The present study was designed to evaluate the anti-hyperalgesic effect of kaempferol-3,7-di-O-α-L-rhamnopyranoside isolated from the ethyl acetate soluble part of Dryopteris cycadina. Pretreatment ...of the compound at the doses of 2.5, 5, and 10 mg/kg caused a significant reduction in abdominal constrictions in acetic acid-induced writhing test with maximum effect of 63.03% (P < 0.001) at 10 mg/kg i.p. When subjected in formalin test, it evoked a marked antinociceptive effect in both phases in a dose-dependent manner. The maximum (p < 0.01) pain-inhibiting effects were 61.36% and 65.89% in 1st and 2nd phases at 10 mg/kg i.p., respectively. Administration of atropine (non-selective cholinergic receptor antagonist) significantly (p < 0.05) antagonized the antihyperalgesic effect of the compound, while glibenclamide and naloxone did not alter the induced antinociceptive effect and thus, antinociceptive activity of the compound is mediated, at least in part, through cholinergic system antagonism; independent of calcium channel and opioidergic receptor participation. Furthermore, docking studies underlined strong COX-2 inhibitory activity of the compound.
Our data concluded that overall analgesic activity of the compound seems to involve COX-2 inhibition and activation of cholinergic receptors. However, further detailed studies are required in this direction to confirm the analgesic effect of the compound for its possible clinical utility.
Curcumin (1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione) is a is an important consituitents present in Curcuma longa L. (turmeric) rhizome. It is also a lipophilic molecule that rapidly ...permeates cell membrane. Curcumin has been used as pharmacological traditional medicinal agent in Ayurvedic medicine for ∼6000 years. Being chemopreventive agent, curcumin has been found to modulate multiple molecular pathways through several mechanisms, e.g. induction of apoptosis, inhibition survival signals, and prevention from reactive oxidative species (ROS). Curcumin significantly caused reduction in lung cancer stem cells markers (CD133, ALDHA1, CD44, Nanog, and Oct4) and the number of CD133-positive cells as well as efficiently decreased the tumorsphere formation, inhibited proliferation, and induced apoptotic cell death. It also suppressed the activation of both Wnt/β-catenin and Sonic Hedgehog pathways. Curcumin has been also reported to diminish renal hypertrophy, reduce mesangial matrix expansion, and cause a lower level of albuminuria. It also inhibited the upregulated protein and mRNA expressions of collagen IV and fibronectin in the renal cortices as well as significantly reduced the mature interleukin-1β, cleaved caspase-1, and NLRP3 protein levels in the renal cortices of db/db mice as well as in HK-2 cells. It also ameliorated the defective insulin signalling pathway by upregulating insulin-like growth factor (IGF)-1R, IRS-2, PI3K, p-PI3K, Akt and p-Akt protein expression while downregulating IR and IRS-1. Besides, curcumin lowered the heart MDA and DNA fragmentation levels, increased concentration of SOD, catalase, and gluathione levels, decreased the percentage of TUNEL-positive cells and γH2AX protein expression, while it lowered the percentage (%) of capspase 3 positive cells and improved the percentage of Bcl-2 positive cells. The current review article presents effective role of curcumin against cancer, diabetes, oxidative stress, cardiovascular, obesity, and aging.
•Curcumin (1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione) is a is an significant constituents present in Curcuma longa L. (turmeric) rhizome.•Curcumin has been used as pharmacological traditional medicinal agent in Ayurvedic medicine.•Curcumin curcumin has been found to modulate multiple molecular pathways through several mechanisms, e.g. induction of apoptosis and oxidative species (ROS) etc.•Curcumin curcumin has been found active against cancer, diabetes, oxidative stress, cardiovascular, obesity, and aging.
Synthesis of nanoparticles is a fast-growing area of interest in the current development in science and technology. Nanoparticles are also used in biomedical applications. Green synthesis of ...nanoparticles is an environmental friendly and cost-effective technique.
Wall. Ex. Royle crude extract was used for the eco-friendly genesis of silver nanoparticles (AgNPs). Aromatic amines were the functional groups involved in the bio-fabrication and synthesis of the AgNPs. The production of AgNPs was established by the appearance of brown color. The manufactured AgNPs were characterized by UV-Vis spectrophotometer, X-ray diffractometer, and FTIR spectrophotometer. AgNPs were face-centered cubic in nature with an average size of 9.99 nm. The produced AgNPs (18 µL disc
) showed substantial antibacterial (53.74, 52.75, 51.61, 43.00, 36.84, and 36.84%) and antifungal (54.05, 42.11, 41.10, 40.85, 30.55, and 29.73%) potential against the tested bacterial (
,
,
,
,
, and
) and fungal (
,
,
,
,
, and
) strains, respectively.
•Naphthoquinones (1-9) were isolated from chloroform soluble fraction of Diospyros lotus.•Compound (1-9) was studied for in vitro antiglycation potential; among tested compound; compound 4 and 5 was ...found most active.•It is concluded that naphthoquinones (1-8) exhibited good antiglycation and lipoxygenase inhibitory potential.
Medicinal plants are a key source of important natural products, which are used for discovery of new drugs. The aim of this work was to explore the natural compounds having in vitro antiglycation and lipoxygenase inhibition potential. Consequently, compounds such as di-naphthodiospyrols A (1), di-naphthodiospyrols B (2), di-naphthodiospyrols C (3), di-naphthodiospyrols D (4), di-naphthodiospyrols E (5), di-naphthodiospyrols F (6), di-naphthodiospyrols g (7), 8-hydroxyisodiospyrin (8), and diospyrin (9) were isolated for the first time from Diospyros lotus Linn. In vitro antiglycation and lipoxygenase inhibitory activity results indicated that compound 4 exhibits the highest antiglycation activity with inhibition IC50 = 287.45 ± 1.60 μM), followed by compound 5 with an IC50 value of 248.72 ± 2.09 μM respectively. Similarly, compounds 7 and 8 showed moderate activity with IC50 values of 234.87 ± 2.00 , and 228.98 ± 1.98 μM, respectively, when compared with rutin (IC50 = 295.22 ± 1.55 μM). . The isolated compounds (1‒9) were also subjected to lipoxygenase inhibitory activity. Results revealed that secondary metabolites (1‒7) exhibit an excellent inhibitory effect against lipoxygenase, with IC50 values of 90.35 ± 0.96, 87.09 ± 1.00, 84.01 ± 1.01, 40.49 ± 0.49, 44.70 ± 0.49, 79.04 ± 0.86, and 62.09 ± 0.18 μM, for compounds 1, 2, 3, 4, 5, 6, and 7, respectively. The standard drugs Baicalein and Tenidap sodium exhibited inhibitory effect with IC50 values of 40.98 ± 0.08 μM and 23.00 ± 0.05 µM, respectively. Within this context, compounds with high inhibition potential against lioxygenase can be regarded as lead compounds in drug discovery. Furthermore, these compounds can be further studied as antiglycating agents to increase the chemical space for new chemical entities having drug-like properties.
Analgesic, anti-inflammatory, and sedative drugs are available with potential side effects such as peptic ulcer and addiction among other things. In this regard, research is underway to find safe, ...effective, and economical drugs free of these side effects. In this study, an isolated natural product from Diospyros lotus, was tested for the aforementioned bioactivities.
To evaluate analgesic, anti-inflammatory, and sedative potential of D. lotus extracts in animal paradigms using BALB/c mice as experimental model.
Analgesic, anti-inflammatory and sedative activities of dinaphthodiospyrol G (1) isolated from the chloroform fraction of D. lotus were evaluated using different experimental procedures. Anti-inflammatory effect was evaluated using the carrageenan and histamine-induced paw edema, whereas the antinociceptive effect was quantified by means of the hot plate analgesiometer. On the other hand, the sedative effect was determined using animal assay for screening the locomotors effects of compound 1. Compound 1 was also subjected to molecular modeling studies against cyclooxygenase enzymes.
Results from this investigation showed that the extract is devoid of anti-inflammatory and antinociceptive potentials but has a significant sedative effect, whereas the tested compound exhibited 55.23 and 78.34% attenuation in paw edema by carrageenan and histamine assays, respectively. A significant (p < 0.001) and dose-dependent antinociceptive and sedative effects were demonstrated by the isolated compound. Molecular docking and dynamics simulation studies of the isolated compound against cyclooxygenase enzyme indicated that compound 1 forms specific interactions with key residues in the active site of the target receptor, which validates the potential use of the isolated compound as cyclooxygenase inhibitor.
Compound 1 exhibited remarkable analgesic, anti-inflammatory, and sedative activities. These findings strongly justify the traditional use of D. lotus in the treatment of inflammation, pain, and insomnia.
Pistacia integerrima leaf galls are used in several traditional medicines to cure many diseases such as diarrhea, asthma, fever, cough, vomiting, and hepatitis. The main goal of the present ...investigation was to assess the antidiarrheal effect of the Pistacia integerrima extracts/fractions and four isolated flavonoid compounds (1–4) on mice. An in vivo assay involving castor-oil-induced diarrhea was used to evaluate the antidiarrheal potential of extracts/fractions at 100, 200, and 400 mg/kg p.o., as well as isolated compounds at 5, 10, and 20 mg/kg p.o. Pretreatment of mice with extracts/fractions significantly attenuated castor-oil-induced diarrhea in a dose-dependent manner. Among all crude extracts and fractions, the ethyl acetate extract was the most effective with 100% protection against diarrhea followed by chloroform (75% protection) at 400 mg/kg p.o. Although all the isolated compounds exhibited strong antidiarrheal activity, isolated compounds 1 and 4 demonstrated 100% protection against diarrhea. Moreover, docking models were performed using the Molecular Operating Environment (MOE) and AutoDock software and suggested that the extracts and isolated compounds exert antidiarrheal activity by inhibiting mu-opioid and delta-opioid receptors. Therefore, our finding affords a strong pharmacological basis for the traditional use of P. integerrima galls in the treatment of diarrhea.
The present study explores the potential of
shoot extract for Ag-metal bio-reduction and its antimicrobial activity. Among the different ratios of AgNO
and extract tested, 1:5 (1 mL AgNO
and 5 mL ...extract) gave maximum SPR peak at 411.0 nm during UV-Vis spectrophotometric analysis, indicating the synthesis of maximum amount of AgNPs in solution. XRD analysis reported the crystalline nature of AgNPs with 13.32 nm nanocrystallite size. FTIR studies suggested the involvement of carboxylic acid (–C–O–O–H) and methane (–CH–) functional groups of different compounds in AgNPs reduction and fabrication. Average size of synthesized uniform shaped nanospheres was 32 nm by SEM image analysis. The produced AgNPs (1.5 mg/disc) showed growth inhibition of 71.46, 65.97, 61.5, 55.32, and 54.83% against
,
,
,
, and
. While the least growth inhibition of 48.55% was recorded for
, suggesting it as the least-susceptible microbe among all the tested microbial species.
a was found to be most sensitive of all tested microbes, while
,
, and
reported moderate susceptibility to AgNPs.
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•The antidiarrheal activity of C. reflexa was evaluated in pigeons using the juice, aqueous, and methanol extracts.•The antidiarrheal effect of C. reflexa was evaluated using ...different reported research models.•The juice, aqueous, and methanol extract of C. reflexa exhibit significant anti-motility and anti-secretory potential.
Cuscuta reflexa (dodder) belonging to the family Convolvulaceae has many ethno-medicinal uses such as antidiarrheal and antiemetic. This plant has been employed to treat diarrhea, where the antidiarrheal use of this plant is well established in different communities around the world without scientific bases. In addition, the antibacterial, anthelmintic, anticholinergic, and antihistaminic effects of this parasitic vine are partly responsible for the folkloric antidiarrheal use of this plant. In the present study, the antidiarrheal activity of C. reflexa was evaluated in pigeons (Columba livia) using the juice (JCR), aqueous (CRAE), and methanol (CRME) extracts.
The antidiarrheal effect of C. reflexa was evaluated using different reported research models, with few modifications. In pigeons, diarrhea was induced by administration of castor oil (6 mL/kg, PO), ampicillin (250 mg/kg, IP), magnesium sulfate (2 gm/kg, PO), and cisplatin (6 mg/kg, IV). In these experiments, loperamide (2 mg/kg, IM) was used as a positive control, whereas JCR (1 mL/kg (1%) and 1 mL/kg (2%), CRAE (50, 100 and 200 mg/kg) and CRME (50, 100 and 200 mg/kg) were administered intramuscularly at different doses into each pigeon in the test groups.
In addition to cisplatin-induced diarrhea, all paradigms tested gave significant results (P < 0.01). The JCR, at different doses, exhibited a significant (p < 0.01) a dose-dependent antidiarrheal effect on both the frequency and the onset of diarrhea. Similarly, CRAE and CRME, at doses of 100 and 200 mg/kg, showed considerable (p < 0.001) inhibition against the onset and frequency of diarrhea. On the other hand, JCR, CRAE, and CRME exerted significant effects (p < 0.001) on the percentage inhibition (PI) of diarrhea and gastrointestinal charcoal transit in a dose-dependent manner. In this respect, the maximum PI (p < 0.01) of JCR, CRAE, and CRME in different experimental paradigms was 43.13, 49.14, and 55.99 %, respectively.
Taken all together, results from this study reveal that the juice, aqueous, and methanol extract of C. reflexa exhibit significant anti-motility and anti-secretory potential. These findings may explain the medicinal use of C. reflexa in folk medicine as an antidiarrheal medicinal plant.
Pistacia integerrima has many medicinal uses in therapeutic as well as folk medicine. P. integerrima has been used for the treatment of different ailments such as blood purifier, anti-inflammatory, ...and as remedy for gastrointestinal disorders such as vomiting and diarrhea, expectorant, cough, asthma and fever.
The main objective of this research work was to evaluate the effect of pistagremic acid (PA) isolated from the galls of Pistacia integerima in acute toxicity and gastrointestinal (GIT) motility tests.
Compound 1 namely pistagremic acid (PA) (at 10, 50, 100 mg/kg i.p) were assessed for their in-vivo gastrointestinal motility test using charcoal screening model.
Results revealed that pretreatment of PA exhibited substantial safety in acute toxicity test up to the dose of 500 mg/kg p.o. However, when studied in charcoal meal GI transit test, PA caused significant (p < 0.05) attenuation of GIT motility and an increase in intestinal transit time, comparable to atropine (a muscarinic receptor blocking agent).
In conclusion, PA displayed a strong dose-dependent reduction in GIT motility with considerable safety.
This study deals with α-glucosidase and β-secretase inhibitory screening of extract/fractions and isolated daturaolone (1), namely, 3-oxo-6-β-hydroxy-β-amyrin (daturaolone) from chloroform fraction ...of Datura metel L. Among entire fractions, the chloroform soluble fraction showed excellent activity against α-glucosidase with % inhibition 90.8 with IC50160.2±1.85 μg and daturaolone (1) with 98.7% inhibition with IC50840.4±1.74 μM, respectively. Similarly, extract and daturaolone (1) also exhibited significant activity against the β-secretase enzyme (BACE1) with % activities 88.27 and 95.19 and with IC50 values 304.21±2.98 μg and 260.70±1.87 μM, respectively, as compared to the standard inhibitor (Ans670, Sta671, Val672)-amyloid-β/A4 precursor protein 770 fragments 662-675) with % activity 94.21 and IC50 value 289.24±1.60 μM. This finding encourages and opens a new window for further detail phytochemical investigation on D. metel in order to isolate novel compounds with promising enzyme inhibitory potential.
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