Chemical constituents and standardization of Piper piedecuestanum TREL & YUNCK. With antiplasmodial and cytotoxic activity

Figures & data

Table 1. Extraction and mg/L of the marker compounds in extracts prepared from the aerial parts P.piedecuestanum.

Code	Extract by percolation, leaves and stems by triplicate	% yield	Marker substance in the extracts (mg/L) X + SD*
			(5) tR= 7,589	(1) tR=7,897	(3) tR=10,078	(4) tR= 11,098
PPEP	Percolation EtOH, 25ºC ZP* :5mm 24h	0.89**	5.1±0.41	1.3±0.31	2.9±0.21	1.21±0.09
PPDP	Percolation DCM, 25ºC ZP* :5mm 24h	1.75**	11.3±0.05	2.3±0.06	3.2±0.61	1.12±0.81
PPAP	Percolation EtoAc, 25ºC ZP* :5mm 24h	1.12**	6.7±0.26	1.1±0.13	2.0±0.11	0.81±0.04
PPDS4	Soxhtlet DCM, 40ºC, ZP:5mm 4 h	2.6±0.17	6.5±0.70	1.9±0.51	2.9±0.3	1.3±0.21
PPAS4	Soxhtlet EtoAc, 40ºC, ZP:5mm 4 h	3.2±0.22	6.8±0.31	0.93±0.84	2.7±0.98	1.2±0.51
PPDMS4	Soxhtlet DCM: MeOH (1:1) 40ºC, ZP:5mm 4 h	5.5±0.32	4.1±0.09	2.0±0.21	4.1±0.51	1.6±0.33
PPDS6	Soxhtlet DCM, 40ºC, ZP:5mm 6 h	3.0±0.31	7.8±0.61	1.9±0.02	4.6±0.39	1.6±0.14
PPAS6	Soxhtlet EtoAc. 40ºC. ZP:5mm 6 h	3.6±0.55	5.9±0.68	1.5±0.07	3.9±0.18	1.2±0.11
PPDMS6	Soxhtlet DCM: MeOH (1:1) 40ºC. ZP:5mm 6 h	5.2±0.53	4.2±0.3	1.1±0.09	2.6±0.20	0.38±0.43

* X (Medium) + SD (Standard deviation)

** One data. Compound (2) it was not quantified.

Table 2. Antiplasmodial activity of isolated compounds of P. piedecuestanum

Code	IC 50 (µg/mL) X + SD*	CC50 (µg/mL) X + SD	IS***
	Strain of P. falciparum NF-54**	Cell Line U-937
PPEP	25.2±0.35	12.35±0.333	0.49
PPDP	17.9±2.0	16.72±2.27	0.93
PPAP	19.5±1.8	27.38±4.98	1.40
PPDS4	40.3±1.3	13.98±3.99	0.35
PPAS4	31.6±1.8	17.63±1.77	0.56
PPDMS4	>50	20.69±3.56	ND
PPDS6	24.7 ±3.1	17.17±1.19	0.69
PPAS6	32.6±1.1	22.09±2.72	0.69
PPDMS6	>50	45.41±2.83	ND

* X (Medium) + SD (Standard deviation)

ND = Not determined

** Chloroquine positive control IC₅₀ = 23.91 + 2.78 nM

*** Selectivity Index (IS) = CC₅₀ (μg / mL) / IC₅₀ (μg / mL)

Only Compound (1) presented promising antiplasmodial activity with an IC₅₀ = 7.325 μg / mL (25.69 μM); IS_HUVEC =13.65

Classification of antiplasmodial activity: highly active <5 μg / mL, promising 6-15 μg / mL, moderate activity 16-30 μg / mL, low activity 31-50 μg / mL and inactive> 50 μg / mL.

Classification of cytotoxic activity: highly toxic <10 μg / mL, cytotoxic 10-40 μg / mL, moderately cytotoxic 41-100 μg / mL and non-cytotoxic> 100 μg / mL.

Figure 1. Chemical constituents from extracts of Piper piedecuestanum

Figure 2. Chromatographic profiles of the extracts obtained from the aerial parts of P. piedecuestanum: (A) dichloromethane extract obtained by percolation, (B) ethyl acetate extract obtained by percolation (C) extract of dichloromethane obtained after 6 hours of Soxhlet extraction