scholarly journals Sesame Extract Promotes Chemopreventive Effect of Hesperidin on Early Phase of Diethylnitrosamine-Initiated Hepatocarcinogenesis in Rats

Pharmaceutics ◽  
2021 ◽  
Vol 13 (10) ◽  
pp. 1687
Author(s):  
Napaporn Khuanphram ◽  
Sirinya Taya ◽  
Prachya Kongtawelert ◽  
Rawiwan Wongpoomchai
Keyword(s):  
Fatty Acid Synthase ◽  
Early Stage ◽  
Biological Activities ◽  
Lipid Lowering ◽  
Anticancer Activities ◽  
Inhibitory Mechanisms ◽  
Alternative Approach ◽  
Triglyceride Content ◽  
Induce Hepatocarcinogenesis ◽  
Chemopreventive Effect

The combination of natural products is an alternative approach to achieving chemopreventive potential. Accordingly, citrus hesperidin exhibits numerous biological activities, including anticarcinogenic activities, while the sesamin in sesame exhibits potent anticancer activities and lipid-lowering effects. We investigated the cancer chemopreventive effects of mixed sesame and orange seed extract (MSO) containing hesperidin and sesamin in diethylnitrosamine (DEN)-induced hepatocarcinogenesis. Rats were injected with DEN once a week for 3 weeks to induce hepatocarcinogenesis. Rats were fed with MSO and various compositions that included sesame extract (SE) and hesperidin. The 10-week administration of MSO more effectively inhibited the number and size of hepatic GST-P-positive foci than hesperidin in DEN-initiated rats. MSO and hesperidin decreased the number of PCNA-positive hepatocytes but increased the apoptotic cells in DEN-induced rats. Furthermore, MSO and its constituents suppressed hepatic triglyceride content concurrently along with the expression of fatty acid synthase. Although the 5-week administration of MSO or hesperidin did not alter hepatic, preneoplastic lesion formation in DEN-initiated rats, it alleviated DEN-induced hepatotoxicity. MSO and its applied compositions did not impact upon the cytochrome P450 system. In conclusion, sesame extract promoted the chemopreventive effect of hesperidin on DEN-induced early stage of hepatocarcinogenesis in rats. The inhibitory mechanisms are likely involved with the induction of cell apoptosis, suppression of cell proliferation and modulation of hepatic lipogenesis. This study may provide revelations in the development of alternative treatments against hepatocellular carcinoma.

Structure and Activity of Pentacyclic Triterpenes Codrugs. A Review

2021 ◽  
Vol 21 ◽  
Author(s):  
Justyna Żwawiak ◽  
Anna Pawełczyk ◽  
Dorota Olender ◽  
Lucjusz Zaprutko
Keyword(s):  
Biological Activities ◽  
Anticancer Activities ◽  
Drug Molecule ◽  
Pentacyclic Triterpene ◽  
Formation Pathway ◽  
Chemical Systems ◽  
Drug Molecules ◽  
Wide Range ◽  
Anti Hiv ◽  
Structure And Activity

: Triterpenes are a wide and important group of compounds that have several promising pharmacological properties, such as hepatoprotective, anti-inflammatory, anti-HIV, antioxidant, or anticancer activities. Such potent substances can be successfully incorporated in more complex chemical systems e.g. codrugs or pro-drugs that have better pharmacological profile. The codrug is connected with a drug formation pathway to chemically cohere at least two drug molecules to improve positive therapeutic efficiency or decrease side effects. The codrug can be cleaved in the organism to generate effective compounds previously used as substrates. This article presents an overview of codrugs that consist of pentacyclic triterpene moiety that is chosen as a basic codrug moiety due to their wide range of vital activities and another drug molecule fragment. It was found that triterpenoid codrugs are characterized by a wide range of biological activities. However, most of them have anticancer potency.

scholarly journals Plant-Derived Nano and Microvesicles for Human Health and Therapeutic Potential in Nanomedicine

Pharmaceutics ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 498
Author(s):  
Mariaevelina Alfieri ◽  
Antonietta Leone ◽  
Alfredo Ambrosone
Keyword(s):  
Therapeutic Potential ◽  
Biological Activities ◽  
Plant Biotechnology ◽  
Bioactive Metabolites ◽  
Anticancer Activities ◽  
Long Distance ◽  
In Vivo Models ◽  
Therapeutic Tools

Plants produce different types of nano and micro-sized vesicles. Observed for the first time in the 60s, plant nano and microvesicles (PDVs) and their biological role have been inexplicably under investigated for a long time. Proteomic and metabolomic approaches revealed that PDVs carry numerous proteins with antifungal and antimicrobial activity, as well as bioactive metabolites with high pharmaceutical interest. PDVs have also been shown to be also involved in the intercellular transfer of small non-coding RNAs such as microRNAs, suggesting fascinating mechanisms of long-distance gene regulation and horizontal transfer of regulatory RNAs and inter-kingdom communications. High loading capacity, intrinsic biological activities, biocompatibility, and easy permeabilization in cell compartments make plant-derived vesicles excellent natural or bioengineered nanotools for biomedical applications. Growing evidence indicates that PDVs may exert anti-inflammatory, anti-oxidant, and anticancer activities in different in vitro and in vivo models. In addition, clinical trials are currently in progress to test the effectiveness of plant EVs in reducing insulin resistance and in preventing side effects of chemotherapy treatments. In this review, we concisely introduce PDVs, discuss shortly their most important biological and physiological roles in plants and provide clues on the use and the bioengineering of plant nano and microvesicles to develop innovative therapeutic tools in nanomedicine, able to encompass the current drawbacks in the delivery systems in nutraceutical and pharmaceutical technology. Finally, we predict that the advent of intense research efforts on PDVs may disclose new frontiers in plant biotechnology applied to nanomedicine.

Synthesis and characterization of a new series of thiadiazole derivatives as potential anticancer agents

2020 ◽  
Vol 26 (1) ◽  
pp. 6-13 ◽  
Author(s):  
Ulviye Acar Çevik ◽  
Derya Osmaniye ◽  
Serkan Levent ◽  
Begüm Nurpelin Sağlik ◽  
Betül Kaya Çavuşoğlu ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Biological Activities ◽  
Cancer Cell Line ◽  
Chemotherapeutic Agents ◽  
Anticancer Activities ◽  
Normal Tissues ◽  
H Nmr ◽  
Wide Range ◽  
Thiadiazole Derivatives ◽  
Low Efficiency

AbstractCancer is one of the most common causes of death in the world. Despite the importance of combating cancer in healthcare systems and research centers, toxicity in normal tissues and the low efficiency of anticancer drugs are major problems in chemotherapy. Nowadays the aim of many medical research projects is to discover new safer and more effective anticancer agents. 1,3,4-Thiadiazole compounds are important fragments in medicinal chemistry because of their wide range of biological activities, including anticancer activities. The aim of this study was to determine the capacity of newly synthesized 1,3,4-thiadiazole compounds as chemotherapeutic agents. The structures of the obtained compounds were elucidated using 1H-NMR, 13C-NMR and mass spectrometry. Although the thiadiazole derivatives did not prove to be significantly cytotoxic to the tumour tissue cultures, compound 4i showed activity against the C6 rat brain cancer cell line (IC50 0.097 mM) at the tested concentrations.

scholarly journals Mango (Mangifera indica L.) Leaves: Nutritional Composition, Phytochemical Profile, and Health-Promoting Bioactivities

Antioxidants ◽  
2021 ◽  
Vol 10 (2) ◽  
pp. 299 ◽  
Author(s):  
Manoj Kumar ◽  
Vivek Saurabh ◽  
Maharishi Tomar ◽  
Muzaffar Hasan ◽  
Sushil Changan ◽  
...  
Keyword(s):  
Biological Activities ◽  
Mangifera Indica ◽  
The Philippines ◽  
Nutritional Composition ◽  
Lipid Lowering ◽  
Pharmaceutical Drugs ◽  
Beneficial Effects ◽  
Health Promoting ◽  
Phytochemical Profile ◽  
Mango Leaves

Mangifera indica L. belongs to the family of Anacardiaceae and is an important fruit from South and Southeast Asia. India, China, Thailand, Indonesia, Pakistan, Mexico, Brazil, Bangladesh, Nigeria, and the Philippines are among the top mango producer countries. Leaves of the mango plant have been studied for their health benefits, which are attributed to a plethora of phytochemicals such as mangiferin, followed by phenolic acids, benzophenones, and other antioxidants such as flavonoids, ascorbic acid, carotenoids, and tocopherols. The extracts from mango leaves (MLs) have been studied for their biological activities, including anti-cancer, anti-diabetic, anti-oxidant, anti-microbial, anti-obesity, lipid-lowering, hepato-protection, and anti-diarrheal. In the present review, we have elaborated on the nutritional and phytochemical profile of the MLs. Further, various bioactivities of the ML extracts are also critically discussed. Considering the phytochemical profile and beneficial effects of the MLs, they can be used as a potential ingredient for the development of functional foods and pharmaceutical drugs. However, more detailed clinical trials still needed to be conducted for establishing the actual efficacy of the ML extracts.

scholarly journals Custard Apple (Annona squamosa L.) Leaves: Nutritional Composition, Phytochemical Profile, and Health-Promoting Biological Activities

Biomolecules ◽  
2021 ◽  
Vol 11 (5) ◽  
pp. 614
Author(s):  
Manoj Kumar ◽  
Sushil Changan ◽  
Maharishi Tomar ◽  
Uma Prajapati ◽  
Vivek Saurabh ◽  
...  
Keyword(s):  
Biological Activities ◽  
Lipid Lowering ◽  
Pharmaceutical Drugs ◽  
Annona Squamosa ◽  
Tropical Fruit ◽  
Custard Apple ◽  
Health Promoting ◽  
Phytochemical Profile

Annona squamosa L. (custard apple) belongs to the family Annonaceae and is an important tropical fruit cultivated in the West Indies, South and Central America, Ecuador, Peru, Brazil, India, Mexico, the Bahamas, Bermuda, and Egypt. Leaves of custard apple plants have been studied for their health benefits, which are attributed to a considerable diversity of phytochemicals. These compounds include phenol-based compounds, e.g., proanthocyanidins, comprising 18 different phenolic compounds, mainly alkaloids and flavonoids. Extracts from Annona squamosa leaves (ASLs) have been studied for their biological activities, including anticancer, antidiabetic, antioxidant, antimicrobial, antiobesity, lipid-lowering, and hepatoprotective functions. In the current article, we discussed the nutritional and phytochemical diversity of ASLs. Additionally, ASL extracts were discussed with respect to their biological activities, which were established by in vivo and in vitro experiments. A survey of the literature based on the phytochemical profile and health-promoting effects of ASLs showed that they can be used as potential ingredients for the development of pharmaceutical drugs and functional foods. Although there are sufficient findings available from in vitro and in vivo investigations, clinical trials are still needed to determine the exact effects of ASL extracts on human health.

scholarly journals An Alternative Approach for the Synthesis of Sulfoquinovosyldiacylglycerol

Molecules ◽  
2021 ◽  
Vol 26 (14) ◽  
pp. 4275
Author(s):  
Tobias Sitz ◽  
Hendrik Domey ◽  
Judith Fischer ◽  
Sascha Rohn
Keyword(s):  
Fatty Acids ◽  
Functional Foods ◽  
Unsaturated Fatty Acids ◽  
Biological Activities ◽  
Saturated Fatty Acids ◽  
Diverse Range ◽  
Natural Sources ◽  
Model Studies ◽  
Alternative Approach ◽  
Increasing Demand

Sulfoquinovosyldiacylglycerol (SQDG) is a glycolipid ubiquitously found in photosynthetically active organisms. It has attracted much attention in recent years due to its biological activities. Similarly, the increasing demand for vegan and functional foods has led to a growing interest in micronutrients such as sulfolipids and their physiological influence on human health. To study this influence, reference materials are needed for developing new analytical methods and providing enough material for model studies on the biological activity. However, the availability of these materials is limited by the difficulty to isolate and purify sulfolipids from natural sources and the unavailability of chemical standards on the market. Consequently, an alternative synthetic route for the comprehensive preparation of sulfolipids was established. Here, the synthesis of a sulfolipid with two identical saturated fatty acids is described exemplarily. The method opens possibilities for the preparation of a diverse range of interesting derivatives with different saturated and unsaturated fatty acids.

Synthesis and biological activities of chaetocin and its derivatives

2012 ◽  
Vol 84 (6) ◽  
pp. 1369-1378 ◽  
Author(s):  
Mikiko Sodeoka ◽  
Kosuke Dodo ◽  
Yuou Teng ◽  
Katsuya Iuchi ◽  
Yoshitaka Hamashima ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Caspase 3 ◽  
Biological Activities ◽  
Caspase 8 ◽  
Human Leukemia ◽  
Mechanistic Studies ◽  
Anticancer Activities ◽  
Histone Methyltransferases ◽  
Structure Activity ◽  
Apoptosis Inducer

Chaetocin, a natural product isolated from fungi of Chaetomium species, is a member of the epipolythiodiketopiperazines (ETPs), which have various biological activities, including cytostatic and anticancer activities. Recently, the inhibitory activity toward histone methyltransferases (HMTs) was discovered for chaetocin. We previously reported the first total synthesis of chaetocin and various derivatives. During studies on the structure–activity relationship for HMT inhibition, we found that the enantiomer of chaetocin (ent-chaetocin) is a more potent apoptosis inducer than natural chaetocin in human leukemia HL-60 cells. Mechanistic studies showed that ent-chaetocin induces apoptosis through the caspase-8/caspase-3 pathway.

Influence of atorvastatin and carboxymethylated glucan on the serum lipoprotein profile and MMP activity of mice with lipemia induced by poloxamer 407

2012 ◽  
Vol 90 (2) ◽  
pp. 141-153 ◽  
Author(s):  
Tatyana A. Korolenko ◽  
Fedor V. Tuzikov ◽  
Marina S. Cherkanova ◽  
Thomas P. Johnston ◽  
Natalia A. Tuzikova ◽  
...  
Keyword(s):  
Total Cholesterol ◽  
Early Stage ◽  
Density Lipoprotein ◽  
Serum Lipoprotein ◽  
Matrix Metalloproteases ◽  
Poloxamer 407 ◽  
Lipid Lowering ◽  
High Dose ◽  
Scattering Method ◽  
Atorvastatin Treatment

The effects of atorvastatin and carboxymethylated β-glucan (CMG) on the lipoprotein-cholesterol (LP-C) and lipoprotein-triglyceride (LP-TG) fractions and subfractions at the early stage of murine hyperlipidemia, and its pleiotropic anti-inflammatory effects, were studied. Atorvastatin and CMG were administered in ICR male mice with acute lipemia induced with a single injection of poloxamer 407 (P-407). A novel small-angle X-ray scattering method for the determination of fractional and subfractional composition of LP-C and LP-TG was used. In P-407-treated animals, there was a drastic increase of total cholesterol and especially TG. Atorvastatin decreased both the total cholesterol and TG, but not to control levels. CMG primarily decreased TG and was not as potent as atorvastatin. P-407 increased atherogenic LDL-C (IDL-C and LDL1–3-C subfractions) and very low-density lipoprotein-C (VLDL-C) (VLDL1–2-C and VLDL3–5-C subfractions) fractions, with an increase of the total anti-atherogenic HDL-C fraction (HDL2-C subfraction). Atorvastatin treatment of lipemia was followed by a decrease in the total LP-C, total LDL-C (LDL1–3-C subfraction), and the LDL1–3-TG subfraction. Additionally, atorvastatin treatment resulted in an increase in the serum matrix metalloproteases activity both in control and P-407-treated mice. In general, high-dose atorvastatin therapy exerts its lipid-lowering and pleiotropic effects in the early stages of acute lipemia induced in mice by treatment with P-407.

Synthesis of a Series of Novel 2-Amino-5-Substituted 1,3,4-oxadiazole and 1,3,4-thiadiazole Derivatives as Potential Anticancer, Antifungal and Antibacterial Agents

2021 ◽  
Vol 17 ◽  
Author(s):  
Em Canh Pham ◽  
Tuyen Ngoc Truong ◽  
Nguyen Hanh Dong ◽  
Duy Duc Vo ◽  
Tuoi Thi Hong Do
Keyword(s):  
Cell Line ◽  
Biological Activities ◽  
Chemical Properties ◽  
Diffusion Method ◽  
Anticancer Activities ◽  
Molecular Docking Study ◽  
Antifungal Activities ◽  
Antibacterial And Antifungal Activities ◽  
Thiadiazole Derivatives ◽  
Antibacterial And Antifungal

Background: Many compounds containing a five-membered heterocyclic ring display exceptional chemical properties and versatile biological activities. Objective: The objective of the present study was the desire to prepare the 5-substituted 2-amino-1,3,4-oxadiazole and 2-amino-1,3,4-thiadiazole derivatives and evaluate their potential anticancer, antibacterial and antifungal activities. Methods: Twenty-seven derivatives were synthesized by iodine-mediated cyclization of semicarbazones or thiosemicarbazones obtained from condensation of semicarbazide or thiosemicarbazide and aldehydes. The structures were confirmed by 1H-NMR, 13C-NMR and MS spectra. The antibacterial and antifungal activities were evaluated by diffusion method and the anticancer activities were evaluated by MTT assay. Results: Twenty-seven derivatives have been synthesized in moderate to good yields. A number of derivatives exhibited potential antibacterial, antifungal and anticancer activities. Conclusion: Compounds (1b, 1e and 1g) showed antibacterial activity against Streptococcus faecalis, MSSA and MRSA with MIC ranging between 4 to 64 µg/mL. Compound (2g) showed antifungal activity against Candida albicans (8 µg/mL) and Aspergillus niger (64 µg/mL). Compound (1o) exhibited high cytotoxic activity against HepG2 cell line (IC50 value 8.6 µM), which is comparable to the activity of paclitaxel, and is non-toxic on LLC-PK1 normal cell line. The structure activity relationship and molecular docking study of the synthesized compounds are also reported.

Recent advances in chalcone-based anticancer heterocycles: A structural and molecular target perspective

2021 ◽  
Vol 28 ◽  
Author(s):  
Vishal Kumar ◽  
Sanjeev Dhawan ◽  
Pankaj Sanjay Girase ◽  
Paul Awolade ◽  
Suraj Raosaheb Shinde ◽  
...  
Keyword(s):  
Histone Deacetylases ◽  
Biological Activities ◽  
Molecular Targets ◽  
Cathepsin K ◽  
Cost Effective ◽  
Sirtuin 1 ◽  
Anticancer Activities ◽  
Structural Variations ◽  
Research Attention ◽  
Endothelial Growth Factor

: Chalcones are an interesting class of compounds endowed with a plethora of biological activities beneficial to human health. These chemo types have continued to attract increased research attention over the years; hence, numerous natural and synthetic chalcones have found with interesting anticancer activities through the inhibition of various molecular targets including ABCG2, BCRP, P-glycoprotein, 5α-reductase, Androgen receptor (AR), Histone deacetylases (HDAC), Sirtuin 1, proteasome, Vascular endothelial growth factor (VEGF), Cathepsin-K, tubulin, CDC25B phosphatase, Topoisomerase, EBV, NF-κB, mTOR, BRAF and Wnt/β-catenin. Moreover, the study of intrinsic mechanisms of action, particularly relating to specific cellular pathways and modes of engagement with molecular targets, may help medicinal chemists to develop a more effective, selective, and cost-effective chalcone-based anticancer drugs. This review, therefore, sheds light on the effect of structural variations on the anticancer potency of chalcone hybrids reported in 2018-2019 alongside their mechanism of action, molecular targets, and potential impacts on effective cancer chemotherapy.

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