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1.
Pak J Pharm Sci ; 34(5(Supplementary)): 1975-1982, 2021 Sep.
Article in English | MEDLINE | ID: mdl-34836869

ABSTRACT

The pharmacological importance and ecofriendly nature of medicinal plants holding a unique edge in the arena of pharmaceutical industries. Therefore, the current research was aimed to evaluate the phytochemical constituents and potential antioxidant, in vitro anticancer and antibacterial activity of Carpesium nepalense seeds essential oil. The analysis performed through Gas chromatography/Mass spectroscopy confirmed the presence of different types of biologically active compounds. At the concentration of 500µg/mL, n-hexane fraction of C. nepalense showed highly significant (P<0.001) antioxidant activity in 2,2-diphenyl-1-picrylhydrazyl, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid and superoxide assays with the percentage inhibitions of 86.60±1.6%, 82.55±1.0% and 80.50±1.0% respectively. The extract also produced highly significant anticancerous activity against different cell lines at 500µg/mL. The significant antibacterial activity of extract was observed against bacterial strains with the zone of inhibitions of 24.3±0.8, 28.20±0.10, 22.33±0.11 and 33.22±0.10 mm respectively. The significant damage in bacterial cell membranes was also observed in atomic force microscopic analysis. In the light of obtained findings, it is concluded that C. nepalence proved to be a potential candidate as an alternative medicinal agent.


Subject(s)
Anti-Bacterial Agents/pharmacology , Antineoplastic Agents, Phytogenic/pharmacology , Antioxidants/pharmacology , Asteraceae/chemistry , Plant Oils/pharmacology , Seeds/chemistry , Bacteria/drug effects , Biphenyl Compounds , Cell Line, Tumor , Cell Membrane/drug effects , Drug Screening Assays, Antitumor , Humans , Microbial Sensitivity Tests , Phytochemicals/pharmacology , Picrates , Superoxides/metabolism
2.
BMC Complement Med Ther ; 21(1): 198, 2021 Jul 12.
Article in English | MEDLINE | ID: mdl-34253216

ABSTRACT

BACKGROUND: Degenerative kidney diseases are mostly associated with oxidative stress. Natural products are considered as the antioxidants enrich food that can restrict the progress of oxidative stress induced disorders. Therefore, the present study was aimed to evaluate the renal protective effect of Ajuga parviflora leaf extract in carbon tetrachloride intoxicated rats. METHODS: The hydromethanolic extract of A. parviflora leaves was obtained by extracting twice in 60% methanol. The principal bioactive constituents were detected by LC/MS analysis. Toxicity of plant extract was assessed using brine shrimp lethal toxicity test and acute toxicity model on healthy Sprague-Dawley male rats. Nephroprotective effects of plant extract were also evaluated on rats by inducing CCl4 renal toxicity in comparison with positive control and naïve groups. The dose of A. parviflora administered to animal was 100, 200 and 300 mg/kg. All administrations were given orally on an alternate day basis for 30 days. Urine and serum biomarkers were analyzed, along with antioxidant enzymes. Finally, the DNA damages, lipid peroxides, hydrogen peroxides and nitrites were assessed in rat's renal tissue. The histopathology alterations in renal tissues were further studied for kidney damages. RESULTS: The LC/MS analysis confirmed the presence of different important pharmacological compounds in A. parviflora methanolic leaf extract. The key bioactive compounds include pyocyanin, zonisamide, D Saccharic acid, altretamine, carbocyclic thromboxane A2, Sinapyl alcohol, and vitamin C. The important polypeptides identified include Lys-Tyr-Lys, His-His-Lys, Met-Asp-Arg, Phe-Val-Arg, and PyroGlu-Val-Arg. The LD50 of A. parviflora was found to be > 1000 µg/mL. A. parviflora administration significantly subsides CCl4 toxicity in rats, reduced the elevated level of RBCs, pus and epithelial cells. The abnormal elevated level of specific gravity, creatinine, urobilinogen, urea and albumin were also reduced to normal physiological level. The reduced urinary protein and pH were also normalized. The serum urobilinogen, urea and total bilirubin levels were also reversed to normal levels while the diminished albumin and total protein levels also came to normal. The important phase I and II enzyme levels were also reversed in A. parviflora administered rats. The H2O2, thiobarbituric acid reactive substance (TBARS) and nitrite levels were significantly decreased. Furthermore, the damaged DNA and histopathological changes in CCl4 exposed rats were also highly significantly reversed after the administration of A. parviflora. All effects were significant (P < 0.05) and highly significant (P < 0.005) at 100 and 300 mg/kg respectively. CONCLUSION: The restored urine and serum profile of various parameters to normal physiological levels suggests that the A. parviflora has potential antioxidant and repairing potential in renal disorders.


Subject(s)
Acute Kidney Injury/chemically induced , Acute Kidney Injury/drug therapy , Ajuga/metabolism , Ajuga/toxicity , Antioxidants/pharmacology , Carbon Tetrachloride/toxicity , Phytochemicals/pharmacology , Plant Extracts/pharmacology , Animals , Rats , Rats, Sprague-Dawley
3.
Pak J Pharm Sci ; 33(2): 675-683, 2020 Mar.
Article in English | MEDLINE | ID: mdl-32276914

ABSTRACT

The present work reports the synthesis of Schiff base series of nicotinic hydrazide (C-1-C-5) and it's antibacterial and wound healing evaluation. The synthetic molecules were characterized with different spectroscopic techniques and explored for their antibacterial potential. The objective of this work was to explore antimicrobial agent using two types of microorganisms, one Gram-positive (S. aureus ATCC 9144) and one Gram-negative (E. coli ATCC 10536). C-2, C-4 and C-5 potentially inhibit bacterial growth (p<0.001). Atomic force microscopy (AFM) imaging was obtained to get high-resolution images of the effect of treated drugs on the bacterial morphology. The images obtained also revealed the antibacterial effects of potent molecule. The magnified pictures captured under AFM suggest significantly damaged cell surface and disturbed morphology. The compounds were further analyzed for in vivo wound healing potential on mice. The compound C-2, C-4 and C-5 heal the wounds comparatively in less time duration as compared to control group (p<0.001). Compound C-1 and C-3 took more time to heal the wound as compare to compound C-2, C-4 and C-5. The re-epithelialization process of wound in animals group treated with potent compound was highly significant (p<0.001) and faster than control. Results of this study suggest that the compounds C-2, C-4 andC-5 possess pronounced antibacterial and wound healing potential and need to be further evaluated for mechanism of action.


Subject(s)
Anti-Bacterial Agents/chemical synthesis , Cell Wall/drug effects , Microscopy, Atomic Force/methods , Nicotine/analogs & derivatives , Schiff Bases/chemical synthesis , Wound Healing/drug effects , Animals , Anti-Bacterial Agents/pharmacology , Cell Wall/physiology , Escherichia coli/drug effects , Escherichia coli/physiology , Mice , Microbial Sensitivity Tests/methods , Nicotine/chemical synthesis , Nicotine/pharmacology , Schiff Bases/pharmacology , Staphylococcus aureus/drug effects , Staphylococcus aureus/physiology , Wound Healing/physiology
4.
Pak J Pharm Sci ; 33(1(Supplementary)): 325-331, 2020 Jan.
Article in English | MEDLINE | ID: mdl-32122865

ABSTRACT

Owing to its traditional applications, the current study focuses on Ajuga parviflora (A. parviflora) leaves extract for phytochemical and pharmacological analysis. The principle constituents were identified through gas chromatography (GC), and gas chromatography/mass spectroscopy (GC/MS), these includes phthalic acid, squalene, α-tocopherol, vitamin E, phytol, 2-methylenecholestan-3-ol, stigmasterol, cholest-22-ene-21-ol and 3,5-dehydro-6-methoxy. Hepatoprotective effect of A. parviflora was evaluated through isoniazid and rifampicin (INH and RFP) induced hepatotoxicity in rat. Animals in group A were treated with INH and RFP 50 mg/kg. Animals in group B, C, and D were pre-treated with A. parviflora extract at 100, 200 and 300 mg/kg dose prior drug administration. A. parviflora extract at 200 and 300 mg/kg in group C and D significantly reduced aspartate aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase (ALP), and bilirubin (p<0.001) as compare to group B (100mg/kg). Total protein (TP) was also significantly (p<0.01) reduced in group C and D at dose of 200 and 300 mg/kg, respectively. The extract pre-treated animals with (A. parviflora, 200, and 300 mg/kg) showed that the epithelium of the central portal vein is intact with replete glucagon. The pre-treatment with A. parviflora protected the liver from INH and RFP induced hepatotoxicity. The results of pre-treated animals with A. parviflora 200, and 300 mg/kg dose prettily revert the severely disturb parameters like, cytolysis, lymphocytic infiltration, and lymphoid aggregate in portal vein and hydropic degeneration. The decrease peroxisome proliferator-receptor activator-δ (PPAR-δ) gene expression by INH, and RFP was significantly up regulated by A. parviflora extract in pre-treated animals at 200 and 300 mg/kg dose. These findings provide baseline pharmacological uses of A. parviflora in liver disorders. Further investigations are required for identification and isolation of biologically active components responsible for pharmacological activity.


Subject(s)
Ajuga , Antitubercular Agents/toxicity , Chemical and Drug Induced Liver Injury/drug therapy , Plant Extracts/isolation & purification , Plant Extracts/therapeutic use , Plant Leaves , Animals , Chemical and Drug Induced Liver Injury/pathology , Chromatography, Gas/methods , Male , Mass Spectrometry/methods , Phytochemicals/isolation & purification , Phytochemicals/therapeutic use , Rats , Rats, Wistar
5.
Pak J Pharm Sci ; 33(5): 1987-1994, 2020 Sep.
Article in English | MEDLINE | ID: mdl-33824105

ABSTRACT

The threat of multi-drug resistant bacterial pathogens evokes researchers to synthesized safe and effective chemotherapeutic agents for nano-drug delivery system. In current study, Schiff base of nicotinic hydrazide(NHD) and its silver nanoparticles(NHD-AgNPs) were synthesized and characterized. These compounds were investigated for cytotoxicity, antibacterial and AFM activity. The NHD showed LD50 at >1000µg/mL while NHD-AgNPs didn't exhibit toxicity at 1000µg/mL against 3T3 cell line. The NHD showed zone of inhibition against two strains of salmonella enteric (ATCC 14028 and 700408) 45.29±1.66 and 48.01±1.43mm respectively at 160µg/mL (p<0.01) while NHD-AgNPs exhibited 55.87±2.08 and 52.88±1.42 mm respectively at 130µg/mL (p<0.001) in disc diffusion method. NHD showed more than 70% growth inhibition for both strains at 85 and 125µg/ml (p<0.01) respectively, while NHD-AgNPs inhibit 80% and 75% respectively at 75 and 125 µg/ml (p<0.01, p<0.001) against Alamar blue antibacterial assay. For morphological changes in bacterial cell wall NHD and NHD-AgNPs treated bacterial cells were observed under atomic force microscope(AFM) and treated bacterial cells were severely damaged with leaked cytoplasmic contents as compare to untreated bacterial cell. These results validate that NHD-AgNPs were highly active as compared to NHD against both strains at their MIC concentrations. In future, comparative wound healing potential will be emphasized.


Subject(s)
Anti-Bacterial Agents/pharmacology , Cell Wall/drug effects , Hydrazines/pharmacology , Metal Nanoparticles , Microscopy, Atomic Force , Nicotinic Acids/pharmacology , Salmonella enterica/drug effects , Schiff Bases/pharmacology , Silver Compounds/pharmacology , 3T3 Cells , Animals , Anti-Bacterial Agents/chemical synthesis , Anti-Bacterial Agents/toxicity , Disk Diffusion Antimicrobial Tests , Drug Compounding , Hydrazines/chemical synthesis , Hydrazines/toxicity , Mice , Nicotinic Acids/chemical synthesis , Nicotinic Acids/toxicity , Salmonella enterica/growth & development , Schiff Bases/chemical synthesis , Schiff Bases/toxicity , Silver Compounds/chemical synthesis , Silver Compounds/toxicity
6.
Pak J Pharm Sci ; 32(5(Special)): 2405-2413, 2019 Sep.
Article in English | MEDLINE | ID: mdl-31894025

ABSTRACT

Monotheca buxifolia has traditionally been employed in folk medicines to cure of infectious diseases. Current study was aimed to standardize the M. buxifolia leaves extract and evaluate its antibacterial and anticancer activity. Phytochemical analysis was carried through GC, GC/MS, FTIR, and ICP-OES analytical techniques. Antibacterial assay of the crude extract was performed by using tetrazolium micro plates. The extract treated bacteria were observed under (AFM) atomic force microscope and PCR was used for DNA amplification. The anti-proliferative activity of M. buxifolia leaves extract was examined through MTT cytotoxicity assay. The bacterial strains employed in this study were S. epidermidis ATCC (13518), S. aureus ATCC (25923), P. aeruginosa ATCC (10145), and E. coli ATCC (10536). Minimum inhibitory concentration (MIC50) against gram positive bacteria was significantly (p<0.01) achieved at 50 and 75µg/mL. MIC50 against E. coli and P. aeruginosa was also significant at 100µg/mL (p<0.01). M. buxifolia leaves extract damaged the cell walls gram-positive and gram-negative bacteria, while biofilm around gram positive bacteria was significantly damaged. The DNA decantation was also inhibited of S. aureus and S. epidermidis, however, no any impact was observed on E. coli and P. aeruginosa DNA decantation. The cytotoxicity findings suggested that the crude extract of M. buxifolia leaves at 1000µg/mL gives significant inhibition 73.96±2.0%, 83.76±1.2%, 77.66±1.2% and 72.67±1.6% against MDA-MB-231, MCF-7, HeLa and H460 cell lines respectively at (p<0.001). It may be concluded that M. buxifolia leaves extract have significant and promising antibacterial and anti-cancer activities which could be helpful to establish new antimicrobial and anticancer agents.


Subject(s)
Anti-Bacterial Agents/pharmacology , Antineoplastic Agents, Phytogenic/pharmacology , Plant Extracts/pharmacology , Sapotaceae/chemistry , Anti-Bacterial Agents/chemistry , Antineoplastic Agents, Phytogenic/chemistry , Bacteria/drug effects , Cell Line, Tumor , Cell Survival/drug effects , Humans , Plant Extracts/chemistry , Plant Leaves/chemistry
7.
Pak J Pharm Sci ; 31(4(Supplementary)): 1519-1528, 2018 Jul.
Article in English | MEDLINE | ID: mdl-30058544

ABSTRACT

Owing to its pharmacological versatility, the current study focuses the evaluation of Monotheca buxifolia (M. buxifolia) bark crude extract and its fractions for phytochemical and pharmacological analysis. Phytochemical investigation of bark extract was carried out through GC-MS, LC-MS and FT-IR. ICP-OES was used for analyzing essential metals in bark extract. Plant samples were further investigated for their in vitro antioxidant and in vivo neuropharmacological activities in mice. Phytochemical analysis of bark extract revealed the presence of various active constituents such as serotonin, α-tocopherol, 3-deoxyestradiol, ascorbyl palmitate and cirsimaritin. Metal analysis showed presence of various metals in diverse concentration. M. buxifolia bark extract and its chloroform fraction showed significant antioxidant activity against DPPH (89.55 ±1.29; 84.80±1.66%), superoxide (82.10 ±1.86; 80.0±1.0%), H2O2 (80.55±2.0; 78.10±2.26%) at 500µg/mL concentration. Similarly, bark extract and its chloroform fraction demonstrated antidepressant activity in mice and improve generalized locomotive behavior. The effective use of M. buxifolia in treatment and management of depression and free radicals based disorders can be safely concluded from the results of present study.


Subject(s)
Antioxidants/pharmacology , Phytochemicals/pharmacology , Plant Bark , Plant Extracts/pharmacology , Sapotaceae , Animals , Antioxidants/chemistry , Antioxidants/isolation & purification , Dose-Response Relationship, Drug , Drug Evaluation, Preclinical/methods , Female , Immobilization/physiology , Male , Mice , Motor Activity/drug effects , Motor Activity/physiology , Phytochemicals/chemistry , Phytochemicals/isolation & purification , Plant Extracts/chemistry , Plant Extracts/isolation & purification
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