The risks of artificial intelligence: A narrative review and ethical reflection from an Oral Medicine group.

As a relatively new tool, the use of artificial intelligence (AI) in medicine and dentistry has the potential to significantly transform the healthcare sector. AI has already demonstrated efficacy in medical diagnosis across several specialties, used successfully to detect breast, lung and skin cancer. In Oral Medicine, AI may be applied in a similar fashion, used in the detection and diagnosis of oral cancers and oral potentially malignant diseases. Despite its promise as a transformative diagnostic aid, the use of AI in healthcare presents significant safety, reliability and ethical concerns. There is no formal consensus on the safe and ethical implementation of AI systems in healthcare settings, but the literature converges on several key principles of ethical AI use including transparency, justice and fairness, non-maleficence, responsibility and privacy. This article provides a narrative review of the key ethical issues surrounding AI use in medicine, and reflects on these, providing view-points of a bioethicist and Oral Medicine clinicians from several units.

Prevalence of Dental Abnormalities, Soft Tissue Pathologies and Occlusion Disorders in Patients with High BMI: A Cross-sectional Study.

PURPOSE: The relationship between body mass index (BMI) and oral disorders remains unclear. This study examined the prevalence and types of dental abnormalities and oral mucosal lesions among female students with obesity attending a Taif University sports centre. MATERIALS AND METHODS: This non-interventional cross-sectional study enrolled female students with high BMI from a university sports facility using a convivence sampling method. The participants were divided into three BMI groups. Data were collected using an interview and by clinical oral examination. Prevalence and oral disorder types and possible mechanisms linking BMI and dental development were evaluated. RESULTS: Ultimately, 86 female students with obesity were analysed. The mean BMI was 42.8 kg/m2, indicating high obesity levels. A weak although statistically significant correlation was observed between age and BMI (r=0.27), indicating that older students had higher BMI. A statistically significant association was observed between BMI and dental abnormalities (p0.05). The dental abnormality prevalence increased with BMI, ranging from 37.5% to 40.7% in the ≤40 and >45 kg/m2 groups, respectively. Most participants (66.3%) had oral mucosal lesions, with the highest prevalence among participants in the 40-45 kg/m2 group (71.4%). CONCLUSION: A statistically significant relationship was observed between BMI and dental abnormalities; obesity may negatively affect oral health.

A Novel Technique for Improving Cyclic Behavior of Steel Connections Equipped with Smart Memory Alloys.

Residual drifts are an important measure of post-earthquake functionality in bridges and buildings, and can determine whether the structure remains fit for its intended purpose or not. This study aims at investigating numerically, through finite element (FE) analysis in ABAQUS, the cyclic response of exterior steel I beam-hollow column connection using welded shape memory alloys (SMA) bolts and seat angles. This is followed by validating the numerical model using an accredited experimental data available in the literature through different techniques, (1) SMA bolts, (2) SMA angles, (3) SMA bolts and angles. The parameters investigated included: SMA type, SMA angle thickness, SMA bolt diameter, SMA angle stiffener and SMA angle direction. The cyclic performance of the steel connection was enhanced further by varying the bolt diameter, plate thickness, angle type and direction. The results revealed that the connections equipped with a combination of SMA plates and SMA angles reduced the residual drift by up to 94%, and doubled the self-centering capability compared to conventional steel connections. Moreover, the parametric analysis showed that Fe-based SMA members could be a good alternative to NiTi based SMA members for improving the self-centering capability and reducing the residual drifts of conventional steel connections.

Oral Potentially Malignant Disorders and Oral Cancer in Saudi Arabia: An Epidemiological Review of the Literature.

Background: Oral potentially malignant disorders (OPMDs) are a group of chronic oral mucosal diseases associated with an increased risk of malignant transformation. Multiple studies have investigated the prevalence of these conditions in multiple regions; however, there are limited data about the prevalence of OPMDs in the Kingdom of Saudi Arabia (KSA). This paper aims to review the prevalence of OPMDs in the KSA, to ensure better understanding of the population risk and propose a more standardised approach to the diagnosis and management of this group across the KSA. In addition, this review will discuss the prevalence of oral cancer in the KSA, considering independent risk factors for oral cancer development. Methods: Electronic databases including PubMed, Medline, Medscape, ScienceDirect, StatPearls, BMC Oral Health and the Cochrane Library were searched with the keywords "Oral Potentially Malignant Disorders"; "Saudi Arabia"; and "Oral Cancer". Identified articles were reviewed independently by 2 reviewers against defined inclusion and exclusion criteria. Results: 16 studies were included in this review. The prevalence of OPMDs in KSA varies significantly depending on age, gender, social habits, background disease and dental status. Conclusions: This review highlights the need for up-to-date data on the prevalence, distribution, and characteristics of OPMDs in KSA. The diverse prevalence rates and distinct characteristics of various OPMDs emphasise the necessity for targeted preventive measures. As the data on OPMDs in KSA remains limited, future research efforts should prioritise the establishment of comprehensive epidemiological studies to inform effective public health interventions in this region.

Ratiometric fluorometric determination of sulfide using graphene quantum dots and self-assembled thiolate-capped gold nanoclusters triggered by aluminum.

A ratiometric-based fluorescence emission system was proposed for the determination of sulfide. It consists of blue emissive graphene quantum dots (GQDs) and self-assembled thiolate-protected gold nanoclusters driven by aluminum ion (Al3+@GSH-AuNCs). The two types of fluorophores are combined to form a ratiometric emission probe. The orange emission of Al3+ @GSH-AuNCs at 624 nm was quenched in the presence of sulfide ion owing to the strong affinity between sulfide and Au(I), while the blue GQDs fluorescence at 470 nm remained unaffected. Interestingly, the Al3+@GSH-AuNCs and GQDs were excited under the same excitation wavelength (335 nm). The response ratios (F470/F624) are linearly proportional to the sulfide concentration within the linear range of 0.02-200 µM under the optimal settings, with a limit of detection (S/N = 3) of 0.0064 µM. The proposed emission probe was applied to detect sulfide ions in tap water and wastewater specimens, with recoveries ranging from 95.3% to 103.3% and RSD% ranging from 2.3% to 3.4%, supporting the proposed method's accuracy.

Superelastic Nickel-Titanium (NiTi)-Based Smart Alloys for Enhancing the Performance of Concrete Structures.

Recent advances in materials science have led to the development of smart materials that can continuously adapt to different loading conditions and changing environment to meet the growing demand for smart structural systems. The unique characteristics of superelastic NiTi shape memory alloys (SMAs) have attracted the attention of structural engineers worldwide. SMAs are metallic materials that can retrieve their original shape upon exposure to various temperatures or loading/unloading conditions with minimal residual deformation. SMAs have found increasing applications in the building industry because of their high strength, high actuation and damping capacities, good durability, and superior fatigue resistance. Despite the research conducted on the structural applications of SMAs during the previous decades, the existing literature lacks reviews on their recent uses in building industry such as prestressing concrete beams, seismic strengthening of footing-column connections, and fiber-reinforced concrete. Furthermore, scarce research exists on their performance under corrosive environments, elevated temperatures, and intensive fires. Moreover, the high manufacturing cost of SMA and the lack of knowledge transfer from research to practice are the main obstacles behind their limited use in concrete structures. This paper sheds light on the latest progress made in the applications of SMA in reinforced concrete structures during the last two decades. In addition, the paper concludes with the recommendations and future opportunities associated with expanding the use of SMA in civil infrastructures.

Identifying promising GSK3ß inhibitors for cancer management: a computational pipeline combining virtual screening and molecular dynamics simulations.

Glycogen synthase kinase-3 (GSK3ß), a serine/threonine protein kinase, has been discovered as a novel target for anticancer drugs. Although GSK3ß is involved in multiple pathways linked to the etiology of various cancers, no specific GSK3ß inhibitor has been authorized for cancer therapy. Most of its inhibitors have toxicity effects therefore, there is a need to develop safe and more potent inhibitors. In this study, a library of 4,222 anti-cancer compounds underwent rigorous computational screening to identify potential candidates for targeting the binding pocket of GSK3ß. The screening process involved various stages, including docking-based virtual screening, physicochemical and ADMET analysis, and molecular dynamics simulations. Ultimately, two hit compounds, BMS-754807 and GSK429286A, were identified as having high binding affinities to GSK3ß. BMS-754807 and GSK429286A exhibited binding affinities of -11.9, and -9.8 kcal/mol, respectively, which were greater than that of the positive control (-7.6 kcal/mol). Further, molecular dynamics simulations for 100 ns were employed to optimize the interaction between the compounds and GSK3ß, and the simulations demonstrated that the interaction was stable and consistent throughout the study. These hits were also anticipated to have good drug-like properties. Finally, this study suggests that BMS-754807 and GSK429286A may undergo experimental validation to evaluate their potential as cancer treatments in clinical settings.

Adult Knowledge About Postoperative Complications of Rhinoplasty in the Western Region of Saudi Arabia.

Background Rhinoplasty, a prevalent cosmetic surgical procedure worldwide, is not exempt from associated risks and complications, as with any other surgery. In light of the surging demand for rhinoplasty amongst young adults, it is imperative to acknowledge that the procedure can engender various complications that can be classified as either early or late complications. Examples of early complications include epistaxis and periorbital ecchymosis, while late complications may manifest as enophthalmos or septal perforation. The present study endeavors to gauge the knowledge of rhinoplasty complications among adult residents of the Western region of Saudi Arabia. Methods To achieve the research objectives, a cross-sectional study design was implemented, utilizing a self-administered online questionnaire. The study targeted male and female adults aged 18 years and above residing in the Western region of Saudi Arabia. The questionnaire comprised of 14 items, categorized into socio-demographic and rhinoplasty postoperative complications sections, respectively. Results The study gathered responses from a total of 968 participants, of which 60.95% fell within the age range of 18-30 years. The majority of participants identified as female (77.89%), and Saudi citizens constituted the vast majority of the respondents (96.28%). Among the participants, 22.62% expressed a desire to undergo rhinoplasty, whereas 77.38% indicated no interest in the procedure. Of those who sought rhinoplasty, the majority favored having the surgery performed by a skilled physician (81.74%). Notably, participants exhibited a relatively high level of awareness regarding the postoperative complications of rhinoplasty, with respiratory issues being the most widely recognized complication (66.63%). Conversely, headache, nausea, and vomiting were the least familiar complications (100%). Conclusion The study findings reveal a considerable knowledge gap among adults residing in the Western region of Saudi Arabia concerning rhinoplasty's possible postoperative complications. The results underscore the pressing need to establish comprehensive educational and awareness-raising programs to equip individuals contemplating the procedure with the requisite information to make informed decisions. Future research endeavors could delve into the underlying determinants that drive the desire for rhinoplasty and assess potential interventions geared toward augmenting individuals' comprehension and knowledge of the procedure.

Negative Impacts of Psychiatric Medications on Oral Health: A Literature Review.

Evidence reveals that people with mental illnesses have a greater risk of experiencing oral diseases such as dry mouth and dental caries and have greater oral treatment needs. This is related to multifactorial causes such as factors related to the condition itself, symptoms, side effects of polypharmacy, and a lack of accessibility to dental services. This article aims to provide a summary of the reported prevalence of the most common mental illnesses in Saudi Arabia (SA), such as schizophrenia, obsessive-compulsive disorder (OCD), bipolar disorders, and dementia. The article further aims to review the negative impacts of anti-psychotic medications on oral health and the role of dentists toward people with mental illnesses. PubMed, Scopus, and Google Scholar were searched using the following keywords: special care dentistry, schizophrenia, OCD, bipolar disorder, and dementia. The main inclusion criteria were any studies describing "dental management of patients with mental illnesses" and "dental management of patients treated with anti-psychotic medications." Thematic analysis was used to summarize the findings of the included studies into main headings. Forty-eight articles/studies discussed dentistry, people with mental illnesses, and/or the negative impacts of psychotic medication on oral health. All studies were published between 1991 and 2021. In SA, the number of people with mental illnesses is increasing. Therefore, it is crucial for the dental team to understand the negative impacts of anti-psychotic medications on oral health, such as dry mouth and the increased risk of dental caries. This necessitates the need for regular dental visits and patient education on how they can mitigate the side effects of anti-psychotic medications on oral and general health.

Natural Reno-Protective Agents against Cyclosporine A-Induced Nephrotoxicity: An Overview.

CA (cyclosporine A) is a powerful immunosuppressing agent that is commonly utilized for treating various autoimmune illnesses and in transplantation surgery. However, its usage has been significantly restricted because of its unwanted effects, including nephrotoxicity. The pathophysiology of CA-induced kidney injury involves inflammation, apoptosis, tubular injury, oxidative stress, and vascular injury. Despite the fact that exact mechanism accountable for CA's effects is inadequately understood, ROS (reactive oxygen species) involvement has been widely proposed. At present, there are no efficient methods or drugs for treating CA-caused kidney damage. It is noteworthy that diverse natural products have been investigated both in vivo and in-vitro for their possible preventive potential in CA-produced nephrotoxicity. Various extracts and natural metabolites have been found to possess a remarkable potential for restoring CA-produced renal damage and oxidative stress alterations via their anti-apoptosis, anti-inflammatory, and antioxidative potentials. The present article reviews the reported studies that assess the protective capacity of natural products, as well as dietary regimens, in relation to CA-induced nephrotoxicity. Thus, the present study presents novel ideas for designing and developing more efficient prophylactic or remedial strategies versus CA passive influences.

Aspergillus ochraceus: Metabolites, Bioactivities, Biosynthesis, and Biotechnological Potential.

Fungus continues to attract great attention as a promising pool of biometabolites. Aspergillus ochraceus Wilh (Aspergillaceae) has established its capacity to biosynthesize a myriad of metabolites belonging to different chemical classes, such as isocoumarins, pyrazines, sterols, indole alkaloids, diketopiperazines, polyketides, peptides, quinones, polyketides, and sesquiterpenoids, revealing various bioactivities that are antimicrobial, cytotoxic, antiviral, anti-inflammatory, insecticidal, and neuroprotective. Additionally, A. ochraceus produces a variety of enzymes that could have variable industrial and biotechnological applications. From 1965 until June 2022, 165 metabolites were reported from A. ochraceus isolated from different sources. In this review, the formerly separated metabolites from A. ochraceus, including their bioactivities and biosynthesis, in addition, the industrial and biotechnological potential of A. ochraceus are highlighted.

Advances in Fungal Phenaloenones-Natural Metabolites with Great Promise: Biosynthesis, Bioactivities, and an In Silico Evaluation of Their Potential as Human Glucose Transporter 1 Inhibitors.

Phenaloenones are structurally unique aromatic polyketides that have been reported in both microbial and plant sources. They possess a hydroxy perinaphthenone three-fused-ring system and exhibit diverse bioactivities, such as cytotoxic, antimicrobial, antioxidant, and anti-HIV properties, and tyrosinase, α-glucosidase, lipase, AchE (acetylcholinesterase), indoleamine 2,3-dioxygenase 1, angiotensin-I-converting enzyme, and tyrosine phosphatase inhibition. Moreover, they have a rich nucleophilic nucleus that has inspired many chemists and biologists to synthesize more of these related derivatives. The current review provides an overview of the reported phenalenones with a fungal origin, including their structures, sources, biosynthesis, and bioactivities. Moreover, more than 135 metabolites have been listed, and 71 references have been cited. SuperPred, an artificial intelligence (AI) webserver, was used to predict the potential targets for selected phenalenones. Among these targets, we chose human glucose transporter 1 (hGLUT1) for an extensive in silico study, as it shows high probability and model accuracy. Among them, aspergillussanones C (60) and G (60) possessed the highest negative docking scores of -15.082 and -14.829 kcal/mol, respectively, compared to the native inhibitor of 5RE (score: -11.206 kcal/mol). The MD (molecular dynamics) simulation revealed their stability in complexes with GLUT1 at 100 ns. The virtual screening study results open up a new therapeutic approach by using some phenalenones as hGLUT1 inhibitors, which might be a potential target for cancer therapy.

Absent right internal carotid associated with posterior cerebral artery aneurysm: A case report.

Introduction: and importance: An uncommon condition is congenital unilateral agenesis of the internal carotid artery (ICA). Most instances are asymptomatic due to adequate collateral circulation via the circle of Willis, but individuals might potentially manifest (or show) ischemic or aneurysmal dilatation hemorrhagic cerebrovascular lesions. The bony carotid canal must be absent from distinguishing this abnormality from chronic ICA blockage. Neuroradiologists must be aware of this condition since these patients have a higher risk of developing numerous intracranial diseases. Case presentation: This report focuses on the case of 39 years male with an absent right internal carotid artery with posterior cerebral artery aneurism whose main symptoms were on and off headaches. In a discussion that includes demographic characteristics, clinical manifestations, radiologic findings, and an assessment of the risks associated with ICA agenesis. Conclusion: Congenital agencies absence of carotid artery is rare variant anatomy although most of the time they are asymptomatic, it is known to increase the risk of aneurism and therefore, they need screening and close follow up.

Gender Differences in the Attitudes and Management of People with Obesity in Saudi Arabia: Data from the ACTION-IO Study.

Purpose: Several studies have investigated gender differences in various obesity-related outcomes. Females were found to have more accurate weight perception and reported more frequency of attempted weight loss. The objective of this study was to assess gender differences in the attitudes and management of people with obesity (PwO) in Saudi Arabia using data from the ACTION-IO study. Patients and Methods: A survey was conducted in Saudi Arabia in June and July 2018 on adults with obesity (based on self-reported body mass index of ≥30 kg/m2). Results: A total of 1000 people with obesity completed the survey; 565 (56.5%) were male (mean age of 36.9 years and mean BMI of 33.5 kg/m2) and 435 (43.5%) were female (mean age of 36.3 years and mean BMI of 34.5 kg/m2). The two most reported motivations for wanting to lose weight for both groups were to improve appearance (38%) and to have more energy (35%). Females were more likely to trust their health-care provider (HCP) advice about weight management when compared to males (87% females, 82% males, p = 0.059) and were more likely to have concerns regarding long-term safety associated with prescription weight loss medications (65% female versus 59% males, p = 0.043). On the other hand, males were more likely to seek their physician to prescribe weight loss medication if they hear of a new medication (55% males versus 46% females, p = 0.014), and more to believe that there are good options available for weight loss medications (74% males versus 67% females, p = 0.040). Also, more males prefer to take weight loss medications than to have a weight loss surgery (65% males, 59% females, p = 0.054). Conclusion: Overall, this study increases our understanding on the attitudes of both females and males towards the management of weight loss and opens the discussion for gender-specific weight loss interventions.

Design, synthesis, antiproliferative activity, estrogen receptors binding affinity of C-3 pregnenolone-dihydropyrimidine derivatives for the treatment of breast cancer.

Breast cancer (BCa) is very common malignancy and globally, has become the second leading cause of cancer death among women. For the treatment of BCa, estrogen receptors-alpha (ERα) has proven to be a therapeutic target. In continuation of our previous reported dihydropyrimidine-based pregnenolone derivatives, we modified at C-3 hydroxyl group. Structural architecture of estrogen receptors (ER) with excellent ER binding affinity was used for modification. MTT assay was used to evaluate the synthesized steroidal analogs for their antiproliferative activities against ER-positive MCF-7, ER-negative MDA-MB-231 (ER-) breast cancer cells and non-cancerous HEK-293 cells. Structure activity relationship (SAR) studies revealed that diethanolamine containing pregnenolone derivatives showed significant cytotoxicity against ER + MCF-7 and also showed good binding affinity with ERα and are relatively safe against HEK-293 cell model. Docking studies demonstrated that high binding affinity of diethanolamine analogs is due to their binding interaction with key amino acid residues present in the binding site of Erα.

Extracellular ATP targets Arabidopsis RIBONUCLEASE 1 to suppress mycotoxin stress-induced cell death.

Extracellular ATP is a purinergic signal with important functions in regulating plant growth and stress-adaptive responses, including programmed cell death. While signalling events proximate to receptor activation at the plasma membrane have been characterised, downstream protein targets and the mechanism of cell death activation/regulation are unknown. We designed a proteomic screen to identify ATP-responsive proteins in Arabidopsis cell cultures exposed to mycotoxin stress via fumonisin B1 (FB1) application. Arabidopsis RIBONUCLEASE 1 (RNS1) was identified by the screen, and transgenic plants overexpressing native RNS1 showed greater susceptibility to FB1, while a gene knockout rns1 mutant and antisense RNS1 transgenic plants were resistant to FB1-induced cell death. Native RNS1 complemented rns1 mutants and restored the cell death response to FB1, while a catalytically inactive version of the ribonuclease could not. The FB1 resistance of salicylic acid (SA)-depleted nahG-expressing plants was abolished by transformation with native RNS1, but not the catalytically dead version. The mechanism of FB1-induced cell death is activation of RNS1-dependent RNA cleavage, which is blocked by ATP via RNS1 suppression, or enhanced by SA through induction of RNS1 expression. Our study reveals RNS1 as a previously unknown convergence point of ATP and SA signalling in the regulation of stress-induced cell death.

Hematocolpos: An Unusual Cause of Right Iliac Fossa Pain.

Acute appendicitis is the most frequent indication for emergency abdominal surgery in childhood. Despite being a common condition, the diagnosis of acute appendicitis can be challenging. Ultrasound examination remains the imaging tool of choice for the diagnosis of acute appendicitis. We report the case of a nine-year-old girl who presented with acute abdominal pain in the right lower quadrant accompanied by nausea and vomiting. Physical examination revealed right iliac fossa rebound tenderness. Ultrasound examination showed a dilated blind-ended structure in the right iliac fossa conferring the diagnosis of acute appendicitis. The patient underwent a CT scan which made the diagnosis of imperforate hymen with hematocolpos. The patient underwent hymenotomy and her symptoms showed complete resolution. Imperforate hymen with hematocolpos is a rare congenital genital tract anomaly. The case highlights the importance of appropriate genital examination in pediatric patients. In the present case, the patient might have undergone an unnecessary abdominal surgery if the correct diagnosis was not established.

Structural Modification, In Vitro, In Vivo, Ex Vivo, and In Silico Exploration of Pyrimidine and Pyrrolidine Cores for Targeting Enzymes Associated with Neuroinflammation and Cholinergic Deficit in Alzheimer's Disease.

To obtain a multipotent framework that can target simultaneously COX-2, 5-LOX, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE) to treat neuroinflammation, a series of derivatives containing pyrimidine and pyrrolidine cores were rationally synthesized and evaluated. Pyrazoline-pyrimidine hybrid (23g), (3-acetylcoumarin derivative of pyrrolidin-1-yl)benzenesulfonamide (27), and tacrine derivatives of (pyrrolidin-1-yl)benzenesulfonamide (31, 38) displayed excellent in vitro COX-2 inhibition having IC50 value in the nanomolar range. Tacrine-pyrrolidine hybrids 36 and 38, and tacrine-pyrimidine hybrid (46) emerged as the most potent eeAChE inhibitors with IC50 values of 23, 16, and 2 nM, respectively. However, compounds 27, 31, and 38 possessed excellent simultaneous and balanced inhibitory activity against all of the four tested targets and thus emerged as optimal multipotent hybrid compounds among all of the synthesized series of the compounds. In the ex vivo, transgenic animal models treated with compounds 36 and 46 displayed a significant decline in both AChE and BChE potentials in the hippocampus and cortical tissues. In anti-inflammatory activities, animals treated with compounds 36 and 46 displayed a significant % inhibition of edema induced by carrageenan and arachidonic acid. Biochemical analysis and histopathological examination of mice liver indicate that tacrine derivatives are devoid of hepatotoxicity and neurotoxicity against SH-SY5Y neuroblastoma cell lines. In vivo acute toxicity study showed the safety of synthesized compounds up to 1000 mg/kg dose. The inhibitory manner of interaction of these potent drugs on all of the studied in vitro targets was confirmed by molecular docking investigations.

Cytotoxicity, anti-angiogenic, anti-tumor and molecular docking studies on phytochemicals isolated from Polygonum hydropiper L.

BACKGROUND: According to the recent global cancer statistics, breast cancer is the leading cause of deaths among women with 2.3 million new cases globally. Likewise, cervical cancer is also among the leading causes of mortality among women. Polygonum hydropiper is traditionally known for its cytotoxic effects and several bioactive cytotoxic compounds were isolated from it. This study was aimed to isolate potential anticancer compounds from its most potent fractions and evaluate their anticancer potentials. METHODS: Based on our earlier studies, active fractions including chloroform and ethyl acetate were subjected to column chromatography for isolation of compounds. Chemical structures of isolated compounds were confirmed via 1H NMR, 13C NMR, mass spectrometry. Purified compounds were tested for cytotoxicity against breast cancer cells (MCF-7), cervical cancer cells (HeLA) and NIH/3T3 fibroblasts cells cultures using MTT assy. Anti-angiogenic potentials of isolated compounds were evaluated via chorioallantoic membrane assay. Anti-tumor studies were done using Agrobacterium tumefaciens induced potato tumor assay. Furthermore, to understand the binding modes of Isolated compounds, molecular docking was performed against EGFR, HER2 and VEGFR using MOE as docking software. RESULTS: Two bioactive compounds PH-1 (4-methyl-5-oxo-tetrahydrofuran-3-yl acetate) and PH-2 (methyl 4-hydroxy-3-methoxybenzoate) were purified from the active fractions. In cytotoxicity studies, PH-1 exhibited highest cytotoxicity against HeLA cells with 87.50% lethality at 1 mgmL-1 concentration and LD50 of 60 µgmL-1. Likewise, PH-2 showed 82.33% cytotoxicity against HeLA cells with LD50 of 160 µgmL-1. Similarly, PH-1 and PH-2 exhibited LD50 of 170 and 380 µgmL-1 respectively. Moreover, PH-1 and PH-2 were also very potent cytotoxic compounds against NIH/3T3 cells with 81.45 and 85.55% cytotoxicity at 1 mgL-1 concentration and LD50 of 140 and 58 µgL-1 respectively. Isolated compounds exhibited considerable anti-angiogenic potentials with IC50 of 340 and 500 µgL-1 respectively for PH-1 and PH-2. In anti-tumor assay, PH-1 and PH-2 exhibited 81.15 and 76.09% inhibitions with LD50 of 340 and 550 µgL-1 respectively. Both compounds selectively binds with EGFR and HER2 receptors with low binding energies. Both compounds exhibited stronger interactions with VEGFR through binding pocket residues Lys868, Val916 and Asp1046. CONCLUSIONS: Both compounds cause considerable cytotoxicity against cancer cells. The anti-angiogenic and anti-tumor results suggests additional tumor suppressive properties. Docking analysis suggests that these compound not only has the ability to bind to EGFR and HER2 but also equally binds to VEGFR and may act as potential anti-angiogenic agents.

Superbranched polyglycerol nanostructures as drug delivery and theranostics tools for cancer treatment.

Hyperbranched polymers (HBPs), such as hyperbranched polyglycerols (HPGs) with a dendritic configuration, have been recognized for their excellent biocompatibility and multifunctionalization. HPGs have been studied for use in the delivery diagnostic, imaging and therapeutic molecules in the area of nanobiomedicine. They show superior characteristics to linear polymers and dendrimers, such as compact structure, a simple manufacturing process with easy functionalization ability, low viscosity, and high stability. Owing to these advantages, HPGs are now considered promising carriers for drug delivery, diagnostics, imaging, and theranostics applications for cancer treatment. In this review, we also discuss safety aspects of HPG-based nanoformulations in various animal models and the clinical translation status of such polymers for real-time applications.