant, psoriasis and eczema. To maximise the plant's potential for usage in the future, the review also aims to update information about its significant pharmacological properties. The ethnomedicinal benefits of T. repens have been well studied; however, the facets of the plant have not been explored yet. The current review outlines several bioactive compounds quantified from T. repens and a few of them namely quercetin, kaempferol, myricetin, acacetin and linamarin, have been reported to have biological activities such as antibacterial, antifungal, antileishmanial, anti-inflammatory, antiaging and anti-hepatotoxic activities. A significant number of in vitro studies have been done on the plant extract, but little is known about the isolation and efficacy of the potent natural bioactive compounds of T. repens . The bioactive compounds in T. repens can be used for advanced drug development against various health disorders.

Ethno-Pharmacological Relevance: Gymnosporia montana (Roth) Benth an herbaceous shrub used in Indian traditional medicine their leaves decoction was used as mouthwash to get relieve from toothache, hence it is also known as Dantakashta in Sanskrit language which means the plant used for tooth problems. Traditionally the leaves juice used to alleviate inflammation and in some parts of India like Saurashtra in Gujarat, leaves were chewed as a folklore cure for Jaundice and in Bhandra region Karnataka, leaves extract mixed with cow milk used for jaundice. Hepatoprotective activity for G. montana leaves was well reported however, its use for inflammation and toothache are still not studied to investigate active phytoconstituents responsible for anti-inflammatory activity., Aim of the Study: The present study aimed at bioactivity guided isolation of G. montana leaves extracts using inhibition of pro-inflammatory mediators such as nitric oxide (NO), tumor necrosis factor (TNF-α), and interleukins (IL-1β and IL-6) in RAW 264.7 cells in vitro assay to yield bioactive phytoconstituents., Materials and Methods: The n-hexane, ethyl acetate and methanol extracts prepared from G. montana leaves were evaluated for cell viability using MTT assay. The effect of extracts to inhibit the pro-inflammatory mediators like NO, TNF-α, IL-1β and IL-6 in RAW 264.7 macrophages was measured by enzyme-linked immunosorbent assay (ELISA). The quantitative analysis of the isolated phytoconstituents was performed using quantitative Nuclear Magnetic Resonance (qNMR)., Results: The n-hexane, ethyl acetate, and methanol extracts of G. montana leaves exhibited cell viability in the range of 97.43-84.88% at 50 μg/mL concentration in RAW 264.7 macrophages. In-vitro evaluation of extracts showed that n-hexane extract was most effective in inhibiting NO, TNF-α, IL-1β and IL-6 inflammatory mediators at 50 μg/mL in lipopolysaccharides (LPS) stimulated RAW 264.7 cells. Further n-hexane extract, its fraction GMHA3 and β-amyrin exhibited significant anti-inflammatory activity at 100, 50 and 30 mg/kg per oral, respectively in carrageenan-induced rat paw edema. The quantitative analysis by qNMR revealed β-amyrin as a major compound in the n-hexane extract., Conclusions: In vitro and in vivo bioassay results suggested that G. montana n-hexane extract, its fraction GMHA3 and β-amyrin exhibits significant anti-inflammatory activity proves the traditional uses of G. montana leaves. The reported activity of β-amyrin for periodontitis provides evidence of profound the use of G. montana leaves for toothache and anti-inflammatory activity., (Copyright © 2022 Elsevier B.V. All rights reserved.)

Background: The fronds of Drynaria quercifolia have traditionally been used in rheumatic pain management. The goal of the present study was to validate the potent anti-inflammatory and anti-rheumatoid properties of the methanolic-extract of its rhizome using in vitro, in vivo and in silico strategies., Methods: The plant was collected and the methanolic extract was prepared from its rhizome. Protein denaturation test, hypotonicity and heat-induced haemolysis assays were performed in vitro. The in vivo anti-rheumatoid potential was assessed in Freund's complete adjuvant (FCA)-induced Wistar rat model through inflammatory paw-edema, haematological, biochemical, radiological and histopathological measurements. Moreover, metabolites of methanolic extract were screened by gas chromatography-mass spectrometry (GC-MS) and 3D molecular structures of active components were utilized for in silico docking study using AutoDock., Results: In vitro results evinced a significant (p < 0.05) anti-inflammatory activity of the rhizome methanolic extract in a dose-linear response. Further, Drynaria quercifolia rhizome methanolic extract (DME) significantly ameliorated rheumatoid arthritis as indicated by the inhibition of arthritic paw-edema (in millimeter) in the rat rheumatoid arthritis models in both the low (57.71 ± 0.99, p < 0.01) and high dose groups (54.45 ± 1.30, p < 0.001) when compared to arthritic control. Treatment with DME also normalized the haematological (RBC, WBC, platelet counts and hemoglobin contents) and biochemical parameters (total protein, albumin, creatinine and ceruloplasmin) significantly (p < 0.05), which were further supported by histopathological and radiological analyses. Furthermore, GC-MS analysis of DME demonstrated the presence of 47 phytochemical compounds. Compounds like Squalene, Gamma Tocopherol, n-Hexadecanoic acid showed potent inhibition of cyclooxygenase-2 (COX-2), tumor necrosis factor (TNF-α), and interleukin (IL-6) in the docking analysis., Conclusion: Results from in vivo and in vitro studies indicated that DME possesses a potent anti-inflammatory and anti-arthritic activity. In silico studies delineated the emergent potent inhibitory effects of several bio-active components on the target inflammatory markers (COX-2, TNF-α and IL-6).

Ethnopharmacological Relevance: Peedantak Vati (PV) is a polyherbal ayurvedic formulation, which is regularly prescribed by the ayurvedic practitioner for the inflammatory disorders and joints pain in India. It is composed of 23 different herbs and minerals, described in ayurvedic text for their anti-inflammatory and analgesic properties., Aim of the Study: To investigate anti-inflammatory and anti-nociceptive potential of 'Peedantak Vati' using in vitro and in vivo methods., Materials and Methods: In-vitro anti-inflammatory activity of PV was studied by estimating nitric oxide (NO) and LPS-induced pro-inflammatory cytokines IL-6 and TNF-α, using murine macrophage RAW264.7 and human monocyte THP-1 cell lines. PV's anti-inflammatory potential was studied in vivo using carrageenan-induced rat paw edema model. Similarly, anti-nociceptive property of PV was evaluated using hot plate, tail flick, formalin and writhing tests on CD-1 mice. Phytochemical profiling of hydro-alcoholic extract of PV was done using HPLC and HPTLC techniques to identify different marker compounds. These identified marker compounds were confirmed using LC-MS/MS analysis., Results: In vitro results strongly suggest that, PV significantly (p < 0.001) inhibited NO release and LPS-stimulated pro-inflammatory cytokines IL-6 and TNF-α, in murine RAW264.7 and human THP-1 cells. Further, PV demonstrated significant (p < 0.05) anti-inflammatory activity at different time points after carrageenan injection with maximum effect at 2 h (40.4 ± 5.2% at 400 mg/kg). Similarly, PV significantly (p < 0.05) decreased nociceptive pain, studied using hot plate, tail flick, formalin and writhing tests. Moreover, HPLC and HPTLC methods were developed for the standardization of PV. Five marker phytocompounds viz. rutin, caffeic acid, colchicine, withaferin A and curcumin were identified and quantified by HPLC and HPTLC methods. The presence of these phytoconstituents was confirmed by LC-MS/MS analysis., Conclusion: The findings of the study strongly suggest that, the polyherbal ayurvedic formulation 'Peedantak Vati' possesses remarkable anti-inflammatory and analgesic property, providing potent alternative for currently available allopathic medicines such as non steroidal anti-inflammatory drugs (NSAIDs)., (Copyright © 2019 Elsevier B.V. All rights reserved.)

Saraca asoca bark has been used in the Ayurvedic system of medicine for female urino-genital disorders. We have recently reported the isolation and characterization of several compounds as markers to develop HPLC profiling of its methanol and aqueous methanol extracts. Now, a HPLC-PDA inactive compound, (+)-pinitol has been isolated and characterized from the bark of this medicinally important tree. Pinitol is a well known bioactive compound for a variety of biological activities, including hypoglycemic and anti-inflammatory activities. A process for the isolation of relatively good concentration of (+)-pinitol from S. asoca bark has been developed and its in vitro anti TNF-α and anti-inflammatory activities against carragenan-induced edema confirmed. While conducting experiments on the possible agonistic activity, it was found that (+)-pinitol showed up to eight fold reduction in the doses of β-lactam antibiotics. The mechanism of its agonistic activity was studied by docking experiments which showed that different conformations of (+)-pinitol and antibiotics were actually in the same binding site with no significant change in the binding energy. These docking simulations, thus predict the possible binding mode of studied compounds and probable reason behind the synergistic effect of (+)-pinitol along with β-lactam antibiotics.

Liquid-liquid partitioning of Ricinus communis root methanol extract resulted in enrichment of compounds. Purification of the n-hexane fraction led to the isolation and characterisation of two triterpenes: one known compound lupeol (1) and a new diketone pentacyclic triterpene named as erandone (urs-6-ene-3,16-dione) (2), from the plant. Their structures were determined by various spectroscopic techniques. Crude methanolic, enriched n-hexane fraction and isolates at doses 100 mg/kg p.o. exhibited significant (P < 0.001) anti-inflammatory activity in carrageenan-induced hind paw oedema model.

Leea macrophylla (Leeaceae) is a wild edible plant with ethomedicinal importance as anti-inflammatory agent. However, no systematic studies on its anti-inflammatory activity and mechanisms have been reported. Present study was undertaken to evaluate anti-inflammatory activity of methanol extract of L. macrophylla leaves. Phytochemical investigation revealed presence of sterols, triterpenoids and ascorbic acid in extract. Methanol extract inhibited lipopolysaccharide stimulated production of inflammatory mediators viz. prostaglandin E2, tumor necrotic factor-α, interleukin-6 and interleukin-1β in vitro in mouse peritoneal macrophages. Additionally, the in vivo anti-inflammatory activity of this extract was evaluated by using carrageenan induced paw edema and cotton pellet granuloma assays in experimental rats. Oral administration of extract (100 and 200 mg/kg) exhibited dose dependant inhibition of carrageenan induced inflammation (p<0.05) and the reduction of the granuloma tissue formation (p<0.05-0.01). The extract (100 and 200 mg/kg, orally) exhibited significant central and peripheral analgesic activity in hot-plate test (p<0.01) and acetic acid induced writhing test (p<0.05-0.01) respectively in experimental mice. Treatment with extract (100 and 200 mg/kg, orally) significantly reduced the yeast provoked elevated body temperature (p<0.05-0.01) in experimental rats. These results confirmed the traditional anti-inflammatory indication of L. macrophylla leaves., (Copyright © 2013 Elsevier Ltd. All rights reserved.)

Immunomodulation is the process of alteration in immune response due to foreign intrusion of molecules inside the body. Along with the available drugs, a large number of herbal drugs are promoted in traditional Indian treatments, for their immunomodulating activity. Natural coumarinolignoids isolated from the seeds of Cleome viscose have been recognized as having hepatoprotective action and have recently been tested preclinically for their immunomodulatory activity affecting both cell-mediated and humoral immune response. To explore the immunomodulatory compound from derivatives of coumarinolignoids, a quantitative structure activity relationship (QSAR) and molecular docking studies were performed. Theoretical results are in accord with the in vivo experimental data studied on Swiss albino mice. Immunostimulatory activity was predicted through QSAR model, developed by forward feed multiple linear regression method with leave-one-out approach. Relationship correlating measure of QSAR model was 99% (R(2) = 0.99) and predictive accuracy was 96% (RCV(2) = 0.96). QSAR studies indicate that dipole moment, steric energy, amide group count, lambda max (UV-visible), and molar refractivity correlates well with biological activity, while decrease in dipole moment, steric energy, and molar refractivity has negative correlation. Docking studies also showed strong binding affinity to immunomodulatory receptors.

In an attempt to locate the biologically active fraction(s) of the plant Verbena officinalis Linn. (Verbenaceae), a preliminary screening of successive petroleum ether, chloroform and methanol extracts of aerial parts for antiinflammatory activity using carrageenan paw oedema model was carried out. All three extracts were found to exhibit antiinflammatory activity with the chloroform extract being the most active. Chemical investigations of petroleum ether and chloroform extracts led to the isolation of beta-sitosterol, ursolic acid, oleanolic acid, 3-epiursolic acid, 3-epioleanolic acid, and minor triterpenoids of derivatives of ursolic acid and oleanolic acids. Chromatographic purification of the methanol extract yielded two iridoid glucosides, verbenalin and hastatoside, a phenylpropanoid glycoside, verbascoside and beta-sitosterol-D-glucoside., (Copyright 2000 John Wiley & Sons, Ltd.)