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1.
BMC Complement Med Ther ; 24(1): 159, 2024 Apr 12.
Artículo en Inglés | MEDLINE | ID: mdl-38609961

RESUMEN

BACKGROUND: Polyalthia suberosa (Roxb.) Thwaites (Annonaceae) is a medicinal plant that has been reported for its various pharmacological potentials, such as its anti-inflammatory, analgesic, antioxidant, and neuropharmacological activities. This study aimed to analyze the leaf essential oils of P. suberosa (PSLO) collected in different seasons, to evaluate the acetylcholinesterase inhibitory activity, and to corroborate the obtained results via in-silico molecular docking studies. METHODS: The leaf essential oils of P. suberosa collected in different seasons were analyzed separately by GC/MS. The acetylcholinesterase inhibitory activity of the leaves oil was assessed via colorimetric assay. In-silico molecular docking studies were elucidated by virtual docking of the main compounds identified in P. suberosa leaf essential oil to the active sites in human acetylcholinesterase crystal structure. RESULTS: A total of 125 compounds were identified where D-limonene (0.07 - 24.7%), α-copaene (2.25 - 15.49%), E-ß-caryophyllene (5.17 - 14.42%), 24-noroleana-3,12-diene (12.92%), ß-pinene (0.14 - 8.59%), and α-humulene (2.49-6.9%) were the most abundant components. Results showed a noteworthy influence of the collection season on the chemical composition and yield of the volatile oils. The tested oil adequately inhibited acetylcholinesterase enzyme with an IC50 value of 91.94 µg/mL. Additionally, in-silico molecular docking unveiled that palmitic acid, phytol, p-cymene, and caryophyllene oxide demonstrated the highest fitting scores within the active sites of human acetylcholinesterase enzyme. CONCLUSIONS: From these findings, it is concluded that P. suberosa leaf oil should be evaluated as a food supplement for enhancing memory.


Asunto(s)
Aceites Volátiles , Polyalthia , Humanos , Estaciones del Año , Acetilcolinesterasa , Aceites Volátiles/farmacología , Simulación del Acoplamiento Molecular , Antiinflamatorios no Esteroideos
2.
J Ethnopharmacol ; 326: 117922, 2024 May 23.
Artículo en Inglés | MEDLINE | ID: mdl-38403004

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Kidney problems are becoming more common globally and are considered a major health issue in the modern world with high mortality rate. Polyalthia longifolia (Sonn.) Thwaites is a tropical ethnomedicinal plant used to treat various diseases like diabetes, hypertension and urinary disorders and possess antioxidant and anti-inflammatory properties. AIM OF THE STUDY: This study aimed to investigate the phytochemical composition of 70% ethanolic leaf extract of Polyalthia longifolia (Sonn.) Thwaites (PL) and evaluates its nephroprotective effects against cisplatin-induced nephrotoxicity in Wistar rats. MATERIALS AND METHODS: The leaves of PL were extracted with 70% ethanol and performed the phytochemical profiling using Liquid Chromatography-Mass Spectrometry (LC-MS). The nephroprotective effect of PL leaf extract was evaluated at three doses (150, 300 and 600 mg/kg, p.o.) for 14 days against cisplatin toxicity (16 mg/kg, i.p., once) in male Wistar rats. Body and kidney weight indices, kidney function markers and lipid profile markers in serum, and oxidative stress markers in kidney tissue were performed along with the histopathological analysis of kidney. RESULTS: The LC-MS chromatograph confirmed the presence of various phytocompounds include N-Methylhernagine (aporphine alkaloid), 4-Acetamidobutanoic acid (gamma amino acid) and choline, etc. in the PL leaf extract. Exposure of cisplatin (16 mg/kg, i.p., once only) to the animals significantly elevated the levels of kidney functional markers (i.e. serum urea, uric acid, creatinine) and the lipid markers (triglyceride and total cholesterol) in blood circulation with depletion of serum albumin which were reversed by the therapy of PL leaf extract (150, 300 and 600 mg/kg) in dose-dependent manner. The altered level of body and kidney weight in cisplatin treated group was also restored by the therapy. PL leaf extract effectively improved the antioxidant defense system of kidney at all doses by restoring the levels of tissue glutathione, superoxide dismutase, catalase, glutathione peroxidase and glutathione reductase with the dose-dependent reduction of lipid peroxidation against cisplatin-induced renal oxidative stress. The histopathological observations also showed the significant recovery in cellular morphology after PL treatment when compared to the cisplatin toxicity group. The highest dose 600 mg/kg of PL leaf extract showed more pronounced renal recovery (p < 0.001) followed by other two doses, which was similar to the silymarin treatment group (a reference drug) against nephrotoxicity. CONCLUSION: The results of this study revealed the nephroprotective effects of PL leaves against cisplatin-induced nephrotoxicity by reversing the level of biochemical markers and mitigating oxidative stress as well as improving the architecture of renal tissues. This renal protection by PL might be due to the synergistic effect of its phytoconstituents and antioxidant efficacy.


Asunto(s)
Cisplatino , Polyalthia , Ratas , Animales , Cisplatino/toxicidad , Antioxidantes/uso terapéutico , Ratas Wistar , Estrés Oxidativo , Riñón , Etanol/farmacología , Creatinina , Extractos Vegetales/uso terapéutico , Fitoquímicos/farmacología , Fitoquímicos/metabolismo , Lípidos/farmacología
3.
Environ Res ; 246: 118061, 2024 Apr 01.
Artículo en Inglés | MEDLINE | ID: mdl-38157967

RESUMEN

This research was performed to investigate the bactericidal and fungicidal competence of extracts (methanol and petroleum ether extract) of Polyalthia longifolia leaf. Moreover, the major active compounds present in the effective crude extract (either methanol or petroleum ether extract) was determined through initially with UV-Vis spectra, FTIR, and GC-MS analyses. The methanol extract alone showed remarkable bactericidal and fungicidal activity against the bacterial (S. pyogenes > E. coli > S. aureus > S. pneumoniae > C. difficile > P. aeruginosa) and fungal (A. clavatus > C. albicans > A. niger > A. fumigatus > C. tropicalis > C. auris) pathogens at increased concentration (12.5 mg mL-1) than petroleum ether extract. The MIC and MBC values of methanol extract were found as 10-20 mg mL-1 and 30-40 mg mL-1 respectively. The MFC value of methanol extract was found as 10-20 mg mL-1. These MIC, MBC, and MFC values of methanol extract were considerably greater than petroleum ether extract. The FTIR and GC-MS characterization studies revealed that the presence of more acre functional groups belonging to bioactive compounds such as Z)-7-Hexadecenal, Aromandendrene, α-Curcumene, Caryophyllene, Methyl 14-methyl Pentadecanoat, Methyl trans-13-Octadecenoate, 9-Octadecenoic acid (Z)-, and 2-hydroxy-1- (hydroxymethyl)ethyl. As a result of these findings, it is possible that P. longifolia leaf methanol extract contains medicinally important bioactive substances with bactericidal and fungicidal properties.


Asunto(s)
Alcanos , Antiinfecciosos , Clostridioides difficile , Fungicidas Industriales , Polyalthia , Extractos Vegetales/farmacología , Metanol , Escherichia coli , Staphylococcus aureus , Antiinfecciosos/farmacología , Antibacterianos/farmacología , Solventes , Candida albicans
4.
Microsc Microanal ; 29(3): 1153-1167, 2023 06 09.
Artículo en Inglés | MEDLINE | ID: mdl-37749670

RESUMEN

The present study investigated the effects of Polyalthia longifolia leaf extract against the growth of HeLa cell xenograft tumor in nude mice and its underlying mechanism. The nude mice xenografted with HeLa cells were treated with 5% DMSO (vehicle control), 20 mg/kg/body weight of etoposide (positive control), and 500 and 1000 mg/kg/body weight of leaf extract, respectively. Antitumor activity was evaluated with apoptosis, proliferation, and angiogenesis using microscopic-based histological and immunohistochemical microanalyses. The tumor tissue histological and immunohistochemical analyses showed that the HeLa tumor cell death was associated with apoptosis and decreased (p < 0.05) expression of Ki-67 in tumor tissues. The extract also inhibits tumor angiogenesis by downregulating (p < 0.05) the expression of VEGF and CD31 in tumor tissues after treatment for 35 days. Conclusively, the P. longifolia leaf extract effectively inhibited HeLa cell xenograft growth in nude mice. The possible mechanism was related to induction of apoptosis, inhibition of tumor HeLa cell proliferation by decreasing the Ki-67 protein expression, and prevention of tumor angiogenesis by reducing VEGF and CD31 protein expression in HeLa cells.


Asunto(s)
Polyalthia , Animales , Ratones , Humanos , Xenoinjertos , Células HeLa , Ratones Desnudos , Antígeno Ki-67 , Factor A de Crecimiento Endotelial Vascular , Peso Corporal , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico
5.
Fitoterapia ; 170: 105626, 2023 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-37516404

RESUMEN

Obesity-related metabolic disorders are increasing at an alarming rate worldwide. The FDA has approved many molecules for weight loss therapy; most of them act on the gut level by inhibiting lipid uptake or on the central nervous system by controlling appetite. Limitations and drawbacks have propelled the search for new pharmacophores exhibiting favourable metabolic alteration at adipocytes, and natural products have always been there to prove their worth. In our efforts, we have identified 16-hydroxy-ent-halima-5(10),13-dien-15,16-olide (PLH), a halimane diterpene isolated from Polyalthia longifolia, demonstrating anti-adipogenic and anti-dyslipidemic activity. It inhibited adipogenesis in 3T3-L1 preadipocyte and C3H10T1/2 mesenchymal stem cell lines. Furthermore, it decreased set of adipogenic markers at transcript and protein levels. Cell cycle studies indicated that PLH halts the mitotic clonal expansion. Mechanistic studies shows that PLH activate Wnt/ß-catenin signaling pathway to inhibit the adipogenesis. The study suggested that PLH inhibited adipogenesis during the early phase of differentiation by targeting mitotic clonal expansion and arresting the cell cycle in the G1 phase of the cell cycle. It improved the dyslipidemic condition in HFD-fed hamsters by decreasing the body weight, fat mass, eWAT weight and improving the serum lipid profile. Overall, PLH has been found as a potential drug candidate and a pharmacophore for combating metabolic disorders including obesity and dyslipidemia.


Asunto(s)
Dislipidemias , Polyalthia , Cricetinae , Animales , Humanos , Ratones , Adipogénesis , Estructura Molecular , Diferenciación Celular , Obesidad/tratamiento farmacológico , Dislipidemias/tratamiento farmacológico , Lípidos , Células 3T3-L1
6.
J Ethnopharmacol ; 290: 115110, 2022 May 23.
Artículo en Inglés | MEDLINE | ID: mdl-35181488

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Polyalthia longifolia var. angustifolia Thw. (Annonaceae) is commonly used in traditional medicine as a tonic for rejuvenation and exhibiting good antioxidant activities. AIM OF THE STUDY: To evaluate P. longifolia methanolic leaf extract (PLME) antiaging activity at 1 mg/mL in Saccharomyces cerevisiae BY611 yeast. MATERIALS AND METHODS: The antiaging effect of PLME was studied via replicative lifespan assay, antioxidative stress assays, reactive oxygen species (ROS) determination, reduced glutathione (GSH) determination, superoxide dismutase (SOD) and Sirtuin 1 (SIRT1) genes regulation studies and SOD and SIRT1 proteins activities. RESULTS: The PLME treatment increased the growth and prolonged the lifespan of the yeast significantly (p < 0.05) compared to the untreated yeast group. Besides, the PLME also protected the yeast from oxidative stress induced by 4-mM-H2O2 via decreasing (p < 0.05) the ROS from 143.207 to 127.223. The antioxidative action of PLME was proved by spot assay. Phloxine B staining was further confirmed the PLME antioxidative action of PLME, where more whitish-pink live yeast cells were observed. In addition, the PLME also enhanced GSH content significantly (p < 0.05) in yeast treated with PLME from 16.81 to 25.31 µmol. Furthermore, PLME increased the SOD and SIRT1 genes expression significantly (p < 0.05) with ΔCt values of 1.11 and 1.15, respectively. The significantly (p < 0.05) elevated SOD and SIRT1 protein activities were recorded as 51.54 U/mg Prot and 1716 ng/mL, respectively. CONCLUSIONS: PLME exhibited good antiaging activities in S. cerevisiae, by modulating oxidative stress, enhancing GSH content, and increasing SOD and SIRT1 genes expression.


Asunto(s)
Envejecimiento/efectos de los fármacos , Antioxidantes/farmacología , Extractos Vegetales/farmacología , Polyalthia/química , Polifenoles/farmacología , Saccharomyces cerevisiae/efectos de los fármacos , Estrés Oxidativo/efectos de los fármacos , Sirtuina 1/efectos de los fármacos , Superóxido Dismutasa/efectos de los fármacos
7.
Nat Prod Res ; 36(16): 4187-4192, 2022 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-34491152

RESUMEN

Renoprotectors are highly demanded due to environmental nephrotoxic factors. P. longifolia leaves extract alleviating effect was assessed in nephritic-induced rats by whole body shot dose of γ-radiation. Many biomarkers were detected using several assays. Renohistopathological examinations were performed. Moreover, the extract phytoconstituents were identified using spectroscopic analysis. In-vitro anti-inflammatory activity of some compounds was examined using histamine release assay. Post-irradiation treatment with the extract significantly ameliorated all elevated biomarker levels. Creatinine and urea were adjusted, TGF-ß/Smad signaling was suppressed causing down-regulation to microRNA-21. Nitric oxide, reactive oxygen species, glutathione and kidney injury molecule-1 were normalized in comparison with the γ-irradiated group. The renohistopathological analysis was consistent with the biochemical study. Phytochemical analysis resulted in the isolation of two diterpenoids (γ-methoxybutenolide clerodane diterpene and 16(R/S)-hydroxycleroda-3,13-dien-16,15-olide-2-one), aporphine alkaloid (anonaine) and flavonol (kaempferol-3-O-rutinoside). The latter two showed moderate anti-histaminic activities. Our results indicated that P. longifolia reduced oxidative stress and nephropathy in rats due to its anti-inflammatory principles.


Asunto(s)
Diterpenos de Tipo Clerodano , MicroARNs , Nefritis , Polyalthia , Animales , Antiinflamatorios/farmacología , Diterpenos de Tipo Clerodano/química , Nefritis/tratamiento farmacológico , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Polyalthia/química , Ratas , Factor de Crecimiento Transformador beta
8.
Pak J Pharm Sci ; 35(6(Special)): 1691-1698, 2022 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-36861230

RESUMEN

Isolation of sodium and potassium salt of kolavenic acid (1,2), as a mixture of (3:1) and sodium and potassium salt of 16 oxo-cleroda-3,13(14) E-dien-15-oic acid (3, 4) as a mixture of (1:1) are first time reported form reddish black ripe and green unripe berries of Polyalthia longifolia var. pendula respectively. Three known constituents obtained, were identified as cleroda-3, 13(14) E-dien-15-oic acid (kolavenic acid) (5), 16(R and S)-hydroxy cleroda-3,13 (14)Z-dien-15,16-olide (6) and 16 oxo-cleroda-3,13(14) E-dien-15-oic acid (7). Structures of all these compounds have been determined through spectral studies while metal analyses were carried out to confirm the structure of the salts. Compounds 3, 4 and 7 possess cytotoxic activity against lung (NCI-H460), oral (CAL-27) and normal mouse fibroblast (NCI-3T3) cancer cell lines. Diterpenoid (7), a bioprivileged, compound shows potent cytotoxic activity against oral cancer cell line (CAL-27) with IC50 11.3±0.6µg/mL in comparison with the standard 5-flourouracil (IC50 12.7±0.1µg/mL) and lungs cancer cell lines (NCI-H460) with IC50 5.3±0.2µg/mL as compared to the standard drug cisplatin (IC50 5.7±0.2µg/mL).


Asunto(s)
Annonaceae , Antineoplásicos , Diterpenos de Tipo Clerodano , Plantas Medicinales , Polyalthia , Animales , Ratones , Diterpenos de Tipo Clerodano/farmacología , Sales (Química) , Antineoplásicos/farmacología , Potasio
9.
J Cancer Res Ther ; 17(6): 1339-1346, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-34916363

RESUMEN

AIMS: The aim was to compare the anticancer and antimutagenic potency of Polyalthia cerasoides seeds and stem bark. AIM OF THE STUDY: The aim of this study was to investigate the antiproliferative, apoptotic, antioxidation to DNA, and antimutagenic activity of alcoholic (PS-1 and PS-3) and petroleum ether (PS-2 and PS-4) stem bark and seed fractions of P. cerasoides. METHODS: P. cerasoides stem bark and seeds were extracted with ethanol: water mixture (9:1 ratio v: v) and fractionated with petroleum ether. Fractions were investigated for antiproliferative effect using cell by 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide, a tetrazole assay (cell line used liver [HepG2] and cervical [HeLa] cancer cell lines), DNA damage protection using hydroxyl radical and antimutagenic effect using chromosome aberration test. RESULTS: PS-1 (IC50 10 µg/ml) and PS-3 (IC50 11 µg/ml) showed maximum antiproliferative activity against HepG2 cell lines, whereas, PS-1 (IC50 10 µg/ml), PS-2 (IC50 24 µg/ml), and PS-3 (IC50 11 µg/ml) showed better antiproliferative activity against HeLa cell lines. PS-3 and PS-4 were protective against oxidation to the supercoiled DNA molecule. Further, petroleum ether extract of both seed (PS-2) and stem bark (PS-4) showed good antimutagenicity as revealed by the less chromosomal aberrations compared to PS-1 and PS-3 fractions. CONCLUSIONS: This study demonstrated the beneficial effect of fractions against oxidation of DNA, antiproliferative, apoptotic, and antimutagenic activity. Probably, this property would be attributable by their phenolic and steroid constituents. Therefore, this plant could be used as a potential source of nutraceutical agents.


Asunto(s)
Antimutagênicos/farmacología , Antineoplásicos/farmacología , Neoplasias/tratamiento farmacológico , Corteza de la Planta/química , Extractos Vegetales/farmacología , Polyalthia/química , Semillas/química , Animales , Apoptosis , Proliferación Celular , Etanol/química , Células HeLa , Células Hep G2 , Humanos , Ratones , Neoplasias/patología
10.
J Agric Food Chem ; 69(36): 10527-10535, 2021 Sep 15.
Artículo en Inglés | MEDLINE | ID: mdl-34469148

RESUMEN

In the search for new natural resources showing plant disease control effects, we found that the methanol extract of Polyalthia longifolia suppressed fungal disease development in plants. To identify the bioactive substances, the methanol extract of P. longifolia was extracted by organic solvents, and consequently, four new 2-oxo-clerodane diterpenes (1-4), a new 4(3 → 2)-abeo-clerodane diterpene (5), together with ten known compounds (6-16) were isolated and identified from the extracts. Of the new compounds, compound 2 showed a broad spectrum of antifungal activity with moderated minimum inhibitory concentration (MIC) values in a range of 50-100 µg/mL against tested fungal pathogens. Considering with the known compounds, compound 6 showed the most potent antifungal activity with an MIC value in the range of 6.3-12.5 µg/mL. When compound 6 was evaluated for an in vivo antifungal activity against rice blast, tomato late blight, and pepper anthracnose, compound 6 reduced the plant disease by at least 60% compared to the untreated control at concentrations of 250 and 500 µg/mL. Together, our results suggested that the methanol extract of twigs and leaves of P. longifolia and its major compound 6 could be used as a source for the development of eco-friendly plant protection agents.


Asunto(s)
Diterpenos de Tipo Clerodano , Polyalthia , Antifúngicos/farmacología , Diterpenos de Tipo Clerodano/farmacología , Pruebas de Sensibilidad Microbiana , Extractos Vegetales/farmacología , Hojas de la Planta
11.
Molecules ; 26(17)2021 Sep 03.
Artículo en Inglés | MEDLINE | ID: mdl-34500802

RESUMEN

Polyalthia belong to the Annonaceae family and are a type of evergreen tree distributed across many tropical and subtropical regions. Polyalthia species have been used long term as indigenous medicine to treat certain diseases, including fever, diabetes, infection, digestive disease, etc. Recent studies have demonstrated that not only crude extracts but also the isolated pure compounds exhibit various pharmacological activities, such as anti-oxidant, anti-microbial, anti-tumor, anti-cancer, etc. It is known that the initiation of cancer usually takes several years and is related to unhealthy lifestyle, as well as dietary and environmental factors, such as stress, toxins and smoking. In fact, natural or synthetic substances have been used as cancer chemoprevention to delay, impede, or even stop cancer growing. This review is an attempt to collect current available phytochemicals from Polyalthia species, which exhibit anti-cancer potentials for chemoprevention purposes, providing directions for further research on the interesting agents and possible clinical applications.


Asunto(s)
Antiinflamatorios/farmacología , Antineoplásicos Fitogénicos/farmacología , Antioxidantes/farmacología , Fitoquímicos/farmacología , Polyalthia/química , Antiinflamatorios/química , Antiinflamatorios/aislamiento & purificación , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/aislamiento & purificación , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Humanos , Estructura Molecular , Fitoquímicos/química , Fitoquímicos/aislamiento & purificación
12.
PLoS One ; 16(6): e0253572, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-34191831

RESUMEN

In the present study, in silico predictions and molecular docking were performed on five clerodane diterpenes (1-5) from Polyalthia longifolia seeds to evaluate their potential as xanthine oxidase (XO) inhibitors. The initial screening was conducted by target prediction using TargetNet web server application and only compounds 3 and 4 showed a potential interaction with XO. Compounds 3 and 4 were subsequently subjected to in silico analyses on XO protein structure (PDB: 1N5X) using Schrödinger Release 2020-3 followed by structural modeling & molecular simulation studies to confirm the initial prediction result and identify the binding mode of these compounds to the XO. Molecular docking results revealed that compounds 3 (-37.3 kcal/mol) and 4 (-32.0 kcal/mol) binds more stably to XO than the reference drug allopurinol (-27.0 kcal/mol). Interestingly, two residues Glu 802 and Thr 1010 were observed as the two main H-bond binding sites for both tested compounds and the allopurinol. The center scaffold of allopurinol was positioned by some π-π stacking with Phe 914 and Phe 1009, while that of compounds 3 and 4 were supported by many hydrophobic interactions mainly with Leu 648, Phe 649, Phe 1013, and Leu 1014. Additionally, the docking simulation predicted that the inhibitory effect of compounds 3 and 4 was mediated by creating H-bond with particularly Glu 802, which is a key amino acid for XO enzyme inhibition. Altogether, in vitro studies showed that compounds 3 and 4 had better inhibitory capacity against XO enzyme with IC50 values significantly (p < 0.001) lower than that of allopurinol. In short, the present study identified cleroda-4(18),13-dien-15,16-olide as novel potential XO inhibitors, which can be potentially used for the treatment of gout.


Asunto(s)
Diterpenos de Tipo Clerodano/farmacología , Extractos Vegetales/farmacología , Polyalthia/química , Xantina Oxidasa/antagonistas & inhibidores , Diterpenos de Tipo Clerodano/química , Diterpenos de Tipo Clerodano/aislamiento & purificación , Pruebas de Enzimas , Gota/tratamiento farmacológico , Gota/metabolismo , Humanos , Simulación del Acoplamiento Molecular , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Semillas/química , Ácido Úrico/metabolismo , Xantina Oxidasa/química , Xantina Oxidasa/metabolismo
13.
Nat Prod Res ; 35(23): 5282-5286, 2021 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-32363939

RESUMEN

Phytochemical studies of methylene chloride soluble fraction from the 70% aqueous-alcoholic extract of Polyalthia longifolia (leaves) resulted in the isolation of two known clerodane diterpenes, namely: 16α-hydroxycleroda-3,13(14)-dien-16,15-olide (1) and (4→2)-abeo-16-hydroxy-cleroda-2,13(14)-dien-15,16-olide-3-al (2). The isolated compounds were evaluated for their anti-histaminic and anti-Helicobacter pylori activities. Compound 1 was more potent than 2 with IC50 29.7 µg/mL and 189.2 µg/mL in the anti-histaminic assay and MIC equals to 31.25 µg/mL and 125 µg/mL in the anti-H. pylori assay, as compared with diclofenac (IC50 = 17.9 µg/mL) and clarithromycin (MIC = 1.95 µg/mL), respectively. The differences in their structures, as well as their activity results, indicated important characteristic features necessary for activity. It was suggested that the decalin moiety in 1 was important for both activities. On the other hand, the (4→2)-abeo migration in 2 reduced both activities. The potent activities of 1 suggest its potential application as an anti-histaminic and antimicrobial agent.


Asunto(s)
Diterpenos de Tipo Clerodano , Diterpenos , Helicobacter pylori , Polyalthia , Diterpenos de Tipo Clerodano/farmacología , Extractos Vegetales/farmacología , Hojas de la Planta
14.
Fitoterapia ; 147: 104734, 2020 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-33007399

RESUMEN

Two new C31 triterpenes, polysimiaric acid A (1) and B (2) as well as one new clerodane diterpenoid, 16,16-dimethoxy-cleroda-3,13Z-dien-15-oic acid (3), together with six known compounds were isolated from Polyalthia simiarum. Their structures were determined by analysis of 1D and 2D NMR data. Three new compounds were tested for their cytotoxicity against five human tumour cell lines. Compound 3 showed cytotoxic activities against SMMC-7721 with the IC50 value of 22.43 µM.


Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Diterpenos de Tipo Clerodano/farmacología , Polyalthia/química , Terpenos/farmacología , Antineoplásicos Fitogénicos/aislamiento & purificación , Línea Celular Tumoral , China , Diterpenos de Tipo Clerodano/aislamiento & purificación , Humanos , Estructura Molecular , Hojas de la Planta/química , Terpenos/aislamiento & purificación
15.
Sci Rep ; 10(1): 15965, 2020 09 29.
Artículo en Inglés | MEDLINE | ID: mdl-32994508

RESUMEN

Natural metabolites with their specific bioactivities are being considered as a potential source of materials for pharmacological studies. In this study, we successfully isolated and identified five known clerodane diterpenes, namely 16-oxo-cleroda-3,13(14)E-dien-15-oic acid (1), 16-hydroxy-cleroda-3,13-dien-15-oic acid (2), 16-hydroxy-cleroda-4(18),13-dien-16,15-olide (3), 3α,16α-dihydroxy-cleroda-4(18),13(14)Z-dien-15,16-olide (4), and 16α-hydroxy-cleroda-3,13(14)Z-dien-15,16-olide (5) from the methanolic extract of seeds of Polyalthia longifolia. Initially, all the isolated metabolites were investigated for COX-1, COX-2, and 5-LOX inhibitory activities using the standard inhibitory kits. Of which, compounds 3, 4, and 5 exhibited to be potent COX-1, COX-2, and 5-LOX inhibitors with the IC50 values similar or lower to those of the reference drugs. To understand the underlying mechanism, these compounds were subjected to molecular docking on COX-1, COX-2, and 5-LOX proteins. Interestingly, the in silico study results were in high accordance with in vitro studies where compounds 3, 4, and 5 hits assumed interactions and binding pattern comparable to that of reference drugs (indomethacin and diclofenac), as a co-crystallized ligand explaining their remarkable dual (COX/LOX) inhibitor actions. Taken together, our findings demonstrated that compounds 3, 4, and 5 functioned as dual inhibitors of COX/5-LOX and can contribute to the development of novel, more effective anti-inflammatory drugs with minimal side-effects.


Asunto(s)
Araquidonato 5-Lipooxigenasa/metabolismo , Ciclooxigenasa 1/metabolismo , Ciclooxigenasa 2/metabolismo , Diterpenos de Tipo Clerodano/farmacología , Polyalthia/química , Araquidonato 5-Lipooxigenasa/química , Simulación por Computador , Ciclooxigenasa 1/química , Ciclooxigenasa 2/química , Inhibidores de la Ciclooxigenasa/química , Inhibidores de la Ciclooxigenasa/farmacología , Diterpenos de Tipo Clerodano/química , Humanos , Inhibidores de la Lipooxigenasa/química , Inhibidores de la Lipooxigenasa/farmacología , Modelos Moleculares , Simulación del Acoplamiento Molecular , Estructura Molecular , Extractos Vegetales/química , Extractos Vegetales/farmacología , Semillas/química
16.
Z Naturforsch C J Biosci ; 75(11-12): 473-478, 2020 Nov 26.
Artículo en Inglés | MEDLINE | ID: mdl-32628641

RESUMEN

Polyalthia is one of the largest genera in the Annonaceae family, and has been widely used in folk medicine for the treatment of rheumatic fever, gastrointestinal ulcer, and generalized body pain. The present investigation reports on the extraction by hydrodistillation and the composition of the essential oils of four Polyalthia species (P. sumatrana, P. stenopetalla, P. cauliflora, and P. rumphii) growing in Malaysia. The chemical composition of these essential oils was determined by gas chromatography (GC-FID) and gas chromatography-mass spectrometry (GC-MS). The multivariate analysis was determined using principal component analysis (PCA) and hierarchical clustering analysis (HCA) methods. The results revealed that the studied essential oils are made up principally of bicyclogermacrene (18.8%), cis-calamenene (14.6%) and ß-elemene (11.9%) for P. sumatrana; α-cadinol (13.0%) and δ-cadinene (10.2%) for P. stenopetalla; δ-elemene (38.1%) and ß-cubebene (33.1%) for P. cauliflora; and finally germacrene D (33.3%) and bicyclogermacrene for P. rumphii. PCA score and HCA plots revealed that the essential oils were classified into three separated clusters of P. cauliflora (Cluster I), P. sumatrana (Cluster II), and P. stenopetalla, and P. rumphii (Cluster III) based on their characteristic chemical compositions. Our findings demonstrate that the essential oil could be useful for the characterization, pharmaceutical, and therapeutic applications of Polyalthia essential oil.


Asunto(s)
Medicina Tradicional , Aceites Volátiles/química , Polyalthia/química , Análisis por Conglomerados , Cromatografía de Gases y Espectrometría de Masas , Humanos , Sesquiterpenos Policíclicos/química , Análisis de Componente Principal , Sesquiterpenos/química , Sesquiterpenos de Germacrano/química , Especificidad de la Especie , Terpenos/química
17.
Molecules ; 25(10)2020 May 21.
Artículo en Inglés | MEDLINE | ID: mdl-32455540

RESUMEN

Elucidation of the mechanism of action of compounds with cellular bioactivity is important for progressing compounds into future drug development. In recent years, phenotype-based drug discovery has become the dominant approach to drug discovery over target-based drug discovery, which relies on the knowledge of a specific drug target of a disease. Still, when targeting an infectious disease via a high throughput phenotypic assay it is highly advantageous to identifying the compound's cellular activity. A fraction derived from the plant Polyalthia sp. showed activity against Mycobacterium tuberculosis at 62.5 µge/µL. A known compound, altholactone, was identified from this fraction that showed activity towards M. tuberculosis at an minimum inhibitory concentration (MIC) of 64 µM. Retrospective analysis of a target-based screen against a TB proteome panel using native mass spectrometry established that the active fraction was bound to the mycobacterial protein Rv1466 with an estimated pseudo-Kd of 42.0 ± 6.1 µM. Our findings established Rv1466 as the potential molecular target of altholactone, which is responsible for the observed in vivo toxicity towards M. tuberculosis.


Asunto(s)
Antituberculosos/farmacología , Productos Biológicos/farmacología , Polyalthia/química , Tuberculosis/tratamiento farmacológico , Antituberculosos/química , Proteínas Bacterianas/antagonistas & inhibidores , Productos Biológicos/química , Descubrimiento de Drogas , Humanos , Mycobacterium tuberculosis/efectos de los fármacos , Mycobacterium tuberculosis/patogenicidad , Extractos Vegetales/química , Extractos Vegetales/farmacología , Proteoma/genética , Tuberculosis/microbiología
18.
Bioorg Med Chem ; 28(10): 115462, 2020 05 15.
Artículo en Inglés | MEDLINE | ID: mdl-32247751

RESUMEN

The first phytochemical investigation of Polyalthia cinnamomea led to the isolation and identification of two new oxoprotoberberine alkaloids, (-)-(13aS)-polyalthiacinnamines A and B, together with eleven known compounds. The structures of the new compounds were elucidated by extensive spectroscopic methods. The absolute configuration of miliusacunine E and consanguine B was established by X-ray diffraction analysis using Cu Kα radiation and ECD spectra, whereas the absolute configurations of polyalthiacinnamines A and B were established by comparison of their ECD spectra and specific rotations with those of miliusacunine E and consanguine B. Compounds 1-4, 6, and 8 exhibited α-glucosidase inhibitory activities (IC50 values ranging from 11.3 to 57.9 µM) better than a positive control (acarbose, IC50 83.5 µM). Compound 2 also exhibited NO production inhibitory activity with an IC50 value of 24.4 µM (indomethacin, a positive control, IC50 = 32.2 µM).


Asunto(s)
Alcaloides/farmacología , Inhibidores de Glicósido Hidrolasas/farmacología , Óxido Nítrico/antagonistas & inhibidores , Extractos Vegetales/farmacología , Polyalthia/química , alfa-Glucosidasas/metabolismo , Alcaloides/química , Alcaloides/aislamiento & purificación , Animales , Supervivencia Celular/efectos de los fármacos , Cristalografía por Rayos X , Relación Dosis-Respuesta a Droga , Inhibidores de Glicósido Hidrolasas/química , Inhibidores de Glicósido Hidrolasas/aislamiento & purificación , Ratones , Modelos Moleculares , Estructura Molecular , Óxido Nítrico/biosíntesis , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Células RAW 264.7 , Relación Estructura-Actividad , Árboles/química
19.
Bioorg Chem ; 95: 102927, 2020 01.
Artículo en Inglés | MEDLINE | ID: mdl-31931286

RESUMEN

Three new methylated Δ8-pregnene steroids, stemphylisteroids A-C (1-3) were isolated from the medicinal plant Polyalthia laui-derived fungus Stemphylium sp. AZGP4-2. Their structures were elucidated by the detailed analysis of comprehensive spectroscopic data. The absolute configuration of 1 was determined by X-ray crystallographic analysis. Compound 1 show antibacterial activity against Escherichia coli with the MIC value of 6.25 µg/mL, and 2 exhibited a broad spectrum of antibacterial activities against six pathogenic bacteria with the MIC values ranging from 12.5 to 50 µg/mL. The discovery of three methylated Δ8-pregnene steroids 1-3 are a further addition to diverse and complex array of methylated steroids.


Asunto(s)
Antibacterianos/farmacología , Ascomicetos/química , Escherichia coli/efectos de los fármacos , Polyalthia/química , Antibacterianos/química , Antibacterianos/aislamiento & purificación , Cristalografía por Rayos X , Relación Dosis-Respuesta a Droga , Metilación , Pruebas de Sensibilidad Microbiana , Modelos Moleculares , Conformación Molecular , Relación Estructura-Actividad
20.
J Ethnopharmacol ; 248: 112279, 2020 Feb 10.
Artículo en Inglés | MEDLINE | ID: mdl-31600562

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Synthetic antiviral drugs have several limitations including high cost. Thus research on antiviral property of medicinal plants is continuously gaining importance. Polyalthia longifolia possesses several medicinal properties and has been used in traditional ayurvedic medicine for treatment of dermatological ailments as kushta, visarpa/herpes virus infection and also to treat pyrexia of unknown origin as mentioned in Visarpa Chikitsa. AIM OF THE STUDY: Keeping in view the cytotoxic, anti-cancer activity and antiviral efficacy of Polyalthia longifolia against herpes, present study was undertaken to evaluate the in vitro antiviral activity of methanolic extract of Polyalthia longifolia leaves, if any, and to unravel the possible target(s)/mechanism of action. MATERIAL AND METHODS: Antiviral activity of Polyalthia longifolia methanolic extract was studied using Vero cell lines against paramyxoviruses, namely-peste des petits ruminants virus (PPRV) and Newcastle disease virus (NDV). Cytotoxicity of the test extract was evaluated employing MTT assay. Virucidal activity, and viral-attachment, virus entry and release assays were determined in Vero cells using standard experimental protocols. The viral RNA in the virus-infected cells was quantified by qRT-PCR. RESULTS: At non-cytotoxic concentration, methanolic extract of Polyalthia longifolia leaves was found to inhibit the replication of PPRV and NDV at viral entry and budding level, whereas other steps of viral life cycle such as attachment and RNA synthesis remained unaffected. CONCLUSIONS: Polyalthia longifolia leaves extract possesses promising antiviral activity against paramyxoviruses and acts by inhibiting the entry and budding of viruses; and this plant extract evidently possesses excellent and promising potential for development of effective herbal antiviral drug.


Asunto(s)
Antivirales/farmacología , Virus de la Enfermedad de Newcastle/efectos de los fármacos , Virus de la Peste de los Pequeños Rumiantes/efectos de los fármacos , Extractos Vegetales/farmacología , Polyalthia , Animales , Chlorocebus aethiops , Virus de la Enfermedad de Newcastle/fisiología , Virus de la Peste de los Pequeños Rumiantes/fisiología , Hojas de la Planta , Células Vero , Internalización del Virus/efectos de los fármacos
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