Kaempferol, a natural flavonoid present in several plants, possesses a wide range of therapeutic properties such as antioxidant, anticancer, and anti‐inflammatory. It has a significant role in ...reducing cancer and can act as a therapeutic agent in the treatment of diseases and ailments such as diabetes, obesity, cardiovascular diseases, oxidative stress, asthma, and microbial contamination disorders. Kaempferol acts through different mechanisms: It induces apoptosis (HeLa cervical cancer cells), decreases cell viability (G2/M phase), downregulates phosphoinositide 3‐kinase (PI3K)/AKT (protein kinase B) and human T‐cell leukemia/lymphoma virus‐I (HTLV‐I) signaling pathways, suppresses protein expression of epithelial‐mesenchymal transition (EMT)‐related markers including N‐cadherin, E‐cadherin, Slug, and Snail, and metastasis‐related markers such as matrix metallopeptidase 2 (MMP‐2). Accordingly, the aim of the present review is to collect information pertaining to the effective role of kaempferol against various degenerative disorders, summarize the antioxidant, anti‐inflammatory, anticancer, antidiabetic, and antiaging effects of kaempferol and to review the progress of recent research and available data on kaempferol as a protective and chemotherapeutic agent against several ailments.
Chrysin is a promising phytochemical that is categorized under the class of flavonoids based on its chemical structure. Naturally, it is widely present in propolis, honey, passion fruit, and even in ...mushrooms and other plant sources, whereas its synthetic counterparts are also being employed for pharmacological purposes. It has widely been employed in treatment of various degenerative disorders and provides cytotoxic and anti-inflammatory functions. Its antioxidant and disease preventing abilities are attributed to its structural diversity arising in ring-A and absence of oxygenation in B and C ring. In this review, the scientific studies are being reported emphasizing benefits and its allied health claims on chrysin in numerous metabolic malfunctions.
Graphical abstract of chrysin sources and its health claims Display omitted
Three novel Schiff bases, namely
N
-(4-((4-((phenylimino)methyl)phenoxy)methoxy)benzylidene)benzenamine (
UA
),
N
...-(3-methoxy-4-((2-methoxy-4-((phenylimino)methyl)phenoxy)methoxy)benzylidene)benzenamine (
UB
), and
N
-(3-ethyl-4-((2-ethyl-4-((phenylimino)methyl)phenoxy)methoxy)benzylidene)benzenamine (
UC
), were synthesized and their structures were elucidated through diverse spectroscopic techniques such as FT-IR, GC-MS,
1
H NMR and
13
C NMR. The corrosion inhibition effect of these Schiff bases on aluminum alloy AA2219-T6 in acidic medium was explored using weight loss, Tafel polarization, and electrochemical impedance spectroscopy. Theoretical quantum chemical calculations using density functional theory were employed to determine the adsorption site. It was found that inhibition efficiencies increase with an increase in the inhibitor concentration. Tafel plots showed that these Schiff bases function as mixed inhibitors. Adsorption of the Schiff bases on aluminum followed the Langmuir adsorption isotherm and the value of
showed a dominant chemical mechanism. FT-IR and SEM techniques were used to investigate the surface morphology. The compounds showed a substantial corrosion inhibition for aluminum alloy in 0.1 M HCl at 298 K.
UB
and
UC
exhibited superior anticorrosion efficiency compared to
UA
originating from the electron-donating methoxy and ethoxy group substitutions, respectively. There was found to be good correlation between molecular structure and inhibition efficiencies.
Novel Schiff bases characterized through spectroscopic techniques and used as anticorrosive agents for aluminium alloy acidic medium. Electrochemical techniques and DFT studies were used to study inhibition effect and molecular interactions.
Penicillium produces a wide range of structurally diverse metabolites with significant pharmacological impacts in medicine and agriculture. For the first time, a complete metabolome of Penicillium ...claviforme (P. claviforme) (FBP-DNA-1205) was studied alongside pharmacological research in this study.
The metabolic profile of P. claviforme fermented on Potato Dextrose Broth (PDB) was investigated in this work. The complete metabolomics studies of fungus were performed using GC-MS and LC-MS-QTOF techniques. An in vitro model was utilised to study the cytotoxic and antioxidant activities, while an in vivo model was employed to investigate the antinociceptive and acute toxicity activities. Molecular Operating Environment (MOE) software was used for molecular docking analysis.
GC-MS study showed the presence of alkanes, fatty acids, esters, azo and alcoholic compounds. Maculosin, obtain, phalluside, quinoline, 4,4'-diaminostilbene, funaltrexamine, amobarbital, and fraxetin were among the secondary metabolites identified using the LC-MS-QTOF technique. The n-hexane fraction of P. claviforme displayed significant cytotoxic activity in vitro, with an LD50 value of 92.22 µgml
−1
. The antinociceptive effects in vivo were dose-dependent significantly (p < .001). Interestingly, during the 72 h of investigation, no acute toxicity was demonstrated. In addition, a docking study of tentatively identified metabolites against the inflammatory enzyme (COX-2) supported the antinociceptive effect in an in silico model.
Metabolic profile of P. claviforme shows the presence of biologically relevant compounds in ethyl acetate extract. In addition, P. claviforme exhibits substantial antioxidant and cytotoxic activities in an in vitro model as well as antinociceptive activity in an in vivo model. The antinociceptive action is also supported by a molecular docking study. This research has opened up new possibilities in the disciplines of mycology, agriculture, and pharmaceutics.
Key messages
The first time explored complete metabolome through GC-MS and LC-MS-QTOF.
Both in vivo & in vitro pharmacological investigation of P. claviforme.
In silico molecular docking of LC-MS-QTOF metabolites.
•We construct a Heterogeneous Bibliographic Network, which exploits semantics among the network objects.•We propose a GAN-based network embedding model to address the network sparsity problem.•We ...propose a citation recommendation model to produce personalized results corresponding to researchers' preferences.•We conduct extensive experiments on two real-world datasets and prove the significance of the proposed model.
The variety and plethora of research papers available on the Web motivated researchers to propose models that could assist users with personalized citation recommendations. In recent years, citation recommendation models using Network Representation Learning (NRL) methods have shown promising results. Nevertheless, existing NRL-based models are limited in terms of exploiting semantic relations and contextual information between the objects of bibliographic papers’ networks. Additionally, these models cannot adequately explore the structure of heterogeneous information networks, topical relevance, and relevant semantics. Consequently, they suffer from network sparsity and inadequate personalization problems. To overcome these shortcomings, we present a network embedding model termed as Global Citation Recommendation employing Generative Adversarial Network (GCR-GAN). The proposed model exploits the Heterogeneous Bibliographic Network (HBN) to generate personalized citation recommendations. In particular, the proposed model utilizes semantic relations corresponding to the objects of the heterogeneous bibliographic network and captures network structure proximity employing the Scientific Paper Embeddings using Citation-informed Transformers (SPECTER) and Denoising Auto-encoder networks to learn semantic-preserving graph representations. Compared to baseline models, the recommendations generated by our model over the DBLP and ACM datasets prove that it outperforms baseline methods by gaining almost 11% and 12% improvement in terms of Mean Average Precision (MAP) and Normalized Discounted Cumulative Gain (nDCG) metrics, respectively. Furthermore, we analyzed the effectiveness of the proposed model considering network sparsity issue, where our model gains almost 7% better recall@100 score against the second-best counterpart.
Recently, numerous novel bioactive fungal metabolites have been identified that possess broad therapeutic activities including anti-inflammatory, antibiotic, antioxidant, and antitumor. The fungal ...mycochemicals as well as extracts have increased the interest of the scientific community in drug discovery research through a combination approach such as, molecular metabolic, pharmacological and computational techniques. Therefore, the natural fungus Aspergillus ficuum (A. ficuum) (FCBP-DNA-1266) was selected for metabolic and pharmacological profiling in this study.
The metabolic profile of A. ficuum was explored for the first time and revealed the presence of bioactive compounds such as choline sulfate, noruron, hydroxyvittatine, aurasperone D, cetrimonium, kurilensoside, heneicosane, nonadecane and eicosane. Similarly, a pharmacological screen of A. ficuum was performed for the first time in in vivo and in vitro models. Interestingly, both the ethyl acetate and n-hexane fractions of A. ficuum were found to be more active against Bacillus subtilis among five tested bacteria with their zone of inhibition (ZOI) values of 21.00 mm ±1.00 and 23.00 mm ±1.00, at a concentration of 150 μgmL
respectively. Similarly, a significant decrease (P<0.001) and (P<0.01) in paw edema was observed in A. ficuum-treated animals at doses of 50 and 150 mgkg
, respectively, reflecting its potent anti-inflammatory effect. Furthermore, the docking results supported the antibacterial and anti-inflammatory effects of A. ficuum. In addition, the crude extract demonstrated no acute toxicity and the highest percent radical scavenging was recorded for both n-hexane and ethyl acetate extracts.
The metabolic profile of A. ficuum indicated the presence of biological relevant compounds. A. ficuum extract exhibited potent antibacterial and anti-inflammatory effects supported by docking results. Furthermore, A. ficuum extract demonstrated the highest percentage of radical scavenging activity along with no acute toxicity.
Abstract
Left ventricular thrombus (LVT) is associated with a significant risk of ischemic stroke (IS) and peripheral embolization. Societal guidelines recommend the use of warfarin, with direct oral ...anticoagulants (DOACs) only for patients unable to tolerate warfarin. We studied the natural history of LVT with anticoagulation (AC) with emphasis on comparing warfarin and DOAC use. In this single center study, we identified patients with a confirmed LVT. Type and duration of anticoagulation, INR levels and clinical outcomes (bleeding, ischemic stroke or peripheral embolization, and thrombus resolution) were recorded. LVT was confirmed in a total of 110 patients. Mean age was 59
+
14 years. 79% were men. Underlying etiology was chronic ischemic cardiomyopathy in 58%, non-ischemic cardiomyopathy in 23%. AC was started in 96 (87%) patients. At 1 year follow up, 11 patients (10%) had a stroke while on any AC (2 had hemorrhagic stroke and 9 had IS). Of those with IS, 7 were on warfarin (71% of those had subtherapeutic INR) and 2 patients on DOACs had IS. The 1-year risk of any stroke was 15% in warfarin group (12% risk of ischemic stroke) compared to 6% in the DOACs group (
p
= 0.33). 37 (63%) patients on warfarin and 18 (53%) on DOACs had resolution of thrombus (
p
= 0.85). One-year risk of stroke with LVT is high (10%) even with AC. Most patients IS on warfarin had subtherapeutic INR. There was no statistical difference in stroke risk or rate of thrombus resolution between warfarin and DOACs treated patients.
Berberine (BBR), a potential bioactive agent, has remarkable health benefits. A substantial amount of research has been conducted to date to establish the anticancer potential of BBR. The present ...review consolidates salient information concerning the promising anticancer activity of this compound. The therapeutic efficacy of BBR has been reported in several studies regarding colon, breast, pancreatic, liver, oral, bone, cutaneous, prostate, intestine, and thyroid cancers. BBR prevents cancer cell proliferation by inducing apoptosis and controlling the cell cycle as well as autophagy. BBR also hinders tumor cell invasion and metastasis by down-regulating metastasis-related proteins. Moreover, BBR is also beneficial in the early stages of cancer development by lowering epithelial-mesenchymal transition protein expression. Despite its significance as a potentially promising drug candidate, there are currently no pure berberine preparations approved to treat specific ailments. Hence, this review highlights our current comprehensive knowledge of sources, extraction methods, pharmacokinetic, and pharmacodynamic profiles of berberine, as well as the proposed mechanisms of action associated with its anticancer potential. The information presented here will help provide a baseline for researchers, scientists, and drug developers regarding the use of berberine as a promising candidate in treating different types of cancers.
Abstract
Serious human health impacts have been observed worldwide due to several life-threatening diseases such as cancer, candidiasis, hepatic coma, and gastritis etc. Exploration of nature for the ...treatment of such fatal diseases is an area of immense interest for the scientific community. Based on this idea, the genus
Aspergillus
was selected to discover its hidden therapeutic potential. The genus
Aspergillus
is known to possess several biologically active compounds. The current research aimed to assess the biological and pharmacological potency of the extracts of less-studied
Aspergillus ficuum
(FCBP-DNA-1266) (
A. ficuum
) employing experimental and bioinformatics approaches. The disc diffusion method was used for the antifungal investigation, and the MTT assay was performed to assess the anticancer effects. Mice were employed as an in vivo
model
to evaluate the antispasmodic effects. A standard spectrophotometric technique was applied to gauge the urease inhibitory activity. The antifungal studies indicate that both n-hexane and ethyl acetate extracts were significantly active against
Candida albicans
(
C. albicans
) with their zone of inhibitions (ZOI) values reported as 19 ± 1.06 mm and 25 ± 0.55 mm, respectively at a dose of 30 µg.mL
−1
. In vitro cytotoxicity assay against HeLa, fibroblast 3T3, prostate PC3, and breast MCF-7 cancer cell lines was performed. The ethyl acetate extract of
A. ficuum
was found to be significantly active against MCF-7 with its IC
50
value of 43.88 µg.mL
−1
. However, no substantial effects on the percent cell death of HeLa cancer cell lines were observed. In addition, the
A. ficuum
extracts also inhibited the urease enzyme compared to standard thiourea. The antispasmodic activity of
A. ficuum
extract was assessed by an in vivo model and the results demonstrated promising activity at 150 mg.kg
−1
. Molecular docking results also supported the antifungal, anticancer, and antiurease potency of
A. ficuum
extract. Overall, the results display promising aspects of
A. ficuum
extract as a future pharmacological source.
Several reviews have been published on Artemisia's derived natural products, but it is the first attempt to review the chemistry and pharmacology of more than 80 alkaloids and allied nitrogen ...compounds obtained from various Artemisia species (covering the literature up to June 2018). The pharmacological potential and unique skeleton types of certain Artemisia's alkaloids provoke the importance of analyzing Artemisia species for bioactive alkaloids and allied nitrogen compounds. Among the various types of bioactive Artemisia's alkaloids, the main classes were the derivatives of rupestine (pyridine–sesquiterpene), lycoctonine (diterpene), pyrrolizidine, purines, polyamine, peptides, indole, piperidine, pyrrolidine, alkamides, and flavoalkaloids. The rupestine derivatives are Artemisia's characteristic alkaloids, whereas the rest are common alkaloids found in the family Asteraceae and chemotaxonomically links the genus Artemisia with the tribes Anthemideae. The most important biological activities of Artemisia's alkaloids are including hepatoprotective, local anesthetic, β‐galactosidase, and antiparasitic activities; treatment of angina pectoris, opening blocked arteries, as a sleep‐inducing agents and inhibition of HIV viral protease, CYP450, melanin biosynthesis, human carbonic anhydrase, 3H‐AEA metabolism, kinases, and DNA polymerase β1. Some of the important nitrogen metabolites of Artemisia include pellitorine, zeatin, tryptophan, rupestine, and aconitine analogs, which need to be optimized and commercialized further.
A review on the chemistry and pharmacology of alkaloids and allied nitrogen compounds from Artemisia is presented for the first time, covers the literature up to June 2018.
The structures of more than 80 alkaloids including the derivatives of rupestine, lycoctonine, pyrrolizidine, purine, indole, polyamine, peptides, alkamides, piperidine, pyrrolidine, ceramide/cerebroside, aromatic/non‐aromatic amines, benzodiazepines, flavoalkaloids, quinazoline, piperazine, pyrazine, pyridine, pyrrole, and 1,4‐diaza‐2,5‐dioxobicyclo4.3.0nonane are explained.
Inhibition of HIV viral protease, melanin biosynthesis, and anti‐parasitic bio‐activities is associated with Artemisia's nitrogen metabolites.
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