Accumulating evidence has demonstrated that cancer stem cells (CSCs) play an essential role in tumor progression and reoccurrence and drug resistance. Multiple signaling pathways have been revealed ...to be critically participated in CSC development and maintenance. Emerging evidence indicates that numerous chemopreventive compounds, also known as nutraceuticals, could eliminate CSCs in part via regulating several signaling pathways. Therefore, in this review, we will describe the some natural chemopreventive agents that target CSCs in a variety of human malignancies, including soy isoflavone, curcumin, resveratrol, tea polyphenols, sulforaphane, quercetin, indole-3-carbinol, 3,3′-diindolylmethane, withaferin A, apigenin, etc. Moreover, we discuss that eliminating CSCs by nutraceuticals might be a promising strategy for treating human cancer via overcoming drug resistance and reducing tumor reoccurrence.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NLZOH, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UILJ, UL, UM, UPCLJ, UPUK, ZAGLJ, ZRSKP
Leishmaniasis is a parasitic disease and categorised as a neglected tropical disease (NTD). Each year, between 70,0000 and 1 million new cases are believed to occur. There are approximately 90 ...sandfly species which can spread the Leishmania parasites (over 20 species) causing 20,000 to 30,000 death per year. Currently, leishmaniasis has no specific therapeutic treatment available. The prescribed drugs with several drawbacks including high cost, challenging administration, toxicity, and drug resistance led to search for the alternative treatment with less toxicity and selectivity. Introducing the molecular features like that of phytoconstituents for the search of compounds with less toxicity is another promising approach. The current review classifies the synthetic compounds according to the core rings present in the natural phytochemicals for the development of antileishmanial agents (2020–2022). Considering the toxicity and limitations of synthetic analogues, natural compounds are at the higher notch in terms of effectiveness and safety. Synthesized compounds of chalcones (Compound 8; IC50: 0.03 μM, 4.7 folds more potent than Amphotericin B; IC50: 0.14 μM), pyrimidine (compound 56; against L. tropica; 0.04 μM and L. infantum; 0.042 μM as compared to glucantime: L. tropica; 8.17 μM and L. infantum; 8.42 μM), quinazoline and (compound 72; 0.021 μM, 150 times more potent than miltefosine). The targeted delivery against DHFR have been demonstrated by one of the pyrimidine compounds 62 with an IC50 value of 0.10 μM against L. major as compared to the standard trimethoprim (IC50: 20 μM). The review covers the medicinal importance of antileishmanial agents from synthetic and natural sources such as chalcone, pyrazole, coumarins, steroids, and alkaloidal-containing drugs (indole, quinolines, pyridine, pyrimidine, carbolines, pyrrole, aurones, and quinazolines). The efforts of introducing the core rings present in the natural phytoconstituents as antileishmanial in the synthetic compounds are discussed with their structural activity relationship. The perspective will support the medicinal chemists in refining and directing the development of novel molecules phytochemicals-based antileishmanial agents.
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•The marketed antileishmanial drugs are associated with toxicity and resistance.•Natural products are promising in treating the leishmanial suffering without the toxic side effects.•Recent developments of natural phytochemicals guided synthesis of potent antileishmanial drugs.•SAR of the different synthesized derivatives to exhibit antileishmanial activity are discussed.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NLZOH, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UILJ, UL, UM, UPCLJ, UPUK, ZAGLJ, ZRSKP
Abstract Natural products represent a rich source for the discovery and development of cancer preventive and anticancer drugs. Nearly, 80% of all drugs approved by the United States Food and Drug ...Administration during the last three decades for cancer therapy are either natural products per se or are based thereon, or mimicked natural products in one form or another. With the advent and refinement of new technologies, such as genetic techniques for production of secondary plant metabolites, combinatorial synthesis and high-throughput screening, it is expected that novel compounds from natural sources, including medicinal plants, would be identified and developed as safe and effective chemopreventive and anticancer drugs. Numerous bioactive natural compounds have been shown to be useful in prevention and therapy of cancer by targeting various signaling molecules and pathways. Extensive literature underscores the anticancer and chemopreventive activity of a plethora of naturally occurring agents, including phytochemicals. Several of these molecules have been tested in clinical trials and some of them have shown promise in combination therapy when administered along with standard chemotherapeutic agents. Thus, accelerated chemopreventive and chemotherapeutic drug development from natural sources is of great importance. In this special theme issue, contributions from eminent scientists and scholars around the world presented critical analysis of the current progress and promise of natural bioactive constituents in cancer prevention and therapy.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NLZOH, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UILJ, UL, UM, UPCLJ, UPUK, ZAGLJ, ZRSKP
•Phytochemical profile of aerial parts of two Onosma species were determined.•Two Onosma extracts exhibited antioxidant activity and enzyme inhibitory abilities.•More than twenty compounds were ...identified in both two Onosma species.•The in vivo antigenotoxic potential of two Onosma extracts were studied.•The extracts may be potential source for designing novel pharmaceutical agents.
Members of the Onosma genus are widely used in folk medicine and they have great interest in the pharmaceutical industry. In this study, phytochemical characterization, antioxidant activity (2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid (ABTS), ferric reducing antioxidant power (FRAP), cupric reducing antioxidant capacity (CUPRAC), metal chelation, and phosphomolybdenum assays), enzyme inhibition (acetylcholinesterase (AChE), butyrylcholinesterase (BChE), α-amylase, α-glucosidase, and tyrosinase), antimicrobial activity (microdilution method), genotoxic and antigenotoxic (by using Drosophila melanogaster larvae and Comet assay) potentials of Onosma sericea Willd. and Onosma stenoloba Hausskn. ex Riedl. were investigated. Additionally, the bioactive compounds were identified by high performance liquid chromatography-mass spectrometry/mass spectrometry (HPLC-MS/MS) analysis. Generally, O. sericea showed stronger antioxidant activity, while O. stenoloba extract exhibited stronger enzyme inhibitory abilities (cholinesterases and α-amylase). The protective effects of extracts, at the concentration range from 25 to 400 μg/mL, against hydroxyl radical-induced DNA damage were dose-dependent, increasing with a higher dosage. The extracts at the highest concentration (80 mg/mL) showed the absence of genotoxicity in vivo. Antigenotoxic effects were evident after treatment with both extracts, with a percentage reduction of over 80 %. Overall antimicrobial activity of studied extracts was weak, with the lowest minimal inhibitory concentration values (MIC) of 2.5 mg/mL. Taken together, obtained results showed that tested Onosma species can be considered as promising sources of bioactive phytochemicals for pharmacological purposes.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NLZOH, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UILJ, UL, UM, UPCLJ, UPUK, ZAGLJ, ZRSKP
Allium species have been widely used for culinary and medicinal purposes. This study attempts for the first time to investigate into the enzyme inhibitory potential of different plant parts of Allium ...scorodoprasum L. subsp. rotundum (L.) Stearn, also known as wild garlic or leek in Turkey. The antioxidant and enzyme inhibitory potential of the flower, stem, and bulb extracts of A. scorodoprasum were assessed using in vitro bio-assays. The phenolic composition of the different plant parts was also established. The flower extract, having high phenolic content (27.69 mg GAEg extract), showed potent antioxidant activity as a metal chelating agent (22.27 mg EDTAE/g extract), radical scavenger (34.83 and 66.02 mg trolox equivalent (TE)/g extract, for 2,2-diphenyl-1-picrylhydrazyl and 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) assays, respectively) and reducing agent (90.53 mg TE/g extract, for the cupric reducing antioxidant capacity assay). Besides, the flower extract was a potent inhibitor of butyrylcholinesterase (3.16 mg galantamine equivalent (GALAE)/g extract) and tyrosinase (55.21 mg kojic acid equivalent/g extract). The flower extract was rich in rosmarinic acid. In silico studies revealed that rosmarinic acid established several hydrogen bonds and π–π interactions in the enzymatic cavity of butyrylcholinesterase. On the other hand, the stem extract of A. scorodoprasum showed inhibitory action against acetylcholinesterase (2.17 mg GALAE/g extract) and α-amylase (0.55 mmol acarbose equivalent/g extract). Interestingly, we noted that the bulb extract of A. scorodoprasum, inferior in phenolic compounds, showed the least activity. These results suggest that the different plant parts of A. scorodoprasum possessed different biological activities and might be used as a medicinal food plants for specific therapeutic applications.
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•Chemical composition and biological properties of Allium scorodoprasum L. subsp. rotundum were investigated.•Antioxidant and enzyme inhibitory properties were done for bioactivities.•Docking studies were performed for molecular modeling.•The tested extracts exhibited significantly biological effects.•The species could be considered as a valuable source for bioactive compounds.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NLZOH, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UL, UM, UPCLJ, UPUK, ZRSKP
Objectives
Paeoniflorin, a representative pinane monoterpene glycoside in plants of Paeoniaceae family, possesses promising anticancer activities on diverse tumours. This paper summarized the advance ...of Paeoniflorin on cancers in vivo and in vitro, discussed the related molecular mechanisms, as well as suggested some perspectives of the future investigations.
Key findings
Anticancer activities of paeoniflorin have been comprehensively investigated, including liver cancer, gastric cancer, breast cancer, lung cancer, pancreatic cancer, colorectal cancer, glioma, bladder cancer and leukaemia. Furthermore, the potential molecular mechanisms corresponding to the antitumour effects of Paeoniflorin might be related to the following aspects: inhibition of tumour cell proliferation and neovascularization, induction apoptosis, and inhibition of tumour invasion and metastasis.
Summary
Paeoniflorin has wide spectrum antitumour activities; however, in vivo and clinical investigations on antitumour effect of Paeoniflorin are lacking which should be focused on further studies. Our present review on antitumour effects of Paeoniflorin would be beneficial for the further molecular mechanisms study, candidate antitumour drug development and clinical research of Paeoniflorin in the future.
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BFBNIB, FZAB, GIS, IJS, KILJ, NLZOH, NUK, OILJ, SBCE, SBMB, UL, UM, UPUK
Natural products are well-known due to their antimicrobial properties. This study aimed to evaluate the antimicrobial effect of Desplac® product (composed of Aloe Vera, Propolis Extract, Green Tea, ...Cranberry, and Calendula) on the subgingival biofilm. Two different protocols were used to treat the 33-species biofilms: (A) 2×/day (12/12 h) for 1 min with Desplac® or Noplak Toothpaste (Chlorhexidine + Cetylpyridinium Chloride) or Oral B ProGengiva (stannous Fluoride) or a placebo gel; (B) a 12-h use of the Desplac® product or 0.12% chlorhexidine gel or a placebo gel. After 7 days of biofilm formation, the metabolic activity (MA) and biofilm profile were determined by 2,3,5-triphenyltetrazolium chloride and Checker-board DNA-DNA hybridization, respectively. Statistical analysis used the Kruskal-Wallis test followed by Dunn's post-hoc. In protocol A, all treatments presented reduced MA compared to the placebo (
≤ 0.05). The Desplac®-treated biofilm showed a similar microbial profile to other antimicrobials, although with higher bacterial total counts. In protocol B, MA of Desplac®-treated biofilms was lower than the placebo's MA but higher than chlorhexidine-treated biofilms (
≤ 0.05). Pathogen levels in Desplac®-treated biofilms were lower than in placebo-treated biofilms and elevated compared to the chlorhexidine-treated biofilms (
≤ 0.05). Desplac® inhibited the biofilm development and disrupted the mature subgingival biofilm, highlighting its effect on
counts.
Abstract Introduction Oral mucositis is most severe complication of cancer therapy characterized by ulcerative lesions of oral mucosa causing negative impact on patient's quality of life. Wide ...variety of therapeutic agents are available to reduce the lesions of mucositis. Currently, natural herbal remedies have become popular in treating this condition due to fewer side effects than synthetic drugs. Aim The aim of this systematic review is to compile evidence based studies to evaluate the effectiveness of natural agents in the management of oral mucositis induced by chemotherapy or radiotherapy in cancer patients. Materials and method Computerized literature searches were performed to identify all published articles in the subject. The following databases were used: PUBMED MEDLINE, SCOPUS, COCHRANE DATABASE, EMBASE and SCIENCE DIRECT using specific keywords. The search was for limited articles published in English which were read in full by two authors. Results Twenty six randomized controlled trials satisfied our inclusion criteria. Most studies showed statistically significant result demonstrating the efficacy of natural agents with minimal side effects except manuka honey which was not tolerated by few patients. Conclusion Natural agents proved to be promising in healing cancer induced oral mucositis but future demands further randomized controlled clinical trials on these agents which should also be focused on drug interactions of the natural remedies.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NLZOH, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UL, UM, UPCLJ, UPUK, ZRSKP
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