Pharmaceutical technological trends containing flavonoids: a patent review DOI
Ana Maria Santos Oliveira, Anamaria Mendonça Santos, José Adão Carvalho Nascimento Júnior

et al.

Future Medicinal Chemistry, Journal Year: 2025, Volume and Issue: 17(3), P. 363 - 379

Published: Jan. 21, 2025

Flavonoids such as silibinin, hesperetin, and phloretin exhibit well-documented biological activities, including anti-inflammatory, cytoprotective, anticarcinogenic, antioxidant effects. However, their clinical application remains limited due to challenges poor aqueous solubility, low bioavailability, restricted intestinal absorption, which can significantly reduce pharmacological efficacy. This review analyzed patents related innovative pharmaceutical technologies for flavonoids. The analysis used databases from the World Intellectual Property Organization European Patent Office. Following a comprehensive screening process, 38 were selected detailed examination. These highlighted numerous studies on novel formulations, characterizations, proprietary conditions. highlights technologies, nanocapsules, nanoemulsions, solid dispersions, phospholipid carriers, inclusion complexes, microemulsions, other advanced systems, enhance bioactive molecules' water solubility stability. Consequently, these improve permeability absorption through intended administration route, demonstrating potential of flavonoids promising candidates various treatments, particularly when integrated into technologies.

Language: Английский

Flavonoids as Potential Anti-Inflammatory Molecules: A Review DOI Creative Commons
Jameel M. Al-Khayri,

Gandasi Ravikumar Sahana,

Praveen Nagella

et al.

Molecules, Journal Year: 2022, Volume and Issue: 27(9), P. 2901 - 2901

Published: May 2, 2022

Hydroxylated polyphenols, also called flavonoids, are richly present in vegetables, fruits, cereals, nuts, herbs, seeds, stems, and flowers of numerous plants. They possess medicinal properties such as antioxidant, anti-cancer, anti-microbial, neuroprotective, anti-inflammation. Studies show that flavonoids activate antioxidant pathways render an anti-inflammatory effect. inhibit the secretions enzymes lysozymes β-glucuronidase secretion arachidonic acid, which reduces inflammatory reactions. Flavonoids quercetin, genistein, apigenin, kaempferol, epigallocatechin 3-gallate modulate expression activation a cytokine interleukin-1beta (IL-1β), Tumor necrosis factor-alpha (TNF-α), interleukin-6 (IL-6), interleukin-8 (IL-8); regulate gene many pro-inflammatory molecules s nuclear factor kappa-light chain enhancer activated B cells (NF-κB), activator protein-1 (AP-1), intercellular adhesion molecule-1 (ICAM), vascular cell (VCAM), E-selectins; inhibits inducible nitric oxide (NO) synthase, cyclooxygenase-2, lipoxygenase, enzymes. Understanding action provides better treatment options, including coronavirus disease 2019 (COVID-19)-induced inflammation, bowel disease, obstructive pulmonary disorder, arthritis, Alzheimer's cardiovascular atherosclerosis, cancer. This review highlights sources, biochemical activities, role enhancing human health.

Language: Английский

Citations

524

Diabetic retinopathy as the leading cause of blindness and early predictor of cascading complications—risks and mitigation DOI Creative Commons
Martina Kropp, Olga Golubnitschaja, Alena Mazuráková

et al.

The EPMA Journal, Journal Year: 2023, Volume and Issue: 14(1), P. 21 - 42

Published: Feb. 13, 2023

Abstract Proliferative diabetic retinopathy (PDR) the sequel of (DR), a frequent complication diabetes mellitus (DM), is leading cause blindness in working-age population. The current screening process for DR risk not sufficiently effective such that often disease undetected until irreversible damage occurs. Diabetes-associated small vessel and neuroretinal changes create vicious cycle resulting conversion into PDR with characteristic ocular attributes including excessive mitochondrial retinal cell damage, chronic inflammation, neovascularisation, reduced visual field. considered an independent predictor other severe complications as ischemic stroke. A “domino effect” highly cascading DM which early indicator impaired molecular signaling. Mitochondrial health control clinically relevant management, multi-omic tear fluid analysis can be instrumental prognosis prediction. Altered metabolic pathways bioenergetics, microvascular deficits disease, tissue remodelling are focus this article evidence-based targets predictive approach to develop diagnosis treatment algorithms tailored individual cost-effective prevention by implementing paradigm shift from reactive medicine predictive, preventive, personalized (PPPM) primary secondary care management.

Language: Английский

Citations

184

The Role of IL-6 in Cancer Cell Invasiveness and Metastasis—Overview and Therapeutic Opportunities DOI Creative Commons

Magdalena Rašková,

Lukáš Lacina, Zdeněk Kejík

et al.

Cells, Journal Year: 2022, Volume and Issue: 11(22), P. 3698 - 3698

Published: Nov. 21, 2022

Interleukin 6 (IL-6) belongs to a broad class of cytokines involved in the regulation various homeostatic and pathological processes. These activities range from regulating embryonic development, wound healing ageing, inflammation, immunity, including COVID-19. In this review, we summarise role IL-6 signalling pathways cancer biology, with particular emphasis on cell invasiveness metastasis formation. Targeting principal components (e.g., IL-6Rs, gp130, STAT3, NF-κB) is an intensively studied approach preclinical research. It significant translational potential; numerous studies strongly imply remarkable potential inhibitors, especially suppression.

Language: Английский

Citations

123

Seaweed-derived phenolic compounds as diverse bioactive molecules: A review on identification, application, extraction and purification strategies DOI
Abbas Sadeghi, Ali Rajabiyan,

Nafise Nabizade

et al.

International Journal of Biological Macromolecules, Journal Year: 2024, Volume and Issue: 266, P. 131147 - 131147

Published: March 26, 2024

Language: Английский

Citations

32

Anti-breast cancer effects of phytochemicals: primary, secondary, and tertiary care DOI Creative Commons
Alena Mazuráková, Lenka Koklesová, Marek Samec

et al.

The EPMA Journal, Journal Year: 2022, Volume and Issue: 13(2), P. 315 - 334

Published: April 14, 2022

Breast cancer incidence is actually the highest one among all cancers. Overall breast management associated with challenges considering risk assessment and predictive diagnostics, targeted prevention of metastatic disease, appropriate treatment options, cost-effectiveness approaches applied. Accumulated research evidence indicates promising anti-cancer effects phytochemicals protecting cells against malignant transformation, inhibiting carcinogenesis spread, supporting immune system increasing effectiveness conventional therapies, others. Molecular sub-/cellular mechanisms are highly complex affecting several pathways considered potent targets for advanced diagnostics cost-effective treatments. Demonstrated affects, therefore, clinically relevant improving individual outcomes might be applicable to primary (protection initial development), secondary potential disease tertiary (towards cascading complications) care. However, a detailed data analysis essential adapt algorithms individuals' patients' needs. Consequently, concepts patient stratification, prevention, treatments tailored individualized profile instrumental application natural substances improve overall benefiting affected individuals society at large.

Language: Английский

Citations

54

Antioxidants in brain tumors: current therapeutic significance and future prospects DOI Creative Commons
Xuchen Qi, Saurabh Kumar Jha, Niraj Kumar Jha

et al.

Molecular Cancer, Journal Year: 2022, Volume and Issue: 21(1)

Published: Oct. 28, 2022

Brain cancer is regarded among the deadliest forms of worldwide. The distinct tumor microenvironment and inherent characteristics brain cells virtually render them resistant to majority conventional advanced therapies. Oxidative stress (OS) a key disruptor normal homeostasis involved in carcinogenesis different cancers. Thus, antioxidants may inhibit tumorigenesis by preventing OS induced various oncogenic factors. Antioxidants are hypothesized initiation endorsing DNA repair suppressing progression creating an energy crisis for preneoplastic cells, resulting antiproliferative effects. These effects referred as chemopreventive mediated antioxidant mechanism. In addition, minimize chemotherapy-induced nonspecific organ toxicity prolong survival. also support prooxidant chemistry that demonstrate chemotherapeutic potential, particularly at high or pharmacological doses trigger promoting free radical production, which essential activating cell death pathways. A growing body evidence revealed roles exogenous adjuvants their ability reverse chemoresistance. this review, we explain influences endogenous on cancers with reference roles. role metabolic reprogramming influence downstream signaling events suppressor gene mutations critically discussed. Finally, review both pro- anticancer mechanisms molecules killing neoplastic inhibiting recurrence followed treatments. requirements treatment under conditions discussed along reasons behind conflicting outcomes reports. mention influencing factors regulate pharmacology treatment. conclusion, achieve consistent clinical treatments cancers, rigorous mechanistic studies required respect types, forms, stages tumors. concomitant regimens need adequate consideration.

Language: Английский

Citations

51

Significance of flavonoids targeting PI3K/Akt/HIF-1α signaling pathway in therapy-resistant cancer cells – A potential contribution to the predictive, preventive, and personalized medicine DOI Creative Commons
Alena Mazuráková, Lenka Koklesová,

Sandra Hurta Csizmár

et al.

Journal of Advanced Research, Journal Year: 2023, Volume and Issue: 55, P. 103 - 118

Published: March 4, 2023

Cancer management faces multiple obstacles, including resistance to current therapeutic approaches. In the face of challenging microenvironments, cancer cells adapt metabolically maintain their supply energy and precursor molecules for biosynthesis thus sustain rapid proliferation tumor growth. Among various metabolic adaptations observed in cells, altered glucose metabolism is most widely studied. The aberrant glycolytic modification has been associated with cell division, growth, progression, drug resistance. higher rates glycolysis as a hallmark modulated by transcription factor hypoxia inducible 1 alpha (HIF-1α), downstream target PI3K/Akt signaling, deregulated pathway cancer. We provide detailed overview current, primarily experimental, evidence on potential effectiveness flavonoids combat glycolysis-induced conventional targeted therapies. manuscript focuses reducing via affecting PI3K/Akt, HIF-1α (as critical that regulated pathway), key mediators PI3K/Akt/HIF-1α signaling (glucose transporters enzymes). working hypothesis proposes – an attractive application mitigate Phytochemicals represent source promising substances applicable primary, secondary, tertiary care. However, accurate patient stratification individualized profiling crucial steps paradigm shift from reactive predictive, preventive, personalized medicine (PPPM / 3PM). article focused targeting molecular patterns natural provides evidence-based recommendations 3PM relevant implementation.

Language: Английский

Citations

30

Transient Mild Photothermia Improves Therapeutic Performance of Oral Nanomedicines with Enhanced Accumulation in the Colitis Mucosa DOI Open Access

Ya Ma,

Shuangquan Gou,

Zhenhua Zhu

et al.

Advanced Materials, Journal Year: 2023, Volume and Issue: 36(14)

Published: Dec. 13, 2023

The treatment outcomes of oral medications against ulcerative colitis (UC) have long been restricted by low drug accumulation in the mucosa and subsequent unsatisfactory therapeutic efficacy. Here, high-performance pluronic F127 (P127)-modified gold shell (AuS)-polymeric core nanotherapeutics loading with curcumin (CUR) is constructed. Under near-infrared irradiation, resultant P127-AuS@CURs generate transient mild photothermia (TMP; ≈42 °C, 10 min), which facilitates their penetration through colonic mucus favors multiple cellular processes, including cell internalization, lysosomal escape, controlled CUR release. This strategy relieves intracellular oxidative stress, improves wound healing, reduces immune responses polarizing proinflammatory M1-type macrophages to anti-inflammatory M2-type. Upon administration hydrogel-encapsulating plus intestinal intralumen TMP, effects acute chronic UC are demonstrated be superior those a widely used clinical drug, dexamethasone. (+ TMP) elevates proportions beneficial bacteria (e.g., Lactobacillus Lachnospiraceae), whose metabolites can also mitigate symptoms regulating genes associated antioxidation, anti-inflammation, healing. Overall, TMP offers promising approach enhance noninvasive medicines UC.

Language: Английский

Citations

27

Mini-encyclopedia of mitochondria-relevant nutraceuticals protecting health in primary and secondary care—clinically relevant 3PM innovation DOI Creative Commons
Olga Golubnitschaja,

Andrea Kapinová,

Nafiseh Sargheini

et al.

The EPMA Journal, Journal Year: 2024, Volume and Issue: 15(2), P. 163 - 205

Published: April 18, 2024

Despite their subordination in humans, to a great extent, mitochondria maintain independent status but tightly cooperate with the "host" on protecting joint life quality and minimizing health risks. Under oxidative stress conditions, healthy promptly increase mitophagy level remove damaged "fellows" rejuvenating mitochondrial population sending fragments of mtDNA as SOS signals all systems human body. As long metabolic pathways are under systemic control well-concerted together, adaptive mechanisms become triggered increasing protection, activating antioxidant defense repair machinery. Contextually, attributes patho-/physiology instrumental for predictive medical approach cost-effective treatments tailored individualized patient profiles primary (to protect vulnerable individuals again health-to-disease transition) secondary affected disease progression) care. Nutraceuticals naturally occurring bioactive compounds demonstrating health-promoting, illness-preventing, other health-related benefits. Keeping mind health-promoting properties nutraceuticals along therapeutic potential safety profile, there is permanently growing demand application mitochondria-relevant nutraceuticals. Application beneficial only if meeting needs at individual level. Therefore, risk assessment creation pivotal importance followed by adapted nutraceutical sets needs. Based scientific evidence available nutraceuticals, this article presents examples frequent which require protective measures targeted holistic following advanced concepts predictive, preventive, personalized medicine (PPPM/3PM)

Language: Английский

Citations

15

Exploration of tumor growth regression of quinoa and chia oil nanocapsules via the control of PIK3CA and MYC expression, anti-inflammation and cell proliferation inhibition, and their hepatorenal safety in rat breast cancer model DOI Creative Commons
Aida I. El Makawy, Sekena H. Abdel‐Aziem, Shaimaa Mohammed

et al.

Bulletin of the National Research Centre/Bulletin of the National Research Center, Journal Year: 2024, Volume and Issue: 48(1)

Published: Jan. 5, 2024

Abstract Background The second most common cancer in the world is breast cancer. Chemotherapy used to treat cancer, but instances of multidrug resistance, targets that are not selective, and physicochemical issues raise doubts about its efficacy. So, exploration chemopreventive agents from efficient natural sources has been required. chia quinoa seeds have health-promoting activities include cardio-protective, antidiabetic, anticancer effects. Given paramount importance their oils potential bioactivities, this work aimed assess repressive effect oil nanocapsules against mammary tumors rats. Rat models chemically induced were gavaged with for one month. was studied by quantifying TNF-α, assessing gene expression proto-oncogenes (PIK3CA MYC) using qRT-PCR, analyzing cell cycle tissue. Results studies clarified inhibition response associated a reduction TNF-α levels, proliferation capability, motivation apoptosis. Furthermore, nanocapsule management repressed activation MYC PIK3CA genes. As well as modulated liver enzymes kidney function alterations tumor animals. Meanwhile, both oils' do an impact on kidneys healthy Conclusions findings indicate safe can reduce growth, suggesting therapeutic target treatment.

Language: Английский

Citations

10