Majoon-E-Piyaz: A Potent Unani Formulation for Premature Ejaculation

Alam, Shah; Anjum, Nighat; Akhtar, Jamal; Bashir, Fouzia; Khan, Asim Ali

doi:10.22270/jddt.v10i3-s.4123

Cited by 3 publications

(5 citation statements)

References 7 publications

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“…The orange solid was heated as a suspension in propan-2-ol (20 mL) at 70 °C in a water bath for 20 min, during which time the solid became pale yellow. The suspension was filtered, and the solid was dried via rotary vapor to afford 2a (970.6 mg, 110.6% quantitative yield) as a pale yellow solid: 1…”

Section: -Hydroxy-7-methylfuro[32-g]chromen-5-one (2a)mentioning

confidence: 99%

“…The crude product (61.8 mg) was purified by SiO 2 column chromatography on a Biotage SNAP KP-Sil 50 g column (40−63 μm, 60 Å, 39 mm × 81 mm) running at 50 mL/min using a hexane/ethyl acetate gradient beginning with 100:0 to 0:100 over 1300 mL. 15 mL fractions were collected and combined based on TLC similarities to afford 1b (62.6 mg, 91.6% yield): 1 4,9-Dibutoxy-7-methylfuro[3,2-g]chromen-5-one (1c). Compound 1a (50.8 mg, 0.75 mmol) and 1-bromobutane (70 μL, 2.25 mmol) were treated as described in the Representative Alkylation for the Production of Synthetic Analogues section.…”

Section: 9-diacetyloxy-7-methylfuro[32-g]chromen-5-one (1b)mentioning

confidence: 99%

“…The crude product (219.5 mg) was purified by SiO 2 column chromatography on a Biotage Sfar 100 g column (60 μm, 100 Å) running at 150 mL/min using a hexane/ethyl acetate gradient beginning with 100:0 to 0:100 over 1500 mL. 15 mL fractions were collected and combined based on TLC similarities to afford 1i (14.4 mg, 9.4% yield): 1 H NMR (400 MHz, CDCl 3 ) δ 7.63 (s, 1H), 6.98 (d, J = 2.2 Hz, 1H), 4.35 (t, J = 6.5 Hz, 2H), 4.16 (t, J = 6.7 Hz, 2H), 2.44 (s, 3H), 1.94− 1.83 (m, 4H), 1.62−1.44 (m, 4H), 1.25 (s, 49H), 0.87 (t, J = 6.7 Hz, 6H). 13…”

Section: -Pentadecoxy-7-methylfuro[32-g]chromen-5-one (2h)mentioning

confidence: 99%

“…Khellin and visnagin are furanochromones from the plant Ammi visnaga with a long history of use in a variety of medicinal applications. 1 Some of the earliest medicinal reports on khellin and its preparations appeared in the literature in the early 1900s. 2,3 More recent medicinal and therapeutic applications have included the use of khellin for the treatment of vitiligo, 4,5 psoriasis, 6 and as a vasodilator.…”

Section: ■ Introductionmentioning

confidence: 99%

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Synthesis, Herbicidal Activity, and Structure–Activity Relationships of O-Alkyl Analogues of Khellin and Visnagin

Cantrell,

Travaini,

Bajsa-Hirschel

et al. 2023

J. Agric. Food Chem.

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Khellin and visnagin furanochromones were recently reported as potential new bioherbicides with phytotoxic activities comparable to those of some commercially available herbicides. In this study, we examined the effect of O-alkylation and O-arylalkylation of both khellin and visnagin on its effect on herbicidal and antifungal activity. Synthetic analogues included Odemethyl khellin and visnagin, acetylated O-demethyl khellin and visnagin, O-benzylated demethyl khellin and visnagin, four Odemethyl alkylated khellin analogues, and six O-demethyl alkylated visnagin analogues, many of which are reported here for the first time. Both acetate analogues of khellin and visnagin indicated more activity as herbicides on Lemna pausicostata than visnagin, with IC 50 values of 71.7 and 77.6 μM, respectively. Complete loss of activity for all O-alkyl analogues with a carbon chain length of greater than 14 carbons was observed. The O-demethyl butylated visnagin analogue was the most active compound with an IC 50 of 47.2 μM against L. pausicostata. O-Demethyl ethylated analogues of both khellin and visnagin were as effective as khellin. In the antifungal bioautography bioassay against Colletotrichum fragariae at 100 μg, the only active O-alkyl and O-arylalkyl analogues were Oethylated, O-butylated, and O-benzylated visnagin analogues with zones of inhibition of 10, 9, and 9 mm, respectively, an effect comparable to that of visnagin and khellin.

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Section: -Hydroxy-7-methylfuro[32-g]chromen-5-one (2a)mentioning

confidence: 99%

Section: 9-diacetyloxy-7-methylfuro[32-g]chromen-5-one (1b)mentioning

confidence: 99%

Section: -Pentadecoxy-7-methylfuro[32-g]chromen-5-one (2h)mentioning

confidence: 99%

Section: ■ Introductionmentioning

confidence: 99%

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Synthesis, Herbicidal Activity, and Structure–Activity Relationships of O-Alkyl Analogues of Khellin and Visnagin

Cantrell,

Travaini,

Bajsa-Hirschel

et al. 2023

J. Agric. Food Chem.

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show abstract

“…In order to find the best descriptors to construct a model, it is important to eliminate unnecessary descriptors to generate a significant model [29]. 2020 In the present study, although we subjected all the 28 molecules for cytotoxic assessment and QSAR analysis, 8 molecules did not show parameters to generate significant QSAR equation and these outliers have been deleted.…”

Section: Qsar Analysismentioning

confidence: 99%

Antiproliferative potential, quantitative structure-activity relationship, cheminformatic and molecular docking analysis of quinoline and benzofuran derivatives

et al. 2020

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Quinoline and benzofuran moieties are commonly used for the synthesis of therapeutically beneficial molecules and drugs since they possess a wide range of pharmacological activities including potent anticancer activity as compared to other heterocyclic compounds. Many of well-known antimalarial, antimicrobial, anti-helminthic, analgesic, anti-inflammatory, antiprotozoal, and antitumor compounds contain quinoline/benzofuran skeleton. The aim of this study was to analyze ten new quinoline and eighteen benzofuran derivatives for carcinoma cell line growth inhibition and to predict possible interactions with the target. The anticancer activity of these compounds against colon cancer (HCT-116) and triple-negative breast cancer (MDA-MB-468) cell lines was determined and performed molecular docking to predict the possible interactions. Among ten quinoline derivatives, Q1, Q4, Q6, Q9, and Q10 were found to be the most potent against HCT-116 and MDA-MB-468 with IC50 values ranging from 6.2-99.6 and 2.7-23.6 μM, respectively. Using the IC50 values, a model equation with quantitative structure activity relationship (QSAR) was generated with their descriptors such as HBA1, HBA2, kappa (1, 2 and 3), Balaban index, Wiener index, number of rotatable bonds, log S, log P and total polar surface area (TPSA). The effect of benzofuran derivatives was moderate in cytotoxicity tests and hence only quinolines were considered for further analysis. The molecular docking indicated the mammalian / mechanistic target of rapamycin (mTOR), Topoisomerase I and II as possible targets for these molecules. The predicted results obtained from QSAR and molecular docking analysis of quinoline derivatives showed high correlation in comparison to the results of the cytotoxic assay. Overall, this study indicated that quinolines are more potent as anticancer agents compared to benzofurans. Further, compound Q9 has emerged as a lead molecule which could be the base for further development of more potent anticancer agents.

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Physicochemical assessment and insilico studies on the interaction of 5-HT2c receptor with herbal medication bioactive compounds used in the treatment of premature ejaculation

Aghanwa

Ekpunobi

Ogbuagu

2023

Physical Sciences Reviews

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Premature ejaculation (PE) affects one in every four men around the world, and there is no known cure for this sexual dysfunction. Many non-herbal and herbal medications are prescribed for their treatment, some of which have not been thoroughly evaluated for their efficacy and role in the body. Premature ejaculation herbal treatment medication produced in Abia State, Nigeria, were analysed for its efficacy using Fluoxetine as a compared compound, a selective serotonin reuptake inhibitor in the treatment of PE. The herbal drugs were analysed using both classical and spectroscopic methods for the determination of its proximate content, phytochemical analysis, heavy metals concentrations and bioactive compounds. The interactions with the 5-HT2c serotonin receptors were investigated using in silico computational analysis, molecular docking, and pharmacokinetic properties of the selected compounds with ADMET screening. The availability of important phytochemicals such as alkaloids, terpenoids, flavonoids, tannins, and saponins was recorded, and the proximate content values were within the recommended ranges. Heavy metals such as Pb (46 mg/kg), Cd (22 mg/kg), Ni (35 mg/kg), and Mn (132 mg/kg) were found in excess of the recommended limits. Fifty-one compounds were discovered in the herbal drug samples, which were then screened for drug-ability using the Lipinski rule. In this study, six (6) compounds with the highest binding affinities among the compounds under investigation were reported. All six compounds were found to have binding affinity scores ranging from −7.5 kcal/mol to −10.5 kcal/mol. Their interactions in the active sites of the target receptors were with amino acids residues like ASP 134, VAL 135, SER 138, VAL 208, PHE 327, VAL 354, TRY 358, PHE 328, GLY 218, ASN 331, ALA 222, and LEU 350 sharing hydrophobic and electrostatic bonds. The study predicted the ADMET properties of the compounds under investigation and discovered that some of them had good pharmacokinetic properties and CYP2C19 enzyme inhibitory potential. This research suggests that these compounds could be active ingredients in herbal medications used to treat premature ejaculation. However, after using this medication, serum concentrations of patients can be measured to further assess its efficacy.

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Majoon-E-Piyaz: A Potent Unani Formulation for Premature Ejaculation

Cited by 3 publications

References 7 publications

Synthesis, Herbicidal Activity, and Structure–Activity Relationships of O-Alkyl Analogues of Khellin and Visnagin

Synthesis, Herbicidal Activity, and Structure–Activity Relationships of O-Alkyl Analogues of Khellin and Visnagin

Antiproliferative potential, quantitative structure-activity relationship, cheminformatic and molecular docking analysis of quinoline and benzofuran derivatives

Physicochemical assessment and insilico studies on the interaction of 5-HT2c receptor with herbal medication bioactive compounds used in the treatment of premature ejaculation

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