Piper species are aromatic plants used as spices in the kitchen, but their secondary metabolites have also shown biological effects on human health. These plants are rich in essential oils, which can be found in their fruits, seeds, leaves, branches, roots and stems. Some Piper species have simple chemical profiles, while others, such as Piper nigrum, Piper betle, and Piper auritum, contain very diverse suites of secondary metabolites. In traditional medicine, Piper species have been used worldwide to treat several diseases such as urological problems, skin, liver and stomach ailments, for wound healing, and as antipyretic and anti-inflammatory agents. In addition, Piper species could be used as natural antioxidants and antimicrobial agents in food preservation. The phytochemicals and essential oils of Piper species have shown strong antioxidant activity, in comparison with synthetic antioxidants, and demonstrated antibacterial and antifungal activities against human pathogens. Moreover, Piper species possess therapeutic and preventive potential against several chronic disorders. Among the functional properties of Piper plants/extracts/active components the antiproliferative, anti-inflammatory, and neuropharmacological activities of the extracts and extract-derived bioactive constituents are thought to be key effects for the protection against chronic conditions, based on preclinical in vitro and in vivo studies, besides clinical studies. Habitats and cultivation of Piper species are also covered in this review. In this current work, available literature of chemical constituents of the essential oils Piper plants, their use in traditional medicine, their applications as a food preservative, their antiparasitic activities and other important biological activities are reviewed.

Piper Species: A Comprehensive Review on Their Phytochemistry, Biological Activities and Applications.

Bioactive compounds from medicinal plants: Focus on Piper species

The traditional use of plants to manage candidiasis and related infections in Venda, South Africa

Universidad Nacional de Colombia - Sede Bogota, Pontificia Universidad Javeriana, MinCiencias

Evaluación del efecto de algunos elicitores sobre la producción de metabolitos secundarios en suspensiones celulares de Piper sp.

Tetranychus urticae Koch (Acari: Tetranychidae) is an economically important pest of agricultural and ornamental crops worldwide. It has been shown that many of natural plant-based pesticides have fewer side effects compared with synthetic chemicals. The essential oils of plants have been broadly studied for pest-control, including toxic and repellent effects, antifeedant, ovicidal, and other properties. Essential oils from stems, flowers, and leaves of Piper marginatum Jacq. were evaluated in the laboratory regarding their acaricidal potential against the two-spotted spider mite (T. urticae) and the results were compared with eugenol as a positive control. The oils were also evaluated with regard to the susceptibility of the natural enemy of T. urticae (Neoseiulus californicus McGregor). Based on LC50 estimates, oils from stems and flowers exhibited the same toxicity and differed significantly from the leaf oil with LC50 0.37, 0.56, and 3.77 μL L -1 , respectively. None of the oils tested exhibited toxicity greater than or equal to that of the positive control. The oil mortality rate was significantly lower for N. californicus (50% to 70%) than for T. urticae (> 95%). The P. marginatum oils also deterred oviposition. Among the chemical constituents tested, sesquiterpenes were more toxic with an LC50 of 2.89 μL L -1 than phenylpropanoids Z-asarone and E-asarone with LC50 6.64 and 8.51 μL L -1 , respectively. The acaricidal

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Toxicity of essential oils of Piper marginatum Jacq. against Tetranychus urticae Koch and Neoseiulus californicus (McGregor)

Piper, the pepper plants or pepper vines are an economically and ecologically important genus in the family Piperaceae. It contains about 1,000-2,000 species of shrubs, herbs, and lianas, many of which are keystone species in their native habitat. Piper species have a pan tropical distribution, and are most commonly found in the understory of lowland tropical rainforests, but can also occur in clearings and in higher elevation life zones such as cloud forests. Most Piper species are either herbaceous or vines; some grow as shrubs or almost as small trees. Many species of piper have been used for treating different diseases in many traditions. E.g P. cubeba has been used in folk medicine, herbalism as well as in the early 20th century, as a cigarette flavoring. P. darienense is used medically by the Kuna people of the Panama-Colombia border region, and elsewhere it is used to intoxicate fish which then can be easily caught. Black Pepper (P. nigrum) essential oil is sometimes used in herbalism, and Long Pepper (P. longum) is similarly employed in Ayurveda, where it was an ingredient of Triphala Guggulu and (together with Black Pepper) of Trikatu pills, used for rasayana (rejuvenating and detoxifying) purposes.

Introduction, phytochemistry, traditional uses and biological activity of genus Piper: a review

The article describes the development of a robust pharmacophore model and investigation of structure activity relationship analysis of 56 isothiazolidinedione derivatives reported as PTP1B inhibitors. A six-point pharmacophore model consisting of four aromatic rings (R), one hydrogen bond donor (D) and one hydrogen bond acceptor (A) with discrete geometries as pharmacophoric features was developed and the generated pharmacophore model was used to derive a predictive 3D QSAR model for the studied dataset. The obtained 3D QSAR model has an excellent correlation coefficient value (r
 2 = 0.98) along with good statistical significance as shown by a high Fisher ratio (F = 428.60). The model also exhibits good predictive power confirmed by the high value of cross-validated correlation coefficient (q
 2 = 0.62). The QSAR model suggests that hydrophobic aromatic character is crucial for the PTP1B inhibitory activity at the R-15 site.

Pharmacophore modeling and 3D QSAR analysis of isothiazolidinedione derivatives as PTP1B inhibitors

Indian traditional medicinal plant Piper attenuatum (Buch-Ham) has been investigated for its antioxidant and anticancer activity. Three extracts were prepared using ethyl acetate, ethanol and methanol. In vitro antioxidant activity was performed by ABTS {2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid)} free radical scavenging method. All three extracts reduced the free radicals produced by ABTS in a concentration-dependent manner which could be compared to the standard (gallic acid). Invitro anticancer activity of all extracts was carried out by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay method against MCF7 (Michigan Cancer Foundation-7) cell lines. None of the extract showed anticancer activity when compared with the standard (mitomycin C) indicating that P. attenuatum is deprived of antiproliferative or cytotoxic components.

In vitro screening of dry fruit extracts of Piper attenuatum for antioxidant and anticancer activity

Novel ester derivatives of 2, 10-dichloro-12H-dibenzo [d,g] 1,3 dioxocin-6-carboxylic acid were synthesized and evaluated for their in vitro human cholesteryl ester transfer protein (CETP) inhibition. Three out of twelve synthesized compounds showed good inhibition of CETP (more than 50 %). Compound 10 showed 81.32 % inhibition of CETP at the dose of 0.5 nM whereas compound 11 showed 75.78 % inhibition when tested at the same concentration. Compound 8 and 13 also showed modest activity with 57.44 and 38.02 % inhibition. All other synthesized compounds were devoid of significant inhibitory activity against CETP. We also performed molecular docking to predict the mode of binding of all compounds at the active site of CETP. Compound 10 showed the dock score of −9.16 whereas the dock score of compound 11 was found to be −9.09.

Synthesis and in vitro cholesteryl ester transfer protein inhibitory activity of novel esters of 2, 10-dichloro-12H-dibenzo [d,g] 1,3-dioxocin-6-carboxylic acid

Objective: The aim of the present work was to design and synthesize 2, 3-aryl substituted 1, 3-benzoxazin-4-one derivatives and evaluate them for in-vitro antiproliferative activity against human breast adeno-carcinoma cells. Methods: The compounds were synthesized and screened for in-vitro antiproliferative activity against MCF-7 cell lines using 96 well plate method. Results: 3 out of 9 synthesized compounds showed good in-vitro inhibition of MCF-7 cell lines. Compound 2 showed least IC 50 (highest active) i.e. 0.89 µg followed by compound 4 (IC 50 = 1.02 µg) and compound 3 (IC 50 = 1.19 µg). 4 compounds showed more than 90 % inhibition at 100 µg after 48 h incubation. Conclusion: This class of compounds showed some initial promising activity which can be further expanded by synthesizing and testing more analogs of this kind against MCF-7 cell lines which may give good leads to proceed. Keywords: 1, 3-benzoxazin-4-one, Antiproliferative activity, MCF-7 cell lines, Molecular docking.

Renu Ohlyan

Papers

Introduction, phytochemistry, traditional uses and biological activity of genus Piper: a review

Pharmacophore modeling and 3D QSAR analysis of isothiazolidinedione derivatives as PTP1B inhibitors

In vitro screening of dry fruit extracts of Piper attenuatum for antioxidant and anticancer activity

Synthesis and in vitro cholesteryl ester transfer protein inhibitory activity of novel esters of 2, 10-dichloro-12H-dibenzo [d,g] 1,3-dioxocin-6-carboxylic acid

Synthesis and in-vitro antiproliferative activity of 2, 3-aryl substituted 1, 3-benzoxazin-4-one derivatives