Datura metel
Linn is used traditionally for the treatment of various diseases including relaxation of smooth muscles, relief of fever, as well as gastrointestinal disorder. This study deals with the ...bio-guided isolation of an active, amyrin-type triterpenoid, namely 3-oxo-6-
β
-hydroxy-
β
-amyrin (daturaolone;
1
), from the chloroform fraction of
Datura metel
L. (Angel’s trumpet) fruits and its gastrointestinal motility, antipyretic, and muscle relaxation effects in animal models. The chemical structure of daturaolone (
1
) was elucidated by NMR spectroscopy and crystallography techniques. The chloroform fraction and daturaolone (
1
) were assessed for the GIT motility test. Data exhibited in charcoal meal GI transit test show that chloroform fraction and daturaolone (
1
) significantly reduce GIT motility and increased intestinal transit time, comparable to the standard (atropine), a muscarinic receptor blocking agent. Muscle relaxant potency of the extract and daturaolone (
1
) was assessed in various animal paradigms. In the inclined plane screening test, it produced a significant (P < 0.05) muscle relaxation potential in a dose-dependent manner after 30, 60, and 90 min. Likewise, the muscle relaxation potential of the extract and daturaolone (
1
) was strongly complemented by the chimney and traction test, representing a dominant effect after 60 min of sample administration. The chloroform fraction showed good antipyretic activity, and while daturaolone (
1
) exhibited significant activity at a higher dose, the maximum effect (84.64%) was at 20 mg/kg i.p. In acute toxicity screening test, the chloroform extract (100, 250, 500, and 1,000 mg/kg) and daturaolone (
1
) (5, 10, 20, and 50 mg/kg) were found safe. In conclusion, the chloroform extract and daturaolone (
1
) exhibited strong gastrointestinal motility, muscle relaxation, and antipyretic activity in different animal models and intestinally, was found safe at higher tested doses.
Anti-inflammatory, analgesic, and sedative medicine is used with numerous side effects, including peptic ulcer, headache, addiction, and other complications. In this regard, discovery research is ...undergoing a process to discover effective, safe, and economical drugs with no side effects. The aim of this study was to assess chloroform extracts and isolated compounds for anti-inflammatory, analgesic, and sedative activities in animal models. The anti-inflammatory potential was measured by using the carrageenan-induced and histamine-induced paw edema procedure, while the analgesic potential was determined using a hot plate analgesiometer. The sedative effect was observed in an animal model for screening of the locomotor effect of the extract and isolated compound 1. Our data exhibited that the extract and compound 1 attenuated carrageenan-induced and histamine-induced paw edema (93.98 and 89.54%, respectively). Furthermore, compound 1 attenuated biphasic edema associated with histamine and prostaglandins. The chloroform extract showed a moderate analgesic effect; however, compound 1 showed a significant analgesic potential (p < 0.001) by increasing the latency time of the animals in the thermally induced algesia model. Compound 1 exhibited a significant sedative effect and dose-dependent analgesic activity. It is concluded that the chloroform extract and compound 1 showed remarkable anti-inflammatory, analgesic, and sedative activities. This research work strongly rationalizes the folkloric usage of Diospyros kaki in the treatment of inflammation, pain, and insomnia.
Tetrasubstituted 2-acetylthiophene derivative 5 was synthesized and then condensed with various nitrogen nucleophiles such as 5-amino-1,2,4-triazole, 2-aminobenzimidazole, aniline or p-chloroaniline ...to afford the corresponding iminothiophene derivatives 6-8a,b. Condensation of thiophene 5 with malononitrile as carbon nucleophile afforded compound 9, which underwent nucleophilic addition with DMF-DMA to afford compound 10. The newly synthesized products were characterized by elemental analysis, IR, MS, ¹H-(13)C-NMR and CHN analysis and then evaluated for their antimicrobial activity. Results of the in vitro antibacterial activity showed that thiophene derivative 7 was found to be more potent than the standard drug gentamicin against Pseudomonas aeruginosa. Some of these compounds showed potential antimicrobial activities. Molecular docking and Osiris/Molinspiration analyses show the crucial role and impact of substituents on bioactivity and indicate the unfavorable structural parameters in actual drug design: more substitution with electronic donor group doesn't guarantee more effective bioactivity. This study should greatly help in an intelligent and a controlled pharmacomodulation of antibiotics.
The green biosynthesis of metal nanoparticles of already explored phytomedicines has many advantages such as enhanced biological action, increased bioavailability, etc. In this direction, keeping in ...view the peculiar medicinal value of
L., we synthesized its silver nanoparticles (AgNPs) by adopting eco-friendly and cost-effective protocol by using methanolic and aqueous extract of
. The synthesized AgNPs were characterized by using several techniques including UV spectroscopic analysis, FTIR analysis, and atomic force microscopy. The methanolic/aqueous extracts of
and synthesized AgNPs were assessed for antioxidant potential and antimicrobial effect. The preliminary screening showed that the
extracts have variety of reducing phytochemicals including tannins, terpenoids, flavonoids, and cardiac glycosides. The green synthesis of AgNPs was confirmed by the appearance of sharp peak at 430–450 nm in the UV-Visible spectra. The FTIR spectral analysis of extract and AgNPs exhibited that peaks at 2947.23, 2831.50, 2592.33, 2522.89, and 1,411 cm
disappeared in the spectra of FTIR spectra of the AgNPs, indicating carboxyl and hydroxyl groups are mainly accountable for reduction and stabilization of AgNPs. Atomic force microscopic scan of the synthesized AgNPs confirmed its cylindrical shape with size of 25 µm. The extracts and AgNPs were investigated for antioxidant potential by DPPH-free radical essay, which showed that aqueous extract has significant and dose-independent antioxidant activity; however, the synthesized AgNPs showed decline in antioxidant activity. The extracts and synthesized AgNPs were also evaluated for antibacterial activity against
,
, and
Neither extract nor AgNPs were active against
The aqueous and methanolic extract exhibited inhibition against
and their synthesized AgNPs were active against
Our data concluded that the extracts of
have necessary capping and reducing agents which make it capable to develop stable AgNPs. The aqueous extract of
has potential antioxidant effect; however, the AgNPs did not enhance its free radical scavenging effect. The bacterial strains’ susceptibility of the extract and AgNPs was changed from
to
, respectively. The biological action of AgNPs is changed in case of antibacterial activity which means that AgNPs might change the specificity of
and likewise other drugs.
Traditionally, Diospyros lotus Linn is used for insomnia and other associated disorders. Insomnia is a worldwide disorder with different etiology which is treated with different synthetic medicine ...associated with addiction. Natural products are generally devoid of such addition with good efficacy. Current research was conducted to evaluate the sedative and hypnotic effects of dimeric naphthoquinones such as dinaphthodiospyrol A (1), dinaphthodiospyrol B (2), dinaphthodiospyrol C (3), dinaphthodiospyrol D (4), dinaphthodiospyrol E (5) and dinaphthodiospyrol F (6) isolated from the chloroform fractions of D. lotus. The sedative and hypnotic effects at the dose of 5 and 10 mg/kg (each compound) were assessed through open field and phenobarbital induced sleep test, respectively. In the case of open field test the administration of tested compounds significantly hindered the movement of animals, while in case of hypnotic effect the tested samples significantly improved the onset and duration of sleep as compared to control. The overall effects were in a dose dependent manner. The compounds were also assessed for acute toxicity, but no toxicity was observed. In this regard, our research triumphantly announced the strong chemical base for the folkloric values of the plant with their fringe benefits and implemented a platform for further aspects of mechanistic and clinical studies. A possible mechanism of in vivo inhibition was studied by using docking simulations on GABA receptors. Binding orientations and types of interactions revealed that a possible mechanism behind these pharmacological actions might be interaction with GABA receptors.
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•Six naphthoquinones; dinaphthodiospyrol (A-F) were isolated from the chloroform fractions of Diospyros lotus.•The dinaphthodiospyrol (A-F) showed excellent sedative effect at the dose of 20 mg/kg.•The dinaphthodiospyrol (A-F) showed significant hypnotic effect at the dose of 20 mg/kg.•Binding orientations and binding energy values show strong binding affinity of compounds with GABA receptors.
Diospyros kaki (Japanese persimmon) is cultivated specious of the Diospyros genus. D. kaki is a multi-medicinal application in the folk system for the cure of ischemic stroke, angina, ...atherosclerosis, muscle relaxation, internal hemorrhage, hypertension, high cough, and infectious disease. The main objective of this study was the isolated bioactive metabolites from chloroform fractions of D. kaki. The extract and fractions were then tested for various in-vitro (antioxidant and lipoxygenase) and in-vivo (muscle relaxant) activities. The repeated chromatographic separation of chloroform extract afforded compound 1. Compound 1, n-hexane, and chloroform fractions were evaluated for in vitro antioxidant, lipoxygenase inhibitory, and in vivo muscle relaxant potency. The chloroform extract has 79.54% interaction with DPPH at higher concentrations (100 μg/ml) while the compound exhibited a maximum effect of 95.09% at 100 μg/ml. Compound 1 exhibited significant lipoxygenase inhibitory activity with an IC50 value of 36.98 μM followed by a chloroform extract of 57.09 μM. Similarly, compound 1 and chloroform extract showed excellent muscle relaxant effects at a higher dose. From this investigation, it is concluded that extracts and pure compounds exhibited promising antioxidant, lipoxygenase inhibitory, and muscle relaxant activity. This study excellently rationalizes the traditional usage of D. kaki in curing various diseases. Furthermore, the docking results indicate, that the isolated compound fits well into the active site of the lipoxygenase, and makes strong interactions with the target protein.
Parthenium hysterophorus
L. (Congress grass, family Asteraceae) is found throughout the global agricultural and vacant lands. In the present work, the pharmacognostic, pharmacological and ...allelopathic traits of various parts (root, stem and leaves) of
P. hysterophorus
grown in Pakistan were investigated.
P. hysterophorus
growing/flowering season starts from March–April till August–September. The plant has tap root with numerous rootlets and root hairs. Stem is straight, with light groove, covered with hairs and numerous profusely branches, wherein the stem reaches up to 150 cm in height. The leaves are simple, dull green in color, alternate, leaflets with profusely dissected regions and hairs are present on the lower surface of leaf. Transverse section (TS) of root revealed epidermis, cortex, endodermis, xylem, phloem and medullary rays running from endodermis towards the center. TS of stem was circular in outline with shallow ridges covered with hairs. TS of leaf consisted of epidermis, which is intermitted by simple, glandular, branched and multicellular trichomes. Powder drug microscopy of roots revealed the presence of epidermal cell, phloem elements, fiber, cluster/group of fibers, root hairs, xylem vessels and medullary rays. The stem powder drug microscopy showed the presence of trichomes, fibers, parenchymatous cells, lignified vessel, group/cluster of vessels, secretory gland with epidermal cells, prismatic crystal of Ca oxalate and phloem elements with parenchyma cells. Phytochemical screening of diethyl ether, ethanol and aqueous extracts of root, stem and leaves showed the presence of amino acids, fixed oils, alkaloids, flavonoids, phenols, carbohydrates, proteins and triterpenoids, while steroidal glycosides, gum and mucilage were absent in all plant parts. Chemical composition showed that moisture, lipids, protein contents and total gross energy were higher in plant grown in summer season as compared to winter season. On the other hand, ash, fibers and carbohydrate contents were higher in winter and declined in summer season.
The current investigation aims to synthesize gold nanoparticles (AuNPs) from aqueous extract of
Tamarindus indica
and to evaluate the in vitro anti-bacterial and in vivo sedative and anelgescic ...activities of crude extract as well as synthesized AuNPs. Several methods have been reported to synthesize AuNPs; however, most of them were not ecofriendly. In the present study, the green synthesis of AuNPs has been carried out. Using the green synthesis method, AuNPs of
T. indica
were synthesized at room temperature (25 °C) by mixing 5 mL of HAuCl
4
(1 mM) with 1 mL of
T. indica
seed extract solution. This extract solution was prepared by taking 5 gm dry seeds in 100 mL of double deionized water with continuous stirring for up to 24 h at 80 °C. The stability of AuNPs was confirmed with the help of relevant experimental techniques including ultraviolet–visible (UV/Vis) showing maximum absorbance at 535–540 nm, Fourier transform infrared showing a broad signal at 3464 cm
−1
which can be attributed to either amide or hydroxyl functionalities and atomic force microscopy analysis showed that the biomaterial surrounding AuNPs was agglomerated which proves the formation of discrete nanostructutres. These AuNPs have been evaluated for their antibacterial potential. The results revealed good antibacterial activity of the samples against
. Klebsiella pneumonia, Bacillus subtilis
and
Staphylococcus epidermidis
with 10–12 mm zone of inhibition range. The AuNPs were also found stable at high temperature, over a range of pH and in 1 mM salt solution. Moreover, the crude extract and respective AuNPs also exhibited interesting sedative and analgesic activities. Hence, we focused on phytochemicals-mediated synthesis of AuNPs considered as greatest attention in the treatment of anti-bacterial, analgesic, and sedative.
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