Melastoma malabathricum (L.) Smith Ethnomedicinal Uses, Chemical Constituents, and Pharmacological Properties: A Review

Table 4

Pharmacological properties of M. malabathricum according to its part.

Pharmacological activity	Pharmacological; assay used	Plant part	Types of extract	Dose (mg/kg) or; concentration (mg/mL)	Observations	Reference(s)
Acute toxicity	Signs of toxicity were observed for 48 h in orally fed mice	Leaves	Water extract	62.5, 125, 250, 500, 1000, and 2000 mg/kg; given orally	The WMML given to mice up to the dose of 2000 mg/kg showed neither mortality nor any visible clinical signs of general weakness in the animals	Sunilson et al. [61]
Antibacterial	Agar diffusion assay	Combination of leaf, stem, and flower	70% methanol extract	Concentration used was not clearly described 20 μL extract was poured into wells	The AMMMlsf was effective only against S. aureus, S. cerevisiae, and F. oxysporum but not E. coli.	Grosvenor et al. [8]
	Disc diffusion assay	Leaves	Methanol extract	Only 1.0 mg/mL extract used	The MMML exhibited poor antimicrobial activity only against B. subtilis, but not B. cereus, E. coli, P. aeruginosa, and C. albicans.	Wiart et al. [63]
	Agar cup assay	Different part (leaf, stem, bark, bulb, fruit and root)	Aqueous extract	100 μL of 200 mg/mL extracts was poured into wells	All extracts exerted antimicrobial activity.; The AMML exhibited the most effective antimicrobial activity.; The AMML was effective against B. brevis, V. cholerae, C. krusei, and B. subtilis, while the AMMBk was effective against S. aureus, B. brevis, and V. cholera.	Thatoi et al. [14]
	Agar-disc dilution assay	Leaves	Methanol, chloroform, and acetone extracts	0.01, 0.10, 1.00, and 10.00 μg/mL.; 1 mL of each extract was mixed with 19 mL of media and poured into petri dishes.; Mycelial discs were inoculated at the center of agar medium	The extracts showed antifungal activity against C. gloeosporioides.; The MIC value obtained for all extracts was 20.00 μg/mL.; The extracts also inhibited the sporulation of tested fungus	Johnny et al. [64]
	Agar well diffusion assay	Leaves	Water, benzene, and; acetone extracts	50 μL of 1.0 mg/mL; extract per well	All extracts possessed moderate antimicrobial activity against E. coli (MDR), S. aureus (MDR), K. pneumoniae, B. cereus, V. cholera, and C. albicans.; The MIC value for all extracts ranged between 0.65 and 0.80 mg/mL, while the MBC value was 0.90 mg/mL against V. cholera.; The MIC value for WMML and AcMML was 0.80 and 0.79 mg/mL, respectively, while the MBC value was 1.00 mg/mL against S. aureus (MDR).; Only AcMML produced the MIC value ranging between 0.62 and 0.80 mg/mL and the MBC value ranging between 0.70 and 0.90 mg/mL against E. coli (MDR), K. pneumoniae, C. albicans, and B. cereus.	Maji et al. [65]
	Agar well diffusion assay	Leaves	Methanol extract	The extract was tested in the concentrations of 0.5, 1.0, 2.0, 3.0, 4.0, 6.0, 8.0, and 16.0 mg/mL	The MMML exhibited antibacterial activity at the MIC value of 3.0 mg/mL for A, B, and D and 7.0 mg/mL for C clinical strains of S. aureus, respectively.; The MIC value recorded for the three clinical isolates of P. aeruginosa (A, B, and C) was 8.0 mg/mL.
	NA	Fruits	Methanol extract	NA	The MMMFr demonstrated antibacterial activity against B. subtilis, S. aureus, E. coli, and P. aeruginosa with MIC value ranging between 62.5 and 125.0 μg/mL	Koay [23]
Antiviral	In vitro cytopathic effect inhibition assay	Aerial part	Methanol extract	Not appropriately described; in text	The MMMAp showed moderate anti-HSV-1 activity with remarkable activity against Poliovirus.; The CC50 value of MMMAp against HSV-1 and Poliovirus was >1000 μg/mL or equal to 1000 μg/mL, respectively.; The EC50 value for MMMAp against HSV-1 virus at 20 TCID50 and 200 TCID50 was 192 and 706 μg/mL.; The EC50 value for MMMAp against Poliovirus at 20 TCID50 and 200 TCID50 was 111 and 225 μg/mL, respectively.	Lohézic-Le Dévéhat et al. [32]
	Three in vitro methods of treatment: (i) cells (C) were inoculated with virus (V) 1 hour before treatment with extract (E), that is (C + V) + E; (ii) virus was inoculated to cells one day after treatment with extract, that is (C + E) + V; (iii) the virus and extract were added concurrently to the cells, that is C + (V + E)	Leaves	Methanol extract	Not appropriately described in text The extract was diluted at 1.0 LC50, 0.1 LC50, and 0.01LC50	The MMML exerted antiviral activity with different modes of action against HSV-1 or measles viruses.; The MMML effectively inhibited cell death by 0.01 LC50 in HSV-1-inoculated cells treated using the ((C + V) + E) mode.; The MMML, at 0.1 and 1.0 LC50, increased the cells survival from viral infection when treated using the (C + (V + E)) mode.; The MMML exhibited no prophylactic effect on both test viruses when treated using the ((C + E) + V) mode	Nazlina et al. [55]
Antiparasitic	In vivo cotton ball-fungal mat assay	NA	Methanol extract	NA	The extract exhibited strong nematocidal activity with the recorded MED of approximately 5 mg/bl	Alen et al. [67]
Antioxidant	In vitro DPPH radical scavenging electron spin resonance (ESR) spectroscopic method	Flowers	Ethanol solution of crude ethyl acetate, and methanol extracts Naringenin, kaempferol and kaempferol-3-O-D-glucoside isolated from ethyl acetate extract Kaempferol-3-O-(2′′,6′′-di-O-p-trans-coumaroyl)-β-glucopyranoside and kaempferol-3-O-D-glucoside isolated from methanol extract	100 μl (1 mg/mL) ethanol solution of the test sample was added to 100 μl of DPPH (39.43 M) in ethanol solution and subjected to the assay	The MMMFw exerted a stronger free radical scavenger activity than the ethyl acetate extract.; Vitamin E and Vitamin C exerted antioxidant activity higher than naringenin, kaempferol, kaempferol-3-O-D-glucoside, kaempferol-3-O-(2′′,6:-di-O-p-trans-coumaroyl)-β-glucopyranoside.; The IC50 value for MMMFw, EAMMFw, naringenin, kaempferol, kaempferol-3-O-D-glucoside, kaempferol-3-O-(2′′,6′′-di-O-p-trans-coumaroyl)-β-glucopyranoside ranging between 6.59–35.8 μg/mL.	Susanti et al. [22]
	Two in vitro models: (i) Ferric thiocyanate (FTC) method; (ii) 2,2-diphenyl-1-picrylhydrazyl (DPPH) (UV and ESR spectroscopic) method	Leaves	n-Hexane, ethyl acetate and methanol extract Isolated compounds (e.g., α-amyrin, patriscabatrine and auranamide, quercetin, quercitrin, and kaempferol-3-O-(2′′,6′′-di-O-p-trans-coumaroyl) glucosides	The exact concentration used in the FTC assay was not appropriately described.; 4.0 mg of sample was mixed with a series of chemical solutions to achieved the final concentration of 0.02% w/v for the FTC assay.; The concentrations of test solutions used were 500, 250, 125, 62.5, 31.3, and 7.8 μg/mL in the DPPH assay	Kaempferol-3-O-(2′′,6′′-di-O-p-trans-coumaroyl) glucoside, kaempferol-3-O-β-D-glucose, kaempferol, hyperin, quercetin, and quercitrin showed strong antioxidative activity in the FTC method.; Quercetin was found to be the most active free radical scavenger in DPPH-UV and ESR method with IC50 of 0.69 and 0.65 μM, respectively, which was greater then vitamin E and vitamin C.	Susanti et al. [56]
	In vitro DPPH assay	Roots and shoots	Methanol extract	NA	The MMMR and MMMSt exhibited antioxidant activity with an IC50 value of 141.9 μg/mL and 154.5 μg/mL, respectively	Faravani [58]
Cytotoxic	In vitro MTT assay against two murine cancer cell lines (e.g., 3LL and L1210) and four human cancer lines (e.g., K562, U251, DU145, and MCF-7)	Aerial part	Methanol extract	Not appropriately described in text	The MMMAp demonstrated cytotoxic activity against 3LL, L1210, K562, DU145, U251, and MCF-7 with the IC50 value recorded ranging between 19>400 μg/mL.; The IC50 value was <25 μg/mL against both murine cell lines but >25 μg/mL against all human cancer cell lines.	Lohézic-Le Dévéhat et al. [32]
	In vitro MTT assay against MCF-7 cell line	Flowers	Ethyl acetate and methanol extracts Isolated compounds (e.g., naringenin, kaempferol and kaempferol-3-O-D-glucoside, kaempferol-3-O-(2′′,6′′-di-O-p-trans-coumaroyl)-β-glucopyranoside, and kaempferol-3-O-D-glucoside)	Not appropriately described in text	The 500 μg/mL EAMMFw, naringenin, and kaempferol-3-O-(2′′,6′′-di-O-p-trans-coumaroyl)-β-glucopyranoside, but not MMMFw, exerted cytotoxic activity against MCF-7 cells line.; The IC50 value for naringenin and kaempferol-3-O-(2′′,6′′-di-O-p-trans-coumaroyl)-β-glucopyranoside was 1.3 μM and 0.28 μM, respectively.; Kaempferol-3-O-(2′′,6′′-di-O-p-trans-coumaroyl)-β-glucopyranoside was more effective than tamoxifen	Susanti et al. [22]
	In vitro MTT assay against Vero (African green monkey, Cercopitheus aethiops kidney cells) and L929 (mouse fibroblast) cells lines	Leaves	Methanol extract	Concentration used were not clearly explained Different concentrations of extract were used and prepared using doubling dilutions from initial stock concentration of 1000 μg/mL	The MMML was not cytotoxic to both cells with LC50 values of 750 μg/mL and >1000 μg/mL, respectively	Nazlina et al. [55]
Anticoagulant	In vitro assay using the blood samples drawn from healthy volunteer donors (𝑛=36) of both genders (18–50 years old) The coagulation parameters measured using STA Compact coagulation analyzer were the activated partial thromboplastin time (aPTT), prothrombin time (PT), and thrombin time (TT) with cut-off time of 180 s Blood-clot-based assay with cut-off time of 300 s	Leaves	Hot water extract, cold water extract, and methanol extract	Concentrations ranging between 100 and 1000 μg/mL	The 1000 μg/mL hot-WMML prolonged aPTT, PT and TT in plasma but did not clot the plasma samples.; The cold-WMML and MMML also prolonged aPTT, PT, but both extracts did not affect the TT.; 100 to 1000 μg/mL hot-WMML prolonged aPTT in a concentration-dependent manner with anticoagulant activity recorded at the concentration beyond 400 μg/mL.; The hot-WMML did not exhibit blood clotting effect as indicated by prolonged aPTT beyond 300 s at 900 and 1000 μg/mL	Manicam et al. [68]
Platelet-activating factor (PAF) inhibitor	In vitro PAF binding to; rabbit platelets assay	Leaves	Methanol extract	200, 100, 50, 20 and 10 μg/mL	The MMML produced <10% inhibitory effect against PAF.	Jantan et al. [69]
	In vitro PAF binding to rabbit platelets assay	Leaves	α-Amyrin, betulinic acid, quercetin and quercitrin	Serial concentrationdilution range of 18.2–1.8 μg/mL (18.2, 9.1, 4.5, and 1.8 μg/mL)	At 18.2 μg/mL, all compounds exerted inhibitory action ranging between 40 to 70% with effectiveness seen in the sequence of α-amyrin, betulinic acid, quercetin, and quercitrin.; The IC50 value for α-amyrin, betulinic acid, quercetin, and quercitrin, ranged between 20.0 and 45.4 μM	Mazura et al. [70]
Wound healing	Two types of in vivo wound models in rats: (i) the excision wound model; (ii) the incision wound model	Leaves	Methanol extract in the; form of ointment	The extract was prepared as 5% ointment; applied topically	In the excision wound model: the MMML exhibited a wound healing activity by increasing wound contracting ability, wound closure time, tensile strength, and regeneration of tissues at the wound site; the time to wound closure of the nitrofurazone- and the MMML-treated groups was same (18±2 days).; In the incision wound studies: the MMML ointment increased the tensile strength of the 10-day-old wound; the MMML ointment also enhanced original tissue regeneration of the skin wounds with less fibrosis formation	Sunilson et al. [66]
Antiulcer	In vivo ethanol-induced gastric mucosal injuries in rats	Leaves	Aqueous extract	250 and 500 mg/kg; given orally	Macroscopically, the AMML reduced the formation of gastric mucosal injuries in a dose-dependent manner.; Microscopically, the 500 mg/kg AMML provided the best protection to the gastric mucosa in rats against ethanol-induced gastric ulcers	Hussain et al. [71]
Antidiarrheal	Four in vivo experimental models of diarrhea in mice: (i) model 1: mice were given test solutions and fecal materials were collected for 12 h after treatment, dried in an incubator and weighed; (ii) model 2: an overnight fasted male mouse was induced with diarrhea by oral administration of castor oil (0.5 mL/mouse, p.o.) 1 hour after the test solutions administration; (iii) model 3: the overnight fasted mice were subjected to the enteropooling assay method to find out the accumulation of intestinal fluid secretion evoked by MgSO4; (iv) model 4: the over night fasted animals were subjected to the gastrointestinal transit test and the distance travelled by the charcoal plug from pylorus to caecum was determined andexpressed as a percentage of the total length of the small intestine	Leaves	Water extract	100, 200, and 500 mg/kg; given orally	The WMML reduced the dried fecal output of the mice (model 1).; The WMML protected the mice against castor-oil-induced diarrheal droppings (model 2).; The WMML dose-dependently reduced the intestinal fluid secretion induced by MgSO4 (model 3).; The WMML inhibited the small intestinal motility of the charcoal marker in mice in a dose-dependent manner (model 4)	Sunilson et al. [61]
Antivenom	In vitro chick embryonic fibroblast cell lysis after H. laoticus scorpion venom treatment	Roots	Aqueous extracts	0.406 and 0.706 mg/mL	The AMMR only caused less than 40% antivenom efficiency at both doses tested	Uawonggul et al. [72]
Anti-inflammatory	In vivo carrageenan-induced; paw edema in rats	Leaves	Aqueous extract	10%, 50%, and 100% strength concentration (equivalent to the doses of 4.87, 24.35, and 48.7 mg/kg); given subcutaneously	The 10–100% AMML demonstrated anti-inflammatory activity in a concentration-independent manner.; The onset of anti-inflammatory action was observed 1 hour after the AMML subcutaneous administration.	Zakaria et al. [30]
	In vivo 12-O-tetradecanoylphorbol-13-acetate- (TPA-) induced mouse ear oedema assay		Pure compounds obtained from n-hexane, ethyl acetate and methanol extracts	20 μL of 0.5 mg/ear; applied topically	0.5 mg/mL kaempferol-3-O-(2′′,6′′-di-O-p-trans-coumaroyl) glucoside and α-amyrin demonstrated the strongest anti-inflammatory activity with the IC50 value of approximately 0.11 and 0.34 mM/ear, respectively.; No data on the anti-inflammatory effect of crude extracts were given for comparison with their pure compounds	Susanti et al. [56]
Antinociceptive	Two in vivo models: (i) acetic acid-induced abdominal constriction test in mice; (ii) hot plate test in mice	Stem barks and leaves	Ethanol extract	30, 100, and 300 mg/kg; given intraperitoneally	The EMMSbl demonstrated antinociceptive activity in a dose-dependent manner in both tests.; The ED50 recorded for the abdominal constriction test was approximately 100 mg/kg 5 mg/kg naloxone (a nonselective opioid antagonist; given intraperitoneally) inhibited the antinociceptive activity of extract in both tests	Sulaiman et al. [73]
	Three in vivo models: (i) acetic-acid-induced abdominal constriction test in mice; (ii) hot plate test in mice; (iii) formalin test in rats	Leaves	Aqueous extract	10%, 50%, and 100% strength concentration (equivalent to the doses of 4.87, 24.35, and 48.7 mg/kg); given subcutaneously	The AMML exerted antinociceptive activity in all three tests.; In the abdominal constriction- and hot plate-test, the AMML antinociceptive activity was observed in a concentration-independent manner.; In the formalin test, the AMML showed antinociceptive activity in both the early and late phases of the test with concentration-dependent activity seen only in the late phase of the test	Zakaria et al. [30]
Antipyretic	In vivo Brewer’s yeast- (BY-) induced pyrexia test in rats	Leaves	Aqueous extract	10%, 50%, and 100% strength concentration (equivalent to the doses of 4.87, 24.35, and 48.7 mg/kg); given subcutaneously	The AMML reduced temperature of pyrexia-induced rats for the first 6 hours after BY administration	Zakaria et al. [30]