scholarly journals Anti-Acne Vulgaris Effects of Pedunculagin from the Leaves of Quercus mongolica by Anti-Inflammatory Activity and 5α-Reductase Inhibition

Molecules ◽  
2020 ◽  
Vol 25 (9) ◽  
pp. 2154
Author(s):  
Min Kim ◽  
Jun Yin ◽  
In Hyeok Hwang ◽  
Dong Hui Park ◽  
Eun Kyeong Lee ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Leaf Extract ◽  
Acne Vulgaris ◽  
Positive Control ◽  
No Production ◽  
Quercus Mongolica ◽  
Main Compound ◽  
Inhibitory Activities

Quercus mongolica (QM)—a member of the Fagaceae family—has been used as traditional medicine in Korea, China and Mongolia as a treatment for inflammation of oral, genital or anal mucosa and for external inflammation of skin. To treat acne vulgaris (AV), we evaluated the inhibition of inflammatory cytokines (IL-6 and IL-8) of QM leaf extract (QML) and its main compound, pedunculagin (PD) in vitro and 5α-reductase inhibitory activity by western blotting. As results, QML and PD showed potent NO production inhibitory activity compared with the positive control (PC), NG-monomethyl-L-arginine (L-NMMA). QML and PD was also showed the decreases of IL-6 and IL-8 compared with the PC, EGCG and exhibited potent 5α-reductase type 1 inhibitory activities compared with the PC, dutasteride.

scholarly journals Anti-acne vulgaris effect including skin barrier improvement and 5α-reductase inhibition by tellimagrandin I from Carpinus tschonoskii

2019 ◽  
Vol 19 (1) ◽  
Author(s):  
Jun Yin ◽  
In Hyoek Hwang ◽  
Min Won Lee
Keyword(s):  
Mrna Expression ◽  
Inhibitory Activity ◽  
Acne Vulgaris ◽  
Skin Barrier ◽  
Positive Control ◽  
Skin Barrier Function ◽  
Rat Liver Microsomes ◽  
Dependent Manner ◽  
Inhibitory Activities ◽  
Anti Inflammatory

Abstract Background Carpinus tschonoskii (CT) has been previously studied for various activities in the improvement of skin diseases. In the present study, we examined the in vitro anti-acne vulgaris (AV) effect of CT leaves (CTL) and tellimagrandin I (TI), one of the main ellagitannins from CT, including skin barrier improvement and 5α-reductase inhibitory activity. Methods To test the anti-AV activities of CTL and TI, firstly, anti-oxidative and anti-inflammatory activities including DPPH radical scavenging activity, nitric oxide (NO) inhibitory activity, and cytokines [interleukin (IL)-6 and IL-8] were tested. Skin barrier improvement experiments were tested using developing cornified envelope (CE) formation, and filaggrin mRNA expression level was determined by RT-PCR. The 5α-reductase inhibitory activity was determined by measuring the testosterone levels in rat liver microsomes. Results CTL and TI showed potent anti-oxidative activity and anti-inflammatory activities. Especially, the cytokine production inhibitory activities of TI were found to be similar to the positive control, epigallocatechin gallate (EGCG). CTL and TI enhanced the CE formation and filaggrin mRNA expression levels and showed potent activities compared to that in the positive control, 1.5 mM Ca2+. In additionally, CTL and TI showed 5α-reductase inhibitory activities in a dose-dependent manner. Conclusion The results showed that CTL and TI inhibit AV endogenous factors such as 5α-reductase and inflammatory cytokines and affect exogenous factors such as developing skin barrier function (CE and filaggrin levels). Therefore, CTL and TI may be plant-derived agent, promising in the treatment of acne vulgaris.

scholarly journals SYNTHESIS OF ACETYL AND BENZOYL ESTERS OF XANTHORRHIZOL AND ITS OXIDATION PRODUCTS AND EVALUATION OF THEIR INHIBITORY ACTIVITY AGAINST NITRIC OXIDE PRODUCTION

2020 ◽  
pp. 135-138
Author(s):  
MAYA DAMAYANTI RAHAYU ◽  
SUSI KUSUMANINGRUM ◽  
HAYUN HAYUN
Keyword(s):  
Inhibitory Activity ◽  
Diclofenac Sodium ◽  
Positive Control ◽  
Oxidation Products ◽  
No Production ◽  
Raw 264.7 ◽  
Ic50 Values ◽  
Inhibitory Activities ◽  
Reduced Toxicity ◽  
Derivatives Of

Objective: Xanthorrhizol is known to have anti-inflammatory activity. However, new xanthorrhizol derivatives with improved anti-inflammatoryactivity and reduced toxicity are needed.Methods: In this study, the derivatives of xanthorrhizol were synthesized and spectroscopically characterized, and their inhibitory activities againstnitric oxide (NO) production were evaluated in RAW 264.7 macrophage cells.Results: The first stage of synthesis produced compounds 2a and 2b in 58.49% and 63.26% yields, respectively. Compounds 2a and 2b were oxidizedusing potassium permanganate, giving compounds 3a and 3b in yields of 51.92% and 43.78%, respectively. Compounds 1, 2a, 3a, and 3b alongwith diclofenac sodium (the positive control) exhibited IC50 values for NO production of 31.82, 73.85, 354.05, 97.19, and 78.43 μM, respectively. Incontrast, compound 2b did not show any inhibitory activity. Based on cytotoxicity assay, compounds 1, 2a, 2b, 3a, 3b, and diclofenac sodium had LD50values of 30.97, 65.15, 31.15, 117.86, 53.40, and 51.67 μM, respectively. The NO inhibitory activities of compounds 2a, 3a, and 3b were lower than thatof xanthorrhizol (compound 1). However, cytotoxicity tests showed that compounds 2a, 3a, and 3b had reduced toxicities compared to xanthorrhizol.Conclusion: The modification of xanthorrhizol through esterification and oxidation produced derivative compounds with weaker anti-inflammatoryactivity but reduced cytotoxicity.

Inhibitory effects of bioaccessible anthocyanins and procyanidins from apple, red grape, cinnamon on α-amylase, α-glucosidase and lipase

2020 ◽  
pp. 1-9
Author(s):  
Pınar Ercan ◽  
Sedef Nehir El
Keyword(s):  
Inhibitory Activity ◽  
Digestive Enzymes ◽  
Positive Control ◽  
Anthocyanin Content ◽  
Inhibitory Effects ◽  
Total Anthocyanin ◽  
Total Anthocyanin Content ◽  
Before And After ◽  
Red Grape

Abstract. The goals of this study were to determine and evaluate the bioaccessibility of total anthocyanin and procyanidin in apple (Amasya, Malus communis), red grape (Papazkarası, Vitis vinifera) and cinnamon (Cassia, Cinnamomum) using an in vitro static digestion system based on human gastrointestinal physiologically relevant conditions. Also, in vitro inhibitory effects of these foods on lipid (lipase) and carbohydrate digestive enzymes (α-amylase and α-glucosidase) were performed with before and after digested samples using acarbose and methylumbelliferyl oleate (4MUO) as the positive control. While the highest total anthocyanin content was found in red grape (164 ± 2.51 mg/100 g), the highest procyanidin content was found in cinnamon (6432 ± 177.31 mg/100 g) (p < 0.05). The anthocyanin bioaccessibilities were found as 10.2 ± 1%, 8.23 ± 0.64%, and 8.73 ± 0.70% in apple, red grape, and cinnamon, respectively. The procyanidin bioaccessibilities of apple, red grape, and cinnamon were found as 17.57 ± 0.71%, 14.08 ± 0.74% and 18.75 ± 1.49%, respectively. The analyzed apple, red grape and cinnamon showed the inhibitory activity against α-glucosidase (IC50 544 ± 21.94, 445 ± 15.67, 1592 ± 17.58 μg/mL, respectively), α-amylase (IC50 38.4 ± 7.26, 56.1 ± 3.60, 3.54 ± 0.86 μg/mL, respectively), and lipase (IC50 52.7 ± 2.05, 581 ± 54.14, 49.6 ± 2.72 μg/mL), respectively. According to our results apple, red grape and cinnamon have potential to inhibit of lipase, α-amylase and α-glucosidase digestive enzymes.

scholarly journals Ingol and Ingenol-Type Diterpenes from Euphorbia trigona Miller with Keratinocyte Inhibitory Activity

Plants ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 1206
Author(s):  
Reham Hammadi ◽  
Norbert Kúsz ◽  
Csilla Zsuzsanna Dávid ◽  
Zoltán Behány ◽  
László Papp ◽  
...  
Keyword(s):  
Liquid Chromatography ◽  
Cytotoxic Activity ◽  
Inhibitory Activity ◽  
High Performance ◽  
Skin Condition ◽  
Positive Control ◽  
Active Species ◽  
The European Union ◽  
Ingenol Mebutate

Ingenol mebutate, isolated from Euphorbia peplus, is an ingenane-type diterpenoid, primarily used for the topical treatment of actinic keratosis, a premalignant skin condition. The aim of our work was to investigate other Euphorbia species to find structurally similar diterpenes that can be used as alternatives to ingenol mebutate. Pharmacological investigation of Euphorbia candelabrum, Euphorbia cotinifolia, Euphorbia ramipressa, and Euphorbia trigona revealed the potent keratinocyte (HPV-Ker cell line) inhibitory activity of these spurge species. From the methanolic extract of the aerial parts of Euphorbia trigona Miller, the most active species, five ingol (1–5) and four ingenane-type diterpenoids (6–9) were isolated by various chromatographic separation techniques, including open column chromatography, vacuum liquid chromatography, thin-layer chromatography, and high-performance liquid chromatography. The structures of the compounds were determined by NMR spectroscopic analysis and by comparison of the assignations with the literature data. The cytotoxic activity of the compounds against keratinocytes was tested in vitro by using ingenol mebutate as a positive control. Among the isolated compounds, two ingenane derivatives (6 and 7) exhibited remarkably stronger cytotoxic activity (IC50 values 0.39 μM and 0.32 μM, respectively) on keratinocytes than ingenol mebutate (IC50 value 0.84 μM). These compounds could serve as starting materials for further investigations to find alternatives to Picato® (with active substance ingenol mebutate), which was withdrawn from marketing authorization in the European Union.

scholarly journals In VitroAntileukemic Activity ofXanthosoma sagittifolium(Taioba) Leaf Extract

2015 ◽  
Vol 2015 ◽  
pp. 1-10 ◽  
Author(s):  
Marina L. C. Caxito ◽  
Rachell R. Correia ◽  
Anne Caroline C. Gomes ◽  
Graça Justo ◽  
Marsen G. P. Coelho ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Leaf Extract ◽  
Leukemia Cells ◽  
No Production ◽  
3T3 Fibroblasts ◽  
Griess Reaction ◽  
Xanthosoma Sagittifolium ◽  
M Phase ◽  
Nih 3T3

Xanthosoma sagittifoliumSchott is a herb of the Araceae family, popularly known as taioba, which is consumed as food in some regions of Brazil, Africa, and Asia. This species has already been evaluated for the antifungal activities. However, based on its potential antitumor activity, the present study further aimed to examine the antitumor, as well as chelation, activity ofX. sagittifoliumleaf extract. Results showed that hydroethanolic extract ofX. sagittifoliumleaves (HEXs-L) exhibits cytotoxic effects against the immortalized line of human T-lymphocytic (Jurkat) and myelogenous (K562) leukemia cells, but not nontumor RAW 264.7 macrophages or NIH/3T3 fibroblasts. HEXs-L inhibited 50.3% of Jurkat cell proliferation, reducing by 20% cells in G2/M phase, but increasing cells in sub-G1 phase, thereby inducing apoptosis by 54%. In addition, HEXs-L inhibited NO production by 59%, as determined by Griess reaction, and chelated 93.8% of free Fe(II), as demonstrated by ferrozine assay. Phytochemical studies were carried out by ESI-MS, identifying apigenin di-C-glycosides as major compounds. Overall, this work revealed that leaf extract ofXanthosoma sagittifoliumpresented chelating activity andin vitroantitumor activity, arresting cell cycle and inducing apoptosis of leukemia cells, thus providing evidence that taioba leaves may have practical application in cancer therapy.

In Vitro HIV Type-1 Reverse Transcriptase Inhibitory Activity from Leaf Extracts ofScoparia dulcisL.

2009 ◽  
Vol 15 (3) ◽  
pp. 241-247 ◽  
Author(s):  
Mahendar Porika ◽  
Mahender Aileni ◽  
Venugopal Rao Kokkirala ◽  
Kranthi Gadidasu ◽  
Pavan Umate ◽  
...  
Keyword(s):  
Reverse Transcriptase ◽  
Inhibitory Activity ◽  
Leaf Extracts ◽  
Hiv Type 1

scholarly journals In vivo hypotensive effect and in vitro inhibitory activity of some Cyperaceae species

2013 ◽  
Vol 49 (4) ◽  
pp. 803-809
Author(s):  
Monica Lacerda Lopes Martins ◽  
Henrique Poltronieri Pacheco ◽  
Iara Giuberti Perini ◽  
Dominik Lenz ◽  
Tadeu Uggere de Andrade ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Colorimetric Assay ◽  
Hypotensive Effect ◽  
Ace Inhibition ◽  
Inhibitory Effect ◽  
Positive Control ◽  
Total Phenolic ◽  
Before And After

In 1820, French naturalist August Saint Hillaire, during a visit in Espírito Santo (ES), a state in southeastern Brazil, reported a popular use of Cyperaceae species as antidote to snake bites. The plant may even have a hypotensive effect, though it was never properly researched. The in vitro inhibitory of the angiotensin converting enzyme (ACE) activity of eigth ethanolic extracts of Cyperaceae was evaluated by colorimetric assay. Total phenolic and flavonoids were determined using colorimetric assay. The hypotensive effect of the active specie (Rhychonospora exaltata, ERE) and the in vivo ACE assay was measured in vivo using male Wistar Kyoto (ERE, 0.01-100mg/kg), with acetylcholine (ACh) as positive control (5 µg/kg, i.v.). The evaluation of ACE in vivo inhibitory effect was performed comparing the mean arterial pressure before and after ERE (10 mg/kg) in animals which received injection of angiotensin I (ANG I; 0,03, 03 and 300 µg/kg, i.v.). Captopril (30 mg/kg) was used as positive control. Bulbostylis capillaris (86.89 ± 15.20%) and ERE (74.89 ± 11.95%, ERE) were considered active in the in vitro ACE inhibition assay, at 100 µg/mL concentration. ACh lead to a hypotensive effect before and after ERE's curve (-40±5% and -41±3%). ERE showed a dose-dependent hypotensive effect and a in vivo ACE inhibitory effect. Cyperaceae species showed an inhibitory activity of ACE, in vitro, as well as high content of total phenolic and flavonoids. ERE exhibited an inhibitory effect on both in vitro and in vivo ACE. The selection of species used in popular medicine as antidotes, along with the in vitro assay of ACE inhibition, might be a biomonitoring method for the screening of new medicinal plants with hypotensive properties.

scholarly journals Skrining Mekanisme Kerja Daun Malaka (Phyllanthus emblica L.) Sebagai Antidiabetes

2018 ◽  
Vol 1 (3) ◽  
pp. 106-110
Author(s):  
Novi Irwan Fauzi ◽  
Seno Aulia Ardiansyah ◽  
Saeful Hidayat
Keyword(s):  
Mechanism Of Action ◽  
Inhibitory Activity ◽  
Leaf Extract ◽  
Test Method ◽  
Diabetic Rat ◽  
Phyllanthus Emblica ◽  
Insulin Sensitizer ◽  
Water Fraction

Daun malaka (Phyllanthus emblica L.) mempunyai potensi digunakan sebagai alternatif obat antidiabetes. Daun malaka menunjukkan efek hipoglikemia pada tikus yang diinduksi aloksan. Namun, mekanisme kerjanya belum diketahui pasti. Penelitian ini dilakukan dalam rangka skrining mekanisme kerja daun malaka sebagai antidiabetes. Skrining mekanisme kerja dilakukan terhadap fraksi air daun malaka melalui uji aktivitas inhibisi enzim α-glukosidase serta α-amilase secara in vitro dan pengujian aktivitas insulin-sensitizer terhadap ekstrak daun malaka dengan metode tes toleransi insulin secara in vivo. Fraksi air daun malaka menunjukkan aktivitas inhibisi terhadap enzim α-glukosidase serta α-amilase dengan nilai IC50 (Inhibitor Concentration 50) pada kedua enzim tersebut berturut-turut adalah 0,87% dan 8,64% b/v. Pada uji aktivitas insulin sensitizer, pemberian ekstrak daun malaka dapat meningkatkan sensitivitas insulin pada tikus diabet dengan kondisi resistensi insulin. Nilai KTTI pada kelompok tikus diabet yang diberi ekstrak daun malaka dosis 100 dan 500 mg/kgbb tikus (74,89 dan 75,57) lebih tinggi dibandingkan kelompok tikus diabet (38,41) dan kadar glukosa darah yang lebih rendah selama interval waktu pengukuran. Daun malaka telah diketahui mampu meningkatkan sekresi insulin dan pada penelitian ini menunjukkan aktivitas inhibisi enzim α-glukosidase serta α-amilase secara in vitro dan menunjukkan aktivitas insulinsensitizer pada tikus diabet dengan kondisi resistensi insulin.   Malaka leaf (Phyllanthus emblica L.) has the potential to be used as an alternative antidiabetic drug. Malacca leaves showed hypoglycemia effect in rat induced by alloxan. However, the mechanism of action is not yet known. This study was conducted to evaluate the mechanism of action of Malaka leaves as antidiabetic. Screening of the mechanism of action was carried out on the water fraction of Malaka leaf  byinhibitory activity examination  on α-glucosidase and α-amylase by in vitro studyand Evaluation of insulin-sensitizer activity of Maaka leaf leaf extract was conducted by invivo  insulin tolerance test method. Malaka leaf water fraction showed inhibitory activity against the α-glucosidase and α-amylase with IC50 values ​​(Inhibitory Concentration 50)  of0.87% and 8.64% b / v on both enzyme, respectively. The evaluation of insulin sensitizer revelead that administration ofMalaka  leaf extract can increase insulin sensitivity in diabetic rat with insulin resistance.KTTI values ​​in diabetic rats given malaka extract  at the dose of 100 and 500 mg / kg BW (74.89 and 75.57) were higher than diabetics rat (38.41) and the extract also decrease blood glucose levels during measurement time intervals . Malaka leafhas been known to increase insulin secretion and the study showedthe  inhibitory activity on α-glucosidase and α-amylase by in vitro study and showed insulinsensitizer activity in diabetic rat with insulin resistance.

scholarly journals Artemisinin-independent inhibitory activity of Artemisia sp. infusions against different Plasmodium stages including relapse-causing hypnozoites

2021 ◽  
Vol 5 (3) ◽  
pp. e202101237
Author(s):  
Kutub Ashraf ◽  
Shahin Tajeri ◽  
Christophe-Sébastien Arnold ◽  
Nadia Amanzougaghene ◽  
Jean-François Franetich ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Plasmodium Falciparum ◽  
Inhibitory Activity ◽  
Parasite Species ◽  
Artemisia Annua ◽  
Combination Therapies ◽  
Lead Compounds ◽  
Low Concentrations ◽  
Inhibitory Activities

Artemisinin-based combination therapies (ACT) are the frontline treatments against malaria worldwide. Recently the use of traditional infusions from Artemisia annua (from which artemisinin is obtained) or Artemisia afra (lacking artemisinin) has been controversially advocated. Such unregulated plant-based remedies are strongly discouraged as they might constitute sub-optimal therapies and promote drug resistance. Here, we conducted the first comparative study of the anti-malarial effects of both plant infusions in vitro against the asexual erythrocytic stages of Plasmodium falciparum and the pre-erythrocytic (i.e., liver) stages of various Plasmodium species. Low concentrations of either infusion accounted for significant inhibitory activities across every parasite species and stage studied. We show that these antiplasmodial effects were essentially artemisinin-independent and were additionally monitored by observations of the parasite apicoplast and mitochondrion. In particular, the infusions significantly incapacitated sporozoites, and for Plasmodium vivax and P. cynomolgi, disrupted the hypnozoites. This provides the first indication that compounds other than 8-aminoquinolines could be effective antimalarials against relapsing parasites. These observations advocate for further screening to uncover urgently needed novel antimalarial lead compounds.

scholarly journals Phytochemical evaluation and in vitro antidiabetic efficiency of isopropanolic leaf extract of pimenta racemosa

2020 ◽  
Vol 7 (2) ◽  
pp. 50-55
Author(s):  
Anitha T A ◽  
Pakutharivu T ◽  
Nirubama K ◽  
Akshaya V
Keyword(s):  
Diabetes Mellitus ◽  
Glucose Uptake ◽  
Inhibitory Activity ◽  
Leaf Extract ◽  
Yeast Cells ◽  
Antidiabetic Activity ◽  
Leaf Extracts ◽  
Pimenta Racemosa

The traditional herbal medicines are mainly obtained from plants are used in the management of Diabetes mellitus. The main objective of this work was to assess the presence of phytochemical compounds and to evaluate the in vitro antidiabetic activity of isopropanolic extracts of Pimenta racemosa leaves by studying their α-amylase inhibitory activity and glucose transport across yeast cells. Screening of phytochemicals showed positive results for alkaloids, steroids, cardiac glycosides, terpenoids, reducing sugars, anthraquinones, and results of in vitro α-amylase inhibitory studies demonstrated there was a dose-dependent increase in percentage inhibitory activity by the isopropanolic leaf extracts of Pimenta racemosa. At a concentration of 1 mg/ml, the extract showed a percentage inhibition 33.6 and for 5 mg/ml it was 91.2. The glucose uptake study was also studied through yeast cells by analyzing theamount of glucose remaining in the medium after a specific time intervals. It serves as an indicator for the capability of isopropanolic leaf extracts of Pimenta racemosa to transport the glucose into yeast cells. As a result, we found that the isopropanolic leaf extract of Pimenta racemosa have inhibitory activity against αamylase and also, which is efficient in glucose uptake. This therapeutic potentiality of Pimenta racemosa could be exploited in the treatment of Type 2 Diabetes mellitus. Further studies are also required to elucidate whether the plant have antidiabetic potential by in vivo for corroborating the traditional claim of the plant.

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