scholarly journals Biological significance of naturally occurring deuterium: the antitumor effect of deuterium depletion

2010 ◽  
Vol 151 (36) ◽  
pp. 1455-1460 ◽  
Author(s):  
Gábor Somlyai ◽  
Miklós Molnár ◽  
Gábor Laskay ◽  
Mariann Szabó ◽  
Tamás Berkényi ◽  
...  
Keyword(s):  
Antitumor Effect ◽  
Biological Significance ◽  
Human Melanoma ◽  
Naturally Occurring ◽  
Ht 29 ◽  
Mcf 7

A felszíni vizekben a deutérium (D) koncentrációja több mint 16 mmol/l (150 ppm), az élő szervezetekben 10 mmol/l fölötti. A csökkentett deutériumtartalmú (30±5 ppm) vízzel folyó kutatások során korábban azt tapasztalták, hogy a deutériummegvonás gátolta a sejtosztódást in vitro különböző tumoros sejtvonalakban (PC-3, humán prosztatatumor; MDA, humán emlőtumor; HT-29, humán vastagbéltumor; M14, humán melanoma). A csökkentett deutériumtartalmú víz tumorregressziót idézett elő humán eredetű tumorral xenotranszplantált, immunszuppresszált egerekben (MDA és MCF-7 humán emlőtumor, PC-3 prosztatatumor), és apoptózist indukált in vitro és in vivo . A csökkentett deutériumtartalmú víz (25±5 ppm) részleges vagy teljes tumorregressziót idézett elő spontán tumoros kutyákban és macskákban. A készítményt 1999-ben daganatellenes állatgyógyszerként törzskönyvezték (Vetera-DDW-25 A.U.V., 13/99 FVM). Injekciós változatát klinikai vizsgálatban sikeresen tesztelték. Az Országos Gyógyszerészeti Intézet 5621/40/95 számú engedélye alapján, a GCP-elvek betartásával lefolytatott randomizált, kettős vak elrendezésű humán fázis II klinikai vizsgálat szignifikáns különbséget igazolt a kontroll- és a kezelt csoport között a vizsgált paraméterek vonatkozásában. Egyéves utánkövetés során a csökkentett deutériumtartalmú víz szignifikánsan csökkentette a prosztatatumoros betegek halálozási arányát, miközben a túlélés hosszát szignifikánsan növelte. Az eredmények azt igazolják, hogy a sejtek képesek szabályozni a deutérium/hidrogén (D/H) arányát és ennek változtatásával elindítani bizonyos molekuláris folyamatokat, amelyeknek kulcsszerepük van a sejtciklus szabályozásában. Feltételezzük, hogy nem az intracelluláris pH változása, hanem az azt kísérő D/H arány változása adja meg a sejteknek a jelet az S-fázisba lépéshez. A D-koncentráció csökkenése beavatkozik a szignáltranszdukciós folyamatokba, így idézve elő a tumor regresszióját. A D szerepének felismerése a sejtosztódás szabályozásában új lehetőségeket nyit meg a daganatterápia és a megelőzés területén, hozzájárulva ezzel a jelenlegi daganatellenes terápiák hatékonyságának növeléséhez.

Derivatives of Deoxypodophyllotoxin Induce Apoptosis Through Bcl-2/Bax Proteins Expression

2020 ◽  
Vol 20 ◽  
Author(s):  
Ya-Nan Li ◽  
Ni Ning ◽  
Lei Song ◽  
Yun Geng ◽  
Jun-Ting Fan ◽  
...  
Keyword(s):  
Annexin V ◽  
Mtt Method ◽  
Anthriscus Sylvestris ◽  
Anti Tumor Activity ◽  
Derivatives Of ◽  
Toxicity In Vitro ◽  
Ht 29 ◽  
Mcf 7

Background: Deoxypodophyllotoxin, isolated from theTraditional Chinese Medicine Anthriscus sylvestris, is well-known because of its significant antitumor activity with strong toxicity in vitro and in vivo. Objective: In this article, we synthesized a series of deoxypodophyllotoxin derivatives, and evaluated their antitumor effectiveness.Methods:The anti tumor activity of deoxypodophyllotoxin derivatives was investigated by the MTT method. Apoptosis percentage was measured by flow cytometer analysis using Annexin-V-FITC. Results: The derivatives revealed obvious cytotoxicity in the MTT assay by decreasing the number of late cancer cells. The decrease of Bcl-2/Bax could be observed in MCF-7, HepG2, HT-29 andMG-63 using Annexin V-FITC. The ratio of Bcl-2/Bax in the administration group was decreased, which was determined by the ELISA kit. Conclusion: The derivatives of deoxypodophyllotoxin could induce apoptosis in tumor cell lines by influencing Bcl-2/Bax.

scholarly journals Injectable Click Polypeptide Hydrogels via Tetrazine-Norbornene Chemistry for Localized Cisplatin Release

Polymers ◽  
2020 ◽  
Vol 12 (4) ◽  
pp. 884
Author(s):  
Zhen Zhang ◽  
Chaoliang He ◽  
Xuesi Chen
Keyword(s):  
Antitumor Effect ◽  
Click Reaction ◽  
Polymer Concentration ◽  
Mechanical Analysis ◽  
Molar Ratio ◽  
Phase Cell ◽  
Mice Model ◽  
Mcf 7

Injectable, covalently cross-linked hydrogels have been widely investigated in drug delivery systems due to their superior mechanical properties and long-term stability. Conventional covalently cross-linked hydrogels are formed by chemical reactions that may interfere with natural biochemical processes. In this work, we developed an injectable polypeptide hydrogel via an inverse electron demand Diels-Alder reaction between norbornene modified poly(L-glutamic acid) (PLG-Norb) and tetrazine functionalized four-arm poly(ethylene glycol) (4aPEG-T) for localized release of cisplatin (CDDP). The rapid and bioorthogonal click reaction allowed for hydrogel formation within a few minutes after mixing the two polymer solutions in phosphate buffer saline (PBS). Dynamic mechanical analysis suggested that the storage modulus of the hydrogel could be readily tuned by changing the polymer concentration and the molar ratio of the two functional groups. The carboxyl groups of PLG-Norb were used to form polymer–metal complexation with CDDP, and the controlled release of the antitumor drug was achieved in PBS. The CDDP-loaded hydrogel displayed an antitumor effect against MCF-7 cells in vitro, through S phase cell cycle arrest. After subcutaneous injection in rats, the hydrogel was rapidly formed in situ and showed good stability in vivo. In an MCF-7-bearing nude mice model, the CDDP-loaded hydrogel exhibited an improved antitumor effect with reduced systemic toxicity. Overall, the injectable click polypeptide hydrogel shows considerable potential as a platform for localized and sustained delivery of antitumor drugs.

scholarly journals Determination of Enzyme Inhibition Potential and Anticancer Effects of Pistacia khinjuk Stocks Raised in In Vitro and In Vivo Conditions

Agronomy ◽  
2021 ◽  
Vol 11 (1) ◽  
pp. 154
Author(s):  
Emine Ayaz Tilkat ◽  
Hayri Batibay ◽  
Ismail Yener ◽  
Pelin Koseoglu Yilmaz ◽  
Mehmet Akdeniz ◽  
...  
Keyword(s):  
Enzyme Inhibition ◽  
Shoot Cultures ◽  
Root Extracts ◽  
Bche Activity ◽  
Pistacia Khinjuk ◽  
Cell Series ◽  
Ht 29 ◽  
Mcf 7

In this study, antihypertensive, anticholinesterase, antiurease, antityrosinase and antielastase enzyme inhibition and anticancer activities of in vivo (male and female) and in vitro samples (root, stem and leaf parts) of the Pistacia khinjuk Stocks were investigated comparatively. In this context, in vitro shoot cultures were obtained from germinated mature seeds. Then, the juvenile shoots were proliferated in Murashige and Skoog (MS) medium supplemented with 1 mg/L 6-Benzylaminopurine (BAP). In terms of anticancer activity, the whole of the samples studied was found to have apoptotic effects against MCF-7 (breast cancer) and HT-29 (colon cancer) cell lines. The extracts obtained from in vivo female root parts showed better cytotoxicity than all the other tested extracts on MCF-7 (IC50: 31.86 ± 1.40 µg/mL) and HT-29 cell series (IC50: 59.60 ± 0.69 µg/mL). Even though all the samples showed a strong butyrylcholinesterase enzyme inhibition (BChE) activity, it was detected that none of the samples had shown acetylcholinesterase enzyme inhibition (AChE). It was also determined that in vivo leaf samples of female trees had the highest BChE activity (Inhibition%: 75.20 ± 1.50). All the samples showed a low-moderate level of urease and tyrosinase enzyme activity, while in vivo samples showed a significant level of the elastase enzyme activities (Inhibition%: 58.72 for female root extracts; 58.25 for female leaf extracts, at 50 µg/mL concentration), and they were more active than the standard oleanolic acid (Inhibition%: 39.46 ± 0.52). The antihypertensive activities as the inhibition of angiotensin I-converting enzyme (ACE) of in vivo samples (Inhibition%: 95.88 for female stem extracts; 95.18 for female root extracts) were detected as close to the standard (Inhibition%: 96.64 ± 1.85) used. In general, it can be stated that in vivo samples had higher biological activities compared to in vitro ones. Consequently, according to our results, it was concluded that in vitro stem parts of khinjuk pistachio could also be evaluated as an alternative new antihypertensive, antielastase and anticancer agent source.

scholarly journals Χαρακτηρισμός βιολογικών δράσεων ενεργών συστατικών αιθέριων ελαίων

2017 ◽  
Author(s):  
Ελένη Φίτσιου
Keyword(s):  
Pistacia Lentiscus ◽  
Lippia Citriodora ◽  
Ht 29 ◽  
Satureja Thymbra ◽  
Mcf 7

Τα αρωματικά φυτά είναι γνωστά για τις ποικίλες ιδιότητές τους από την αρχαιότητα ένα μεγάλο μέρος των οποίων οφείλεται στα αιθέρια έλαια που αποτελούν δευτερογενείς μεταβολίτες. Σήμερα, τα αιθέρια ελαία μελετώνται για τις βιολογικές τους ιδιότητες, ανάμεσα στις οποίες συγκαταλέγεται η χημειοπροληπτική τους δράση, δηλαδή ένας συνδυασμός ενδοκυτταρικών μηχανισμών δράσης συμπεριλαμβανομένων της αντιοξειδωτικής, αντιφλεγμονώδους και προ-αποπτωτικής. Στόχος της έρευνάς μας ήταν να ελέγξουμε έναν αριθμό φυσικών εκχυλισμάτων από ελληνικά φυτά για την πιθανή χημειοπροληπτική τους δράση και να μελετήσουμε περαιτέρω τα πιο υποσχόμενα για τους μοριακούς μηχανισμούς δράσης τους. Πενήντα φυτικά εκχυλίσματα ελέγχθηκαν για την ικανότητα τους να απενεργοποιούν ελεύθερες ρίζες in vitro (τεχνικές DPPH και ABTS). Παράλληλα, 10 αιθέρια έλαια ελέγχθηκαν για την αντιπολλαπλασιαστική τους δράση εναντίον διαφορετικών καρκινικών κυτταρικών σειρών in vitro (Caco2, HepG2, MCF-7) (τεχνική SRB) και αναλύθηκε η χημική τους σύσταση. Τα περισσότερα αιθέρια έλαια είχαν ως κύρια συστατικά τερπένια και τερπενοειδή, ενώ συνολικά την σημαντικότερη δράση επέδειξαν τα έλαια των φυτών Satureja thymbra, Origanum dittany Lippia citriodora (λουίζα) και Pistacia lentiscus var. Chia (μαστίχα). Μετά το τέλος της σάρωσης επιλέξαμε τα δύο τελευταία, καθώς και τα κυριότερα συστατικά τους για περαιτέρω μελέτες. Τα δύο κυριότερα συστατικά του μαστιχέλαιου, α-πινένιο και μυρκένιο, δεν παρουσίασαν σημαντική αντιοξειδωτική δράση, ενώ το έλαιο της λουίζας, παρουσίασε ισχυρότερη δράση από το κύριο συστατικό του, citral. Με εξαίρεση το μυρκένιο, όλοι οι παράγοντες εμφάνισαν υψηλή αντιπολλαπλασιαστική ικανότητα in vitro, η οποία συνδέεται με την ικανότητά τους να προκαλούν βλάβες στο DNA, ενώ τα δύο έλαια επέδειξαν και σημαντική ογκοκατασταλτική δράση in vivo. Χρησιμοποιώντας κυτταρομετρία ροής παρατηρήθηκε αναστολή του κυτταρικού κύκλου στη φάση G2/M σε διαφορετικές κυτταρικές σειρές, με παράλληλη αλλαγή στην έκφραση γονιδίων που σχετίζονται με τον κυτταρικό κύκλο (cyclinA, B1, D, E, p53, p21, survivin) για τη λουίζα και το citral. Επίσης, παρατηρήσαμε πως κανένα φυτοχημικό δεν επάγει την κλασσική απόκριση της απόπτωσης σε καρκινικά κύτταρα παχέος εντέρου (για τις δεδομένες χρονικές επωάσεις και συγκεντρώσεις που χρησιμοποιήθηκαν), καθώς δεν ανιχνεύσαμε ούτε αύξηση του πληθυσμού των προ-αποπτωτικών κυττάρων, ούτε και αύξηση της ενεργότητας του ενζύμου κασπάση-3. Παράλληλα, δεν προκλήθηκε σημαντική αλλαγή στα επίπεδα πρωτεϊνών που σχετίζονται με την απόπτωση εκτός από τις ακόλουθες πρωτεΐνες: ενεργή κασπάση-3, cIAP-2, Livin, catalase, p21, p27 και TRAIL R1 και R2 για το έλαιο της μαστίχας και τις survivin, claspin, TRAILR2, clusterin, HSP60 και Fas για το έλαιο της λουίζας, που μαζί με το citral πιθανόν να ενεργοποιούν το μονοπάτι της αυτοφαγίας βάσει πειραματικών ενδείξεων. Τέλος, η λουίζα διαθέτει μεγαλύτερη ικανότητα ενίσχυσης της δράσης των δύο χημειοθεραπευτικών παραγόντων oxaliplatin και irinotecan στις κυτταρικές σειρές Caco2 και HT-29 σε σχέση με το citral. Συμπερασματικά, τα ευρήματα μας υποδεικνύουν πως τα φυσικά εκχυλίσματα που μελετήσαμε, και κυρίως τα έλαια μαστίχας και λουίζας, διαθέτουν πολλά υποσχόμενες δραστικότητες που αξίζουν περαιτέρω διερεύνησης για τη μελλοντική χρήση τους ως χημειοπροληπτικοί και χημειοθεραπευτικοί παράγοντες.

Репрограммированые in vitro на М3 фенотип макрофаги останавливают рост солидной карциномы in vivo

2018 ◽  
pp. 41-46
Author(s):  
А.А. Раецкая ◽  
С.В. Калиш ◽  
С.В. Лямина ◽  
Е.В. Малышева ◽  
О.П. Буданова ◽  
...  
Keyword(s):  
Solid Tumor ◽  
Antitumor Effect ◽  
Tumor Development ◽  
Significant Inhibition ◽  
The Body ◽  
Ehrlich Carcinoma ◽  
Solid Carcinoma ◽  
Ec Cells

Цель исследования. Доказательство гипотезы, что репрограммированные in vitro на М3 фенотип макрофаги при введении в организм будут существенно ограничивать развитие солидной карциномы in vivo . Методика. Рост солидной опухоли инициировали у мышей in vivo путем подкожной инъекции клеток карциномы Эрлиха (КЭ). Инъекцию макрофагов с нативным М0 фенотипом и с репрограммированным M3 фенотипом проводили в область формирования солидной КЭ. Репрограммирование проводили с помощью низких доз сыворотки, блокаторов факторов транскрипции STAT3/6 и SMAD3 и липополисахарида. Использовали две схемы введения макрофагов: раннее и позднее. При раннем введении макрофаги вводили на 1-е, 5-е, 10-е и 15-е сут. после инъекции клеток КЭ путем обкалывания макрофагами с четырех сторон область развития опухоли. При позднем введении, макрофаги вводили на 10-е, 15-е, 20-е и 25-е сут. Через 15 и 30 сут. после введения клеток КЭ солидную опухоль иссекали и измеряли ее объем. Эффект введения макрофагов оценивали качественно по визуальной и пальпаторной характеристикам солидной опухоли и количественно по изменению ее объема по сравнению с группой без введения макрофагов (контроль). Результаты. Установлено, что M3 макрофаги при раннем введении от начала развития опухоли оказывают выраженный антиопухолевый эффект in vivo , который был существенно более выражен, чем при позднем введении макрофагов. Заключение. Установлено, что введение репрограммированных макрофагов M3 ограничивает развитие солидной карциномы в экспериментах in vivo . Противоопухолевый эффект более выражен при раннем введении М3 макрофагов. Обнаруженные в работе факты делают перспективным разработку клинической версии биотехнологии ограничения роста опухоли, путем предварительного программирования антиопухолевого врожденного иммунного ответа «в пробирке». Aim. To verify a hypothesis that macrophages reprogrammed in vitro to the M3 phenotype and injected into the body substantially restrict the development of solid carcinoma in vivo . Methods. Growth of a solid tumor was initiated in mice in vivo with a subcutaneous injection of Ehrlich carcinoma (EC) cells. Macrophages with a native M0 phenotype or reprogrammed towards the M3 phenotype were injected into the region of developing solid EC. Reprogramming was performed using low doses of serum, STAT3/6 and SMAD3 transcription factor blockers, and lipopolysaccharide. Two schemes of macrophage administration were used: early and late. With the early administration, macrophages were injected on days 1, 5, 10, and 15 following the injection of EC cells at four sides of the tumor development area. With the late administration, macrophages were injected on days 10, 15, 20, and 25. At 15 and 30 days after the EC cell injection, the solid tumor was excised and its volume was measured. The effect of macrophage administration was assessed both qualitatively by visual and palpation characteristics of solid tumor and quantitatively by changes in the tumor volume compared with the group without the macrophage treatment. Results. M3 macrophages administered early after the onset of tumor development exerted a pronounced antitumor effect in vivo , which was significantly greater than the antitumor effect of the late administration of M3 macrophages. Conclusion. The observed significant inhibition of in vivo growth of solid carcinoma by M3 macrophages makes promising the development of a clinical version of the biotechnology for restriction of tumor growth by in vitro pre-programming of the antitumor, innate immune response.

A Novel Triazole Derivative Drug Presenting In Vitro and In Vivo Anticancer Properties

2018 ◽  
Vol 18 (17) ◽  
pp. 1483-1493
Author(s):  
Ricardo Imbroisi Filho ◽  
Daniel T.G. Gonzaga ◽  
Thainá M. Demaria ◽  
João G.B. Leandro ◽  
Dora C.S. Costa ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Hepatic Function ◽  
Anticancer Properties ◽  
Mcf 7

Background: Cancer is a major cause of death worldwide, despite many different drugs available to treat the disease. This high mortality rate is largely due to the complexity of the disease, which results from several genetic and epigenetic changes. Therefore, researchers are constantly searching for novel drugs that can target different and multiple aspects of cancer. Experimental: After a screening, we selected one novel molecule, out of ninety-four triazole derivatives, that strongly affects the viability and proliferation of the human breast cancer cell line MCF-7, with minimal effects on non-cancer cells. The drug, named DAN94, induced a dose-dependent decrease in MCF-7 cells viability, with an IC50 of 3.2 ± 0.2 µM. Additionally, DAN94 interfered with mitochondria metabolism promoting reactive oxygen species production, triggering apoptosis and arresting the cancer cells on G1/G0 phase of cell cycle, inhibiting cell proliferation. These effects are not observed when the drug was tested in the non-cancer cell line MCF10A. Using a mouse model with xenograft tumor implants, the drug preventing tumor growth presented no toxicity for the animal and without altering biochemical markers of hepatic function. Results and Conclusion: The novel drug DAN94 is selective for cancer cells, targeting the mitochondrial metabolism, which culminates in the cancer cell death. In the end, DAN94 has been shown to be a promising drug for controlling breast cancer with minimal undesirable effects.

scholarly journals Conifers Phytochemicals: A Valuable Forest with Therapeutic Potential

Molecules ◽  
2021 ◽  
Vol 26 (10) ◽  
pp. 3005
Author(s):  
Kanchan Bhardwaj ◽  
Ana Sanches Silva ◽  
Maria Atanassova ◽  
Rohit Sharma ◽  
Eugenie Nepovimova ◽  
...  
Keyword(s):  
Experimental Data ◽  
Potential Role ◽  
Therapeutic Potential ◽  
Fungal Infections ◽  
Cell Damage ◽  
Cancer Growth ◽  
Naturally Occurring ◽  
Antioxidant Effects

Conifers have long been recognized for their therapeutic potential in different disorders. Alkaloids, terpenes and polyphenols are the most abundant naturally occurring phytochemicals in these plants. Here, we provide an overview of the phytochemistry and related commercial products obtained from conifers. The pharmacological actions of different phytochemicals present in conifers against bacterial and fungal infections, cancer, diabetes and cardiovascular diseases are also reviewed. Data obtained from experimental and clinical studies performed to date clearly underline that such compounds exert promising antioxidant effects, being able to inhibit cell damage, cancer growth, inflammation and the onset of neurodegenerative diseases. Therefore, an attempt has been made with the intent to highlight the importance of conifer-derived extracts for pharmacological purposes, with the support of relevant in vitro and in vivo experimental data. In short, this review comprehends the information published to date related to conifers’ phytochemicals and illustrates their potential role as drugs.

scholarly journals Anticancer Activity of Triazolo-Thiadiazole Derivatives and Inhibition of AKT1 and AKT2 Activation

Pharmaceutics ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 493
Author(s):  
Dimitrios T. Trafalis ◽  
Sofia Sagredou ◽  
Panayiotis Dalezis ◽  
Maria Voura ◽  
Stella Fountoulaki ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Human Colon ◽  
Tumor Xenograft ◽  
Atp Binding Site ◽  
Anticancer Properties ◽  
Extensive Range ◽  
Dependent Inhibition ◽  
Ht 29

The fusion of 1,2,4-triazole and 1,3,4-thiadiazole rings results in a class of heterocycles compounds with an extensive range of pharmacological properties. A series of 1,2,4-triazolo[3,4-b]-1,2,4-thiadiazoles was synthesized and tested for its enzyme inhibition potential and anticancer activity. The results show that 1,2,4-triazolo[3,4-b]-1,2,4-thiadiazoles display potent anticancer properties in vitro against a panel of cancer cells and in vivo efficacy in HT-29 human colon tumor xenograft in CB17 severe combined immunodeficient (SCID) mice. Preliminary mechanistic studies revealed that KA25 and KA39 exhibit time- and concentration-dependent inhibition of Akt Ser-473 phosphorylation. Molecular modeling experiments indicated that 1,2,4-triazolo[3,4-b]-1,2,4-thiadiazoles bind well to the ATP binding site in Akt1 and Akt2. The low acute toxicity combined with in vitro and in vivo anticancer activity render triazolo[3,4-b]thiadiazoles KA25, KA26, and KA39 promising cancer therapeutic agents.

scholarly journals Thymoquinone, a Dietary Bioactive Compound, Exerts Anti-Inflammatory Effects in Colitis by Stimulating Expression of the Colonic Epithelial PPAR-γ Transcription Factor

Nutrients ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 1343
Author(s):  
Balaji Venkataraman ◽  
Saeeda Almarzooqi ◽  
Vishnu Raj ◽  
Abdullah T. Alhassani ◽  
Ahmad S. Alhassani ◽  
...  
Keyword(s):  
Transcription Factor ◽  
Activity Index ◽  
Nigella Sativa ◽  
Mapk Signaling ◽  
Mitogen Activated Protein Kinase ◽  
Ppar Γ ◽  
Anti Inflammatory ◽  
Ht 29

Inflammatory bowel diseases (IBD) are chronic inflammatory disorders with increasing incidence and prevalence worldwide. Here, we investigated thymoquinone (TQ), a naturally occurring phytochemical present in Nigella sativa, for anti-inflammatory effects in colonic inflammation. To address this, we used in vivo (mice) and in vitro (HT-29 cells) models in this investigation. Our results showed that TQ treatment significantly reduced the disease activity index (DAI), myeloperoxidase (MPO) activity, and protected colon microscopic architecture. In addition, TQ also reduced the expression of proinflammatory cytokines and mediators at both the mRNA and protein levels. Further, TQ decreased phosphorylation of the activated mitogen-activated protein kinase (MAPK) signaling pathway and nuclear factor kappa B (NF-κB) proteins and enhanced colon epithelial PPAR-γ transcription factor expression. TQ significantly decreased proinflammatory chemokines (CXCL-1 and IL-8), and mediator (COX-2) mRNA expression in HT-29 cells treated with TNF-α. TQ also increased HT-29 PPAR-γ mRNA, PPAR-γ protein expression, and PPAR-γ promoter activity. These results indicate that TQ inhibits MAPK and NF-κB signaling pathways and transcriptionally regulates PPAR-γ expression to induce potent anti-inflammatory activity in vivo and in vitro models of colon inflammation.

scholarly journals Identification of the Active Ingredient and Beneficial Effects of Vitex rotundifolia Fruits on Menopausal Symptoms in Ovariectomized Rats

Biomolecules ◽  
2021 ◽  
Vol 11 (7) ◽  
pp. 1033
Author(s):  
Ji Hwan Lee ◽  
Sullim Lee ◽  
Quynh Nhu Nguyen ◽  
Hung Manh Phung ◽  
Myoung-Sook Shin ◽  
...  
Keyword(s):  
Weight Gain ◽  
Body Weight Gain ◽  
Animal Experiments ◽  
Ovariectomized Rats ◽  
Biological Functions ◽  
Menopausal Syndrome ◽  
Active Constituents ◽  
Mcf 7

Estrogen replacement therapy is a treatment to relieve the symptoms of menopause. Many studies suggest that natural bioactive ingredients from plants resemble estrogen in structure and biological functions and can relieve symptoms of menopause. The fruit of V. rotundifolia, called “Man HyungJa” in Korean, is a traditional medicine used to treat headache, migraine, eye pain, neuralgia, and premenstrual syndrome in Korea and China. The aim of the present study was to confirm that V. rotundifolia fruit extract (VFE) exerts biological functions similar to those of estrogen in menopausal syndrome. We investigated its in vitro effects on MCF-7 cells and in vivo estrogen-like effects on weight gain and uterine contraction in ovariectomized rats. Using the polar extract, the active constituents of VFE (artemetin, vitexicarpin, hesperidin, luteolin, vitexin, and vanillic acid) with estrogen-like activity were identified in MCF-7 cells. In animal experiments, the efficacy of VFE in ameliorating body weight gain was similar to that of estrogen, as evidenced from improvements in uterine atrophy. Vitexin and vitexicarpin are suggested as the active constituents of V. rotundifolia fruits.

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