Review Article

Phytochemistry and Biological Activities of Poria

Table 3

Summary table of Poria cocos activity.

Type of the activitiesSubjectsActivitiesMechanismsRef.

Antitumor actionTotal triterpenoidsIn vitro, the concentration of 80 μg/mL extract could induce RKO cell line apoptosis, IC50 was 34.14 μg/mLInhibits the proliferation of colon cancer RKO cells and induces the apoptosis of colon cancer RKO cells through the mitochondrial apoptosis pathway[68]
TriterpenesIn vitro, the concentration of 30 μg/mL extract could inhibit the proliferation of A549 cell line, IC50 was 109.9 μg/mLInhibition of the Nrf2-ARE signaling pathway can prolong the duration of metastasis from early to advanced lung cancer[69]
PAIn vitro, compared with 0 μg/mL group, 10, 20, 40, and 80 μg/mL groups could significantly increase the apoptosis rate of 786–0 renal carcinoma cellsInhibition of Wnt signaling pathway induced apoptosis in 786–0 renal carcinoma cells[70]
PAIn vitro, 20.0 μmol/L PA promoted the apoptosis of Caski cellsInhibit the survival of cervical cancer Caski cells and promote apoptosis by inhibiting TRIM29 expression and downregulating Wnt pathway activity[71]
PAIn vitro, 1, 2, 5 μmol/L PAC inhibited the proliferation and induced apoptosis of MDA-MB-231 cellsThe mechanism of action is related to the activation of PARP[72]
Poria ethanol extractPoria ethanol extract (at 150 μg/mL) could induce apoptosis of MDA-MB-231 cells with IC50 value of 2.13 ± 0.34 μg/mLBy inducing mitochondria and death receptors to mediate apoptosis; the arrest of the G0/G1 cell cycle promotes apoptosis[73]
PAIn vitro, PA inhibited the proliferation of sgc-70901 cells at the concentrations of 0, 20, 40, and 80 μMBlock the G0/G1 cell cycle[74]
PAIn vitro, 50 μg/mL PA can significantly reduce the proliferation of osteosarcoma cellsApoptosis is mediated in part by the PTEN/Akt signaling pathway and caspase 3/7 activity[75]
PACIn vitro, PAC (30, 40, 50 mg/mL) can significantly reduce the migration rate and increase the apoptosis rate of human cancer HeLa cells (IC50 is 60 mg/mL)The proapoptotic mechanism may be related to inhibition of phosphating of the ERK signaling pathway[52]
FMGPIn vitro, the concentration of FMGP at 400 μg/mL significantly inhibited the migration of highly metastatic human lung cancer cell line CL1-5 cellsBy inhibiting the TGFβRI mediated signaling pathway[53]
CMP3In vitro, the IC50 value was 26.34 ± 0.77, and the concentration of CMP3 was 100 μg/mL, which had the highest inhibitory rate on HepG2 cellsApoptosis is induced through the mitochondrial pathway and the death receptor pathway[54]
PPSW-1 and Sul-W-1The concentration of PPSW-1 and Sul-W-1 at 100 μg/mL had a strong inhibitory effect on the migration of MDA-MB-231 cells in vitroInhibition of the expression of the SATB1 gene reduces the migration ability of cancer cells[56]

Immune regulationTotal triterpenes of PoriaTotal triterpenes of Poria can improve the immune function of mice in vitro (at 40, 20, 10 μg/mL) and in vivo (at 400, 200, 100 mg/kg)[76]
S-CMPS-CMP (at 100, 200 mg/kg) showed immunoactivity in BALB/c mice[57]
Poria polysaccharidePoria polysaccharide has immunomodulatory activity in vivo (at 200 mg/kg) and in vitro (at 200 g/mL)Immunoregulatory activity is exerted through TLR4/TRAF6/NF-κB signaling pathway in vitro and in vivo[77]
Poria polysaccharidePoria polysaccharide had immunomodulatory activity in vitro (at 200 μg/mL)Immunoregulatory activity is exerted through Ca2+/PKC/p38/NF-κB signaling pathway in macrophages[78]

Effects on kidneyPoria polysaccharidePoria polysaccharide (at 50, 100, 200 mg/kg) significantly reduced the inflammatory response of diabetic nephropathy rats in vivo[79]
Poria polysaccharidesIn vivo Poria polysaccharides (at 200, 400 mg/kg) had a protective effect on acetaminophen-induced liver injury in miceInhibition of hepatocyte apoptosis and inflammatory stress induced by NF-κB pathway plays a protective role in the kidney[80]
WRPIn vivo, WRP (200 mg/kg) can inhibit the trend of renal cell apoptosis in the diabetic statesInhibition of Bax gene overexpression in renal tissue decreased apoptosis of renal cells[58]
PachymaranPachymaran can prevent renal interstitial fibrosis in rats with type 2 diabetic nephropathy in vivo at doses of 3, 6, and 12 mg/kg, respectively[81]
PPCIn vivo, PPC at 2 g/kg has anti-hyperuricemia activityUric acid excretion was increased by upregulating rOAT1 expression and downregulating rURAT1 expression[59]
Poricoic acid ZC, Poricoic acid ZD, and Poricoic acid ZEPoricoic acid ZC, poricoic acid ZD, and Poricoic acid ZE can prevent tubulointerstitial fibrosis in vivo (at 10 mg/kg) and in vitro (at 10 μM)By inhibiting the activation of the Wnt/β-catenin pathway and blocking Smad3 phosphorylation, renal tubulointerstitial fibrosis was reduced[82]
Poricoic acid ZG and Poricoic acid ZHPoricoic acid ZG and poricoic acid ZH (at 10 μM) can inhibit renal fibrosis in vitroAttenuate renal fibrosis via a Wnt/β-catenin pathway and targeted phosphorylation of smad3 signaling[83]
Poricoic acid APoricoic acid A (at 5, 10, 20 mg/kg) has diuretic activity in vivo[84]
Dehydroabietic acid methyl esterThe authors found that methyl dehydroabietic acid may be the diuretic substance of Poria[85]
Poria aqueous extractIn vivo, Poria aqueous extract can increase the urine volume of rabbits[86]

Hepatoprotective activityPoria polysaccharidesEffects of Poria polysaccharides on liver protection against acetaminophen-injured hepatocytes in vitro (at 200 and 400 mg/kg) and in vivo (at 20 and 40 g/L)Through the molecular mechanisms of reducing hepatocellular inflammatory stress and Hsp90 bioactivity[87]
Carboxymethyl pachymanCarboxymethyl pachyman in vivo (at 50 mg/kg) can alleviate liver injury of CT26 mice induced by 5-FUHepatoprotective activity through regulation of NF-κB, Nrf2-ARE and MAPK/P38/JNK pathways[88]

Effects on blood sugarPachymic acidIn vitro pachymic acid (at 1 μM) can increase glucose uptake in 3T3-L1 adipocytesHypoglycemic activity through regulation of PI3K and AMPK pathways[89]
WRPWRP (at 200 mg/kg) had hypoglycemic effects on NIDDM mice in vitro[90]
Insoluble polysaccharideInsoluble polysaccharide (at 1.0 g/kg and 0.5 g/kg) can improve the symptoms of hyperglycemia in ob/ob mice in vivoHypoglycemic activity through regulation of intestinal flora[91]

Antioxidant effectsCarboxymethyl sulfate Poria polysaccharideCarboxymethyl sulfate Poria polysaccharide had the strongest scavenging effect on OH and O2 and there was an agent-activity relationship. When the sample concentration was 4.5 mg/mL, the scavenging rates of OH and·O2 were 79% and 84.2%, respectively, which indicated that the sample had a certain antioxidant activity.[64]
PCP-MPCP-M polysaccharides (at 2.0 mg/mL) had antioxidant activity in vitro[60]
Carboxymethyl-pachymanIn vivo, carboxymethyl-pachyman (at 200 mg/kg) has antioxidant activity[92]

Anti-inflammatory effectsPoricoic acid AThe concentration of 10, 20, 50 μM showed anti-inflammatory activity in vitroAnti-inflammatory effects through downregulation of iNOS and COX-2 expression and inhibition of NO and PGE2 production[93]
PAIn vitro PA (at 25, 50, 100 mg/L) inhibits TNF-α-induced inflammation and oxidative stress damage in SH-SY5YIt may be a mechanism of action to inhibit apoptosis by downregulating Nrf2 of the ERK/Nrf2 signaling pathway into the nucleus[94]
Poricoic acid CPoricoic acid C (50, 100 μM) had anti-inflammatory activity on RAW264.7 cells stimulated by LPS in vitroInhibition of iNOS and COX-2 expression through downregulation of NF-κB exerts anti-inflammatory effects[30]
CMP33CMP33 (62.5–1000 μg/mL) has anti-inflammatory activity in vitroAnti-inflammatory activity by inhibiting the overproduction of NO, IL-6, TNF-α, and IL-1β in LPS-stimulated RAW264.7 cells[51]
Poria polysaccharideIn vivo, Poria polysaccharide (at 5, 100, 200 mg/kg) can reduce the infiltration degree of colitisAnti-inflammatory activity through inhibition of IL-33/ST2 signaling pathway activation[95]

Effects on the gut16α-Hydroxytrametenolic AcidIn vitro, 16α-hydroxytrametenolic Acid (60 μM) can improve intestinal barrier functionImproving intestinal barrier function via PI3K/Akt/NF-κB pathway[96]
Poria ethanol extractPoria ethanol extract (at 32 g/mL) inhibited intestinal contraction in vitroInhibits spontaneous and spastic contractions of the small intestine by inhibiting M receptors and regulating potassium and calcium channels[97]
Poria powder and water-soluble polysaccharideIn vivo, Poria powder (at 2.0 g/kg) and water-soluble polysaccharide (at 7.6 mg/kg) can protect against intestinal damage caused by cisplatinWater-soluble polysaccharides exert enteroprotective activity through intestinal flora and metabolic regulation[16]
Poria powderPoria powder (at 50 μg/kg) can increase the level of intestinal bifidobacteria in mice in vivo[98]

AntidepressantSulfated pachymaranIn vivo, sulfated pachymaran (25 mg/kg, 50 mg/kg, 100 mg/kg) had an antidepressant effect compared with the depression model groupAntidepressant activity through increased protein expression of p-CREB and BDNF[61]
PCWPW and PCWPSIn vivo, PCWPW and PCWPS (300 mg/kg) possess antidepressant-like effects[62]

Other biological activitiesTotal triterpenes and poricoic acid AIn vitro, the effects of total triterpenes and poricoic acid A on the inhibition of tyrosinase activity in cells increased with a rising concentration of 12.5 μg/mLPharmacological activity through inhibition of monophenolic and diphenolic enzyme activities in tyrosinase[99]
Poria ethanol extractPoria ethanol extract (at 100 μg/mL) can reduce the expression of tyrosinase and MITF in B16F10 in vitro, and applying 2% ointment containing Poria extract on cheeks in vivo can reduce the skin color valueBy regulating tyrosinase activity and MITF expression to reduce the production of melanin[100]
Poria chloroform extractPoria chloroform extract (at 2∼3 mg/mL) has a strong tyrosinase inhibition effect in vitroPoria chloroform extract can inhibit the activity of tyrosinase in the process of melanin production and effectively regulate the production of melanin, which is suitable for the development of whitening products for treating pigmented skin diseases[101]
PAPA (100 mg/kg) has significant neuroprotective effects on cerebral ischemia/reperfusion injury and neuronal apoptosis in vivoThe mechanism of action may be related to the activation of the PI3K/Akt signaling pathway[102]
Total triterpenes in Poria cocos peel (TTP)In vivo, TTP (100 mg/kg) has antiepileptic activity[103]
Poria aqueous extract, alcohol extract, and Poria polysaccharideIn vivo, Poria aqueous extract (at 30, 60, 120 mg/kg), Poria alcoholic extract (at 25, 50, 100 mg/kg), and Poria polysaccharide (at 10, 20, 40 mg/kg) protect against acute liver injury caused by carbon tetrachlorideProtects the liver by enhancing the liver's antioxidant capacity and reducing inflammation[104]