• Advances in Traditional Medicine
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• 제10권4호
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• pp.263-270
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• 2010

Scoparia dulcis L. is widely used in the traditional system of medicine for treating liver ailments. In the present study the terpenoids and terpenoid fractions isolated from 1:1:1 petroleum ether, diethyl ether and methanol (PDM) extract of Scoparia dulcis L. were tested for their in vitro 1, 1-Diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity. Selected samples from the assay were further tested for their in vitro hepatoprotective activity against $CCl_4$ induced hepatotoxicity in freshly isolated rat hepatocytes. In the in vitro antioxidant study, fractions 7, 11, 13, 14, and 15 and PDM extract show the DPPH radical scavenging activity. The phytochemical screening of all these fractions show the presence of terpenoids. In the in vitro hepatoprotective study all these fractions and the PDM extract significantly prevent the $CCl_4$ induced changes in the aspartate aspartate amino transferase, alanine amino transferase and alkaline phosphatase levels (p < 0.05). The above results are comparable with the standard, silymarin. The results of the study indicate that, the PDM extract of Scoparia dulcis L. possesses potential hepatoprotective activity and this may be attributed to its free radical scavenging potential, which in turn may be attributed to the presence of terpenoids.

• Asian Pacific Journal of Cancer Prevention
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• 제17권1호
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• pp.51-55
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• 2016

Phytochemical investigation of Pistacia integerrima has highlighted isolation of two known compounds naringenin (1) and dihydrokaempferol (2). A crude extract and these isolated compounds were here evaluated for their effects on reversion of multidrug resistance (MDR) mediated by P-glycoprotein (P-gp). The multidrug resistance P-glycoprotein is a target for chemotherapeutic drugs from cancer cells. In the present study rhodamine-123 exclusion screening test on human mdr1 gene transfected mouse gene transfected L5178 and L5178Y mouse T-cell lymphoma cells showed excellent MDR reversing effects in a dose dependent manner. In-silico molecular docking investigations demonstrated a common binding site for Rhodamine123, and compounds naringenin and dihydrokaempferol. Our results showed that the relative docking energies estimated by docking softwares were in satisfactory correlation with the experimental activities. Preliminary interaction profile of P-gp docked complexes were also analysed in order to understand the nature of binding modes of these compounds. Our computational investigation suggested that the compounds interactions with the hydrophobic pocket of P-gp are mainly related to the inhibitory activity. Moreover this study s a platform for the discovery of novel natural compounds from herbal origin, as inhibitor molecules against the P-glycoprotein for the treatment of cancer.

• 분석과학
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• 제30권1호
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• pp.26-31
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• 2017

Background and purpose: This study was carried out to learn more about the potential prophylactic or antibacterial activity of the plant Acalypha indica against selective pathogenic bacteria. Experimental: The test organisms were Sarcina lutea IFO 3232, Bacillus subtilis IFO 3026, Pseudomonas denitrificans, Escherichia coli IFO 3007, Klebsiella pneumoniae ATTC 10031, Xanthomonas campestris IAM 1671, and Proteus vulgaris. Leaf, stem, and bud powder of Acalypha indica were dissolved in various solvents, and the extracts were tested for antimicrobial activity through the disc diffusion method. GC-MS profiling was performed to characterize active chemical compounds in the essential oil of Acalypha indica. Results: The ethanol extract showed the highest activity against all bacteria, while the petroleum ether extract yielded the highest zone of inhibition against Proteus vulgaris ($11.83{\pm}1.75mm$). The minimum inhibitory concentration (MIC) of the ethyl acetate extract against Bacillus subtilis was 16 µg/mL. Phytochemical screening by GC-MS revealed a total of 12 bioactive compounds. Conclusion: Extracts of Acalypha indica may be useful in formulating and synthesizing new antibacterial drugs.

• Natural Product Sciences
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• 제27권2호
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• pp.99-114
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• 2021

Type 2 diabetes mellitus (T2DM) and its complications are important noncommunicable diseases with high mortality rates. Protein tyrosine phosphatase 1B (PTP1B) and aldose reductase inhibitors are recently approached and advanced for T2DM and its complications therapy. Matricaria chamomilla L. is acknowledged as a worldwide medicinal herb that has many beneficial health effects as well as antidiabetic effects. Our research was designed to determine the most potential antidiabetic phytochemicals from M. chamomilla employing in silico study. 142 phytochemicals were obtained from the databases. The first screening employed iGEMdock and Swiss ADME, involving 93 phytochemicals. Finally, 30 best phytochemicals were docked. Molecular docking and visualization analysis were performed using Avogadro, AutoDock 4.2., and Biovia Discovery Studio 2016. Molecular docking results demonstrate that ligand-protein interaction's binding affinities were -5.16 to -7.54 kcal/mol and -5.30 to -12.10 kcal/mol for PTP1B and aldose reductase protein targets respectively. In silico results demonstrate that M. chamomilla has potential antidiabetic phytochemical compounds for T2DM and its complications. We recommended anthecotulide, quercetin, chlorogenic acid, luteolin, and catechin as antidiabetic agents due to their binding affinities against both PTP1B and aldose reductase protein. Those phytochemicals' significant efficacy and potential as antidiabetic must be investigated in further advanced research.

• Natural Product Sciences
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• 제29권1호
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• pp.50-58
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• 2023

The phytochemical investigation of the crude methanolic extracts roots and stem bark of Anthonotha cladantha (Harms) J.Léonard led to the isolation and identification of twelve secondary metabolites: 2,3-dihydroxypropyl hexacosanoate (1), hederagenine (2), cycloeucalenol (3), 2α-hydroxylupeol (4), betulinic acid (5), lupeol (6), heptacosan-2-one (7), triacontanoic acid (8), stigmast-4-en-3-one (9), β-sitosterol (10), stigmasterol (11), and stigmasterol-3-O-β-D-glucopyranoside (12). Their structures were elucidated with the help of their spectroscopic and physical data and by comparison with those reported in the literature. To the best of our knowledge, from all those compounds, 2,3-dihydroxypropyl hexacosanoate (1), hederagenine (2), cycloeucalenol (3), 2α-hydroxylupeol (4), and betulinic acid (5) are being reported for the first time from this genus. In addition, the acetylation of compound 1 afforded a new derivative 3-(hexacosanoyloxy)propane-1,2-diyl diacetate (1a). Compound 1 possessed a moderate α-glucosidase inhibitory activity with an IC₅₀ value of 39.2 ± 0.22 μM; it neither showed antioxidant activity nor inhibition against the enzyme urease. Compound 1a exhibited weak antioxidant activity in the DPPH assay with an IC₅₀ value of 80.3 ± 0.83 μM but was inactive against α-glucosidase and urease. Furthermore, both compounds 1 and 1a were inactive against seven pathogenic bacterial strains.

• Journal of Applied Biological Chemistry
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• 제60권1호
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• pp.49-54
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• 2017

본 연구는 천연 미백소재 탐색을 위하여 율무(C. lachryma-jobi var. ma-yuen) 부산물 추출물의 tyrosinase 저해활성을 검증하였으며, 그 중에서 뿌리 추출물은 $159.3g/{\mu}mL$의 $IC_{50}$ 값을 나타내었다. 율무 뿌리 추출물의 순차적 용매 분획에 대한 활성 검증 후 가장 활성이 우수한 EtOAc 분획물에 대하여 Diaion HP-20 column chromatography, MPLC및 preparative HPLC를 수행해 율무근으로부터 여섯 개의 화합물을 정제하였고, 이 물질들의 구조 분석은 LC-MS와 NMR 데이터 해석을 바탕으로 진행하여 각각 (+)-icariol $A_2$ (1), zhepiresionol (2), 4-hydroxybenzaldehyde (3), trans-${\rho}$-coumaric acid (4), N-(2-hydroxy-4-methoxyphenyl)-2-hydroxyacetamide (5), coixol (6)로 구조를 규명하였다. 화합물 1은 이 식물에서 처음으로 분리되었으며, 화합물 5는 자연계로부터 처음으로 분리된 화합물로 확인하였다. 이들 화합물 중 4-hydroxybenzaldehyde (3), trans-${\rho}$-coumaric acid (4)와 coixol (6)은 순서대로 707.4, 6.5, $62.4{\mu}M$의 $IC_{50}$ 값을 나타내어 대조군으로 사용한 arbutin ($IC_{50}=618.7{\mu}M$)과 비교시 유사하거나 우수한 활성을 확인하였다. 이로 미루어 보아, 율무근 추출물과 활성물질의 tyrosinase 저해활성을 확인할 수 있었으며, 율무근 추출물의 미백소재로서의 적용 가능성을 확인할 수 있었다.

• 생명과학회지
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• 제32권9호
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• pp.734-741
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• 2022

전세계적으로 약 4천만 명의 사람들이 인체면역결핍증바이러스(HIV) 감염이 되어 있으며, HIV에 감염된 세포의 수가 치명적인 수준에 다르면 후천성면역결핍증후군을 일으키게 된다. HIV에 감염이 되면 완치 치료가 어려우며 현재 알려진 치료방법으로는 감염, 복제 및 바이러스 방출 억제를 위해 항레트로 바이러스 치료법이 병용되고 있다. 하지만 HIV 바이러스는 지속적인 돌연변이 유발 및 약물에 대한 내성을 갖게 하므로 장기간 약물복용 시 심각한 부작용을 초래한다. 이에 새로운 치료방법과 효능약물에 대한 연구가 필요한 실정이다. 식물유래 천연물은 수많은 생리활성물질들이 보고되어 있으며, 이는 항HIV 효능 지닌 잠재성을 가진 후보 물질이 될 수 있다. 1990년 세계보건기구에서는 플라보노이드, 쿠마린, 탄닌 및 테르펜의 항 HIV 효능을 보고하였으며, 이러한 물질은 SARS-CoV-2와 같은 바이러스 감염을 또한 억제하는 것으로 밝혀졌다. 따라서, 본 연구에서는 항 HIV 효능을 나타내는 식물 추출물 및 파이토케미컬에 대한 최신 연구동향(2021-현재)을 검토하였으며, 이를 통해 항HIV 효능을 지닌 새로운 천연물 발굴의 기초자료로 활용될 것으로 사료된다.

• 셀메드
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• 제11권4호
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• pp.21.1-21.9
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• 2021

Background: Unani System of Medicine (USM) has its origin to Greece. To ensure and develop the quality, authenticity of Unani drugs, standardization on modern analytical parameter is essential requirement for drugs. Objectives: The aimed of the present study was to develop a standard profile of "Qurṣ-e-Mafasil" by systematic study through authenticated ingredients, pharmacognostic identification followed by physicochemical, TLC, HPTLC fingerprinting analysis as per standard protocol. Material and Methods: In this study three batches of "Qurṣ-e-Mafasil" QM were prepared by standard method as per UPI had been followed by organoleptic properties of formulation such as appearance, color, odor, taste. Powder Microscopy and physicochemical studies were carried out such as Uniformity of weight, Friability, Disintegration time, hardness, LOD, ash vales and extractive values in like aqueous, alcohol & hexane. Further qualitative tests such as Thin-Layer Chromatography (TLC), and High-Performance Thin Layer Chromatography (HPTLC) studies were also carried out to develop fingerprint pattern of the alcoholic solvent extract of QM. Phytochemical screening was carried out in different solvent extracts such as alcoholic, aqueous and chloroform extracts to detect the presence phytoconstituents in the formulation QM. Heavy metals, Microbial Load Contamination and pesticidal residues were also determined. Results: Qurṣ-e-Mafasil showed tablet-like appearance, light brown colour, mild pungent odour and acrid taste. Uniformity of weight (mg), friability (rpm), and hardness (kg/cm) and disintegration time was ranged between (500 to 503), (0.0340 to 0.038), (8.40 to 8.67) and (4-5 minutes) respectively for the three batches. Loss in weight on drying at 105℃ was ranged between (8.3425 to 8.7346). Extracted values were calculated in distilled water ranged between (30.9091 to 31.4358), hexane (1.1419 to 1.4281), and alcohol (3.3352 to 3.3962). The ash values recorded were ranged between (3.7336 to 3.8378), and acid insoluble ash (0.5859 to 0.6112).