Groundwater contamination is a growing global concern. The objective of the present study is to assess the groundwater quality of Khairpur district, Sindh, Pakistan-a region which is emblematic of broad environmental and public health challenges prevalent in South Asian countries. The study also aims to comprehend the impact of arsenic (As), fluoride (F), and nitrate (NO) dynamics and its health implications.
View Article and Find Full Text PDFAntibiotics (Basel)
December 2024
In the face of rising the threat of resistant pathogens, antimicrobial peptides (AMPs) offer a viable alternative to the current challenge due to their broad-spectrum activity. This study focuses on enhancing the efficacy of temporin-SHa derived NST-2 peptide (), which is known for its antimicrobial and anticancer activities. We synthesized new analogs of using three strategies, i.
View Article and Find Full Text PDFSecondary biotransformation of 11β-hydroxy-dianabol (11β,17β-dihydroxy-17α-methylandrost-1,4-dien-3-one) (1), catalyzed by using two fungi Gibberella fujikuroi and Cunninghamella blakesleeana at ambient conditions, was carried out to synthesize its analogues. Transformation of compound 1 with G. fujikuroi yielded a new metabolite, 11β, 17β-dihydroxy-17α-methyl-5β-androst-1-ene-3-one (2), while four new derivatives, 6β, 17β-dihydroxy-17α-methylandrost-1,4-diene-3,11-dione (3), 15α,17β-dihydroxy-17α-methylandrost-1,4-diene-3,11-dione (4), 6β,11β,17β-trihydroxy-17α-methylandrost-1,4-dien-3-one (5), and 7β,11β,17β-trihydroxy-17α-methylandrost-1,4-dien-3-one (6) were obtained by transformation with C.
View Article and Find Full Text PDFAntimicrobial peptides (AMPs) are a promising class of therapeutic alternatives with broad-spectrum activity against resistant pathogens. Small AMPs like temporin-SHa () and its first-generation analog [G10a]-SHa () possess notable efficacy against Gram-positive and Gram-negative bacteria. In an effort to further improve this antimicrobial activity, second-generation analogs of were synthesised by replacing the natural glycine residue at position-10 of the parent molecule with atypical amino acids, such as D-Phenylalanine, D-Tyrosine and (2-Naphthyl)-D-alanine, to study the effect of hydrophobicity on antimicrobial efficacy.
View Article and Find Full Text PDFVanillic acid (VA) - a naturally occurring phenolic compound in plants - is not only used as a flavoring agent but also a prominent metabolite post tea consumption. VA and its associated compounds are believed to play a significant role in preventing diseases, underscoring the need for a systematic investigation. Herein, we report a 4-step synthesis employing the classical organic reactions, such as Willamson's alkylation, Fischer-Spier reaction, and Steglich esterification, complemented with a protection-deprotection strategy to prepare 46 VA derivatives across the five series (1a-1i, 2a-2i, 3, 3a-3i, 4a-4i, 5a-5i) in high yields.
View Article and Find Full Text PDF(A.Rich.) Miers (Menispermaceae) has traditionally been used to alleviate headaches, rheumatism, mycetoma, and diabetes, among others.
View Article and Find Full Text PDFThe emergence of multidrug-resistant (MDR) pathogens and the gradual depletion of available antibiotics have exacerbated the need for novel antimicrobial agents with minimal toxicity. Herein, we report functionally substituted pyridine carbohydrazide with remarkable antimicrobial effect on multi-drug resistant strains. In the series, compound 6 had potent activity against four MDR strains of spp.
View Article and Find Full Text PDFA synthetic anabolic-androgenic steroid, methylstenbolone (1), was structurally transformed into a series of nine analogues, 2,17α-dimethyl-7α,17β-dihydroxy-5α-androst-1-en-3-one (2), 2,17α-dimethyl-15β,17β-dihydroxy-5α-androst-1-en-3-one (3), 2,17α-dimethyl-6α,9α,17β-trihydroxy-5α-androst-1-en-3-one (4), 2-methyl-17β-hydroxy-17α-(hydroxymethyl)-5α-androst-1-en-3-one (5), 2-methyl-11β,17β-dihydroxy-17α-(hydroxymethyl)-5α-androst-1-en-3-one (6), 2-methyl-17β-hydroxy-17α-(hydroxymethyl)-5α-androst-1-en-3,6-dione (7), 2-methyl-17β-hydroxy-17α-(hydroxymethyl)-5β-androst-1-en-3,6-dione (8), 2,17α-dimethyl-7β,17β-dihydroxy-5α-androst-1-en-3-one (9), and 2,17α-dimethyl-12β,17β-hydroxy-5α-androst-1-en-3,7-dione (10) by fungal cell suspension cultures, Macrophomina phaseolina and Cunninghamella blakesleeana for the first time. Among those, compounds 2-4 and 6-10 were identified as new. Herein, spectral data of metabolite 5 was reported for the first time.
View Article and Find Full Text PDFA new clerodane diterpene, named 6α-hydroxy-3,13E-clerodien-15-oic acid (1), together with a known clerodane diterpene (2), four known labdane diterpenes (3-6), a triterpenoid (7), a known steroid (8), and two benzenoid compounds (9 and 10) were isolated from Detarium microcarpum Guill. & Perr. The structures of all obtained compounds were determined by chemical properties and spectroscopic evidence, accompanied by comparisons with data in the literature.
View Article and Find Full Text PDFA new sesquiterpene (Prosoterpene, ) and eleven reported compounds (-) of several classes, such as flavonoids, alkaloids, phenolic acids, and long-chain alcohols, were isolated from the BuOH extract of (Guill. & Perr.) Taub.
View Article and Find Full Text PDFTwo new ursane-type triterpenoids, named Polyanside A () and B (), along with eleven known compounds (-), were isolated and elucidated from (Benth.) Prance. The structures of these compounds were elucidated based on chemical evidence and multiple spectroscopic data.
View Article and Find Full Text PDFIn search of anti-inflammatory compounds, novel scaffolds containing isonicotinoyl motif were synthesized via an efficient strategy. The compounds were screened for their in vitro anti-inflammatory activity. Remarkably high activities were observed for isonicotinates - and -.
View Article and Find Full Text PDFEthnopharmacological Relevance: Schefflera is the largest genus in the family Araliaceae, which contains 602 known species indigenous to Asia, Africa, and the southwest Pacific region, several of which are used in traditional medicine.
Aim Of The Review: The review discusses current knowledge of the traditional uses, phytochemistry, and biological activities of Schefflera species, to assess the medicinal potential of this genus.
Materials And Methods: The literature were explored using the keyword "Schefflera" in SciFinder®, Google Scholar®, and PubMed® databases.
Nucleotide-binding oligomerization domain 2 (NOD2) is cytosolic surveillance receptor of the innate immune system capable of recognizing the bacterial and viral infections. Muramyl dipeptide (MDP) is the minimal immunoreactive unit of murein. NOD2 perceives MDP as pathogen-associated molecular pattern, thereby triggering an immune response with undesirable side-effects.
View Article and Find Full Text PDFA new steroidal alkaloid, michainine (), was isolated from Fomin, along with nine known compounds - of different classes, including ribonucleoside, steroids, and fatty acids, which were isolated for the first time from this plant. Their structures were elucidated through extensive spectroscopic techniques, as well as by comparing the data in the literature. Furthermore, the dichloromethane fraction of showed a positive butyrylcholinesterase inhibitory activity, along with non-cytotoxicity against 3T3 cell line.
View Article and Find Full Text PDFMuramyl dipeptide (MDP) - an essential bacterial cell wall component - is recognized by our immune system as pathogen-associated molecular pattern (PAMP) which results in immune responses with adverse toxic effects. In order to harness the beneficial properties from the pro-inflammatory characteristics of the bacterial cell wall motif, MDP was strategically re-designed while conserving the L-D configurations of the dipeptide moiety. The muramic acid was replaced with a hydrophilic arene and lipophilic chain was introduced at peptide end to give the amphiphilic desmuramyl peptides (DMPs).
View Article and Find Full Text PDFJ Coll Physicians Surg Pak
February 2016
Objective: To determine the serum 25-hydroxycalciferol levels [25(OH)D] in adults with pre-diabetes and normoglycaemia to examine a possible association of vitamin D deficiency with pre-diabetes.
Study Design: Case control study.
Place And Duration Of Study: Armed Forces Institute of Pathology, Rawalpindi, from November 2012 to July 2013.
Objective: To study the immunohistochemical expression of vascular endothelial growth factors in urothelial tumours of bladder and its possible association with tumour characteristics and microvessel density.
Methods: The cross-sectional descriptive study was conducted at the Histopathology Department of the Armed Forces Institute of Pathology, Rawalpindi, Pakistan, from July 2011 to December 2012, and comprised cases of non-invasive and invasive urothelial tumours of the bladder. The microvessel density and expression of vascular endothelial growth factors A, C, D were evaluated by immunohistochemistry.
Objective: To evaluate the in vitro effectiveness of multiple breakpoint concentrations of newer antituberculosis agents (Linezolid and Meropenem) against Multi Drug-Resistant Tuberculosis (MDR-TB) isolates.
Study Design: A descriptive cross-sectional study.
Place And Duration Of Study: Microbiology Department, Armed Forces Institute of Pathology (AFIP), Rawalpindi, from September 2011 to August 2013.
Objective: To evaluate the diagnostic efficacy of two rapid methods i.e. Mycobacterium tuberculosis (MTB) Polymerase Chain Reaction (PCR) on Fine Needle Aspiration (FNA) samples by comparing with cytology of respective site sample.
View Article and Find Full Text PDFObjective: To find out the frequency of Extensively Drug Resistant (XDR) and pre-XDR tuberculosis in clinical isolates of Multi-Drug Resistant (MDR) Tuberculosis (TB) by determining the susceptibilities against Levofloxacin and Amikacin (classical second line antituberculosis drugs).
Study Design: Adescriptive cross-sectional study.
Place And Duration Of Study: Microbiology Department, Armed Forces Institute of Pathology (AFIP), Rawalpindi, from September 2011 to August 2013.
Objective: To assess the additional burden of the patients eligible for treatment, based on recommendations on viral load, in the light of 2009 version of AASLD guidelines, as compared to 2004 guidelines and to determine the frequency of HBeAg in chronic HBV carriers.
Study Design: Descriptive cross-sectional study.
Place And Duration Of Study: Virology Department, Armed Forces Institute of Pathology, Rawalpindi, from November 2010 to January 2012.
Objective: To compare the Friedewald and modified Friedewald formulae with direct homogeneous assay for serum lowdensity lipoprotein cholesterol (LDL-C) levels estimation.
Study Design: Cross-sectional study.
Place And Duration Of Study: Armed Forces Institute of Pathology, Rawalpindi, from June to December 2011.